Privileged scaffolds for library design and drug discovery

The evolving role of natural products in drug discovery

Koehn, F. E., & Carter, G. T. (2005) · Nature Reviews Drug Discovery · doi:10.1038/nrd1657 · Cited by 2,579

Target-Oriented and Diversity-Oriented Organic Synthesis in Drug Discovery

Schreiber, S. L. (2000) · Science · doi:10.1126/science.287.5460.1964 · Cited by 2,571

Drugs for bad bugs: confronting the challenges of antibacterial discovery

Payne, D. J., Gwynn, M. N., Holmes, D. J., & Pompliano, D. L. (2007) · Nature Reviews Drug Discovery · doi:10.1038/nrd2201 · Cited by 2,512

A Planning Strategy for Diversity‐Oriented Synthesis

Burke, M. D., & Schreiber, S. L. (2003) · Angewandte Chemie International Edition · doi:10.1002/anie.200300626 · Cited by 1,493

Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists

Evans, B., Rittle, K. E., Bock, M. G., DiPardo, R. M., Freidinger, R. M., Whitter, W. L., Lundell, G. F., Veber, D. F., Anderson, P., Chang, R. S. L., et al. (1988) · Journal of Medicinal Chemistry · doi:10.1021/jm00120a002 · Cited by 1,460

Exploiting Chemical Libraries, Structure, and Genomics in the Search for Kinase Inhibitors

Gray, N. S., Wodicka, L. M., Thunnissen, A. M. W. H., Norman, T., Kwon, S., Espinoza, F. H., Morgan, D. O., Barnes, G., Leclerc, S., Meijer, L., et al. (1998) · Science · doi:10.1126/science.281.5376.533 · Cited by 808

From Nature to Drug Discovery: The Indole Scaffold as a ‘Privileged Structure’

Alves, F. R. S., Barreiro, E. J., & Fraga, C. A. M. (2009) · Mini-Reviews in Medicinal Chemistry · doi:10.2174/138955709788452649 · Cited by 606

Diversity-oriented synthesis: Exploring the intersections between chemistry and biology

Tan, D. S. (2005) · Nature Chemical Biology · doi:10.1038/nchembio0705-74 · Cited by 605

Privileged Structures: Applications in Drug Discovery

DeSimone, R., Currie, K., Mitchell, S. A., Darrow, J. W., & Pippin, D. A. (2004) · Combinatorial Chemistry & High Throughput Screening · doi:10.2174/1386207043328544 · Cited by 579

Towards the Optimal Screening Collection: A Synthesis Strategy

Nielsen, T. E., & Schreiber, S. L. (2007) · Angewandte Chemie International Edition · doi:10.1002/anie.200703073 · Cited by 553

Metal-Free Nitrogenation of 2-Acetylbiphenyls: Expeditious Synthesis of Phenanthridines

Tang, C., Yuan, Y., & Jiao, N. (2015) · Organic Letters · doi:10.1021/acs.orglett.5b00797 · Cited by 61

Synthesis of Atropisomerically Defined, Highly Substituted Biaryl Scaffolds through Catalytic Enantioselective Bromination and Regioselective Cross‐Coupling

Gustafson, J. L., Lim, D., Barrett, K. T., & Miller, S. J. (2011) · Angewandte Chemie International Edition · doi:10.1002/anie.201101147 · Cited by 61

Multicomponent Assembly Strategies for the Synthesis of Diverse Tetrahydroisoquinoline Scaffolds

Granger, B. A., Kaneda, K., & Martin, S. F. (2011) · Organic Letters · doi:10.1021/ol201739u · Cited by 61

Visible‐Light‐Mediated 5‐exo‐dig Cyclizations of Amidyl Radicals

Reina, D. F., Dauncey, E. M., Morcillo, S. P., Svejstrup, T. D., Popescu, M. V., Douglas, J. J., Sheikh, N. S., & Leonori, D. (2017) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201601607 · Cited by 61

Recent Trends and Observations in the Design of High-Quality Screening Collections

Renner, S., Popov, M., Schuffenhauer, A., ROTH, H. ‐., Breitenstein, W., Marzinzik, A. L., Lewis, I., Krastel, P., Nigsch, F., Jenkins, J. L., et al. (2011) · Future Medicinal Chemistry · doi:10.4155/fmc.11.15 · Cited by 61

Construction of a Polyheterocyclic Benzopyran Library with Diverse Core Skeletons through Diversity-Oriented Synthesis Pathway

Oh, S., Jang, H. J., Ko, S. K., Ko, Y., & Park, S. B. (2010) · Journal of Combinatorial Chemistry · doi:10.1021/cc100044w · Cited by 60

Antimycobacterial activity of novel 1,2,4-oxadiazole-pyranopyridine/chromene hybrids generated by chemoselective 1,3-dipolar cycloadditions of nitrile oxides

Kumar, R. R., Perumal, S., Menéndez, J. C., Yogeeswari, P., & Sriram, D. (2011) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2011.04.033 · Cited by 60

Data Sets Representative of the Structures and Experimental Properties of FDA-Approved Drugs

Douguet, D. (2018) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.7b00462 · Cited by 59

Development of an engineered thermostable amine dehydrogenase for the synthesis of structurally diverse chiral amines

Liu, L., Wang, D., Chen, F., Zhang, Z., Chen, Q., Xu, J., Wang, Z., & Zheng, G. (2020) · Catalysis Science & Technology · doi:10.1039/d0cy00071j · Cited by 60

Synthetic approaches to oligomeric natural products

Snyder, S. A., ElSohly, A. M., & Kontes, F. (2011) · Natural Product Reports · doi:10.1039/c1np00001b · Cited by 61

Organophotoredox‐Catalyzed Late‐Stage Functionalization of Heterocycles

Hota, S. K., Jinan, D., Panda, S. P., Pan, R., Sahoo, B., & Murarka, S. (2021) · Asian Journal of Organic Chemistry · doi:10.1002/ajoc.202100234 · Cited by 59

Active machine learning-driven experimentation to determine compound effects on protein patterns

Naik, A. W., Kangas, J. D., Sullivan, D. P., & Murphy, R. F. (2016) · eLife · doi:10.7554/elife.10047 · Cited by 62

Selectivity On-Target of Bromodomain Chemical Probes by Structure-Guided Medicinal Chemistry and Chemical Biology

Galdeano, C., & Ciulli, A. (2016) · Future Medicinal Chemistry · doi:10.4155/fmc-2016-0059 · Cited by 59

Visible-light-mediated generation of nitrile oxides for the photoredox synthesis of isoxazolines and isoxazoles

Svejstrup, T. D., Zawodny, W., Douglas, J. J., Bidgeli, D., Sheikh, N. S., & Leonori, D. (2016) · Chemical Communications · doi:10.1039/c6cc06029c · Cited by 59

Computer-Aided Drug Design: An Overview

Talevi, A. (2018) · Methods in molecular biology · doi:10.1007/978-1-4939-7756-7_1 · Cited by 59

Visible-light-mediated minisci C–H alkylation of heteroarenes with 4-alkyl-1,4-dihydropyridines using O 2 as an oxidant

Dong, J., Yue, F., Xu, W., Song, H., Liu, Y., & Wang, Q. (2020) · Green Chemistry · doi:10.1039/d0gc02111c · Cited by 59

Cu-Catalyzed Cross-Coupling of Nitroarenes with Aryl Boronic Acids to Construct Diarylamines

Guan, X., Zhu, H., & Driver, T. G. (2021) · ACS Catalysis · doi:10.1021/acscatal.1c03113 · Cited by 59

Highly Efficient Cascade Reaction for Selective Formation of Spirocyclobutenes from Dienallenes via Palladium-Catalyzed Oxidative Double Carbocyclization–Carbonylation–Alkynylation

Qiu, Y., Yang, B., Zhu, C., & Bäckvall, J. (2016) · Journal of the American Chemical Society · doi:10.1021/jacs.6b09240 · Cited by 58

Nickel/NHC‐Catalyzed Enantioselective Cyclization of Pyridones and Pyrimidones with Tethered Alkenes

Shen, D., Zhang, W., Li, Z., Shi, S., & Xu, Y. (2020) · Advanced Synthesis & Catalysis · doi:10.1002/adsc.201901582 · Cited by 58

Biodiversity of small molecules – a new perspective in screening set selection

Petrone, P., Wassermann, A. M., Lounkine, E., Kutchukian, P. S., Simms, B., Jenkins, J. L., Selzer, P. M., & Glick, M. (2013) · Drug Discovery Today · doi:10.1016/j.drudis.2013.02.005 · Cited by 58

Silver-Nanoparticle-Catalyzed Dearomatization of Indoles toward 3-Spiroindolenines via a 5-exo-dig Spirocyclization

Schrӧder, F., Sharma, U. K., Mertens, M., Devred, F., Debecker, D. P., Luque, R., & der Eycken, E. V. V. (2016) · ACS Catalysis · doi:10.1021/acscatal.6b02443 · Cited by 58

Lead generation in crop protection research: a portfolio approach to agrochemical discovery

Loso, M. R., Garizi, N. V., Hegde, V. B., Hunter, J. E., & Sparks, T. C. (2016) · Pest Management Science · doi:10.1002/ps.4336 · Cited by 57

A general and practical bifunctional cobalt catalytic system for N-heterocycle assembly via acceptorless dehydrogenation

Tian, H., Xue, W., Wu, J., Yang, Z., Lu, H., & Tang, C. (2022) · Organic Chemistry Frontiers · doi:10.1039/d2qo00683a · Cited by 57

Catalytic remodeling of complex alkenes to oxonitriles through C=C double bond deconstruction

Cheng, Z., Huang, K., Wang, C., Chen, L., Li, X., Hu, Z., Shan, X., Cao, P., Sun, H., Chen, W., et al. (2025) · Science · doi:10.1126/science.adq8918 · Cited by 57

Privileged Structures - Dream or Reality: Preferential Organization of Azanaphthalene Scaffold

Polański, J., Kurczyk, A., Bąk, A., & Musioł, R. (2012) · Current Medicinal Chemistry · doi:10.2174/092986712800167356 · Cited by 59

Palladium‐Catalyzed Cascade Cyclization of Ynamides to Azabicycles

Greenaway, R. L., Campbell, C. D., Holton, O. T., Russell, C. A., & Anderson, E. A. (2011) · Chemistry - A European Journal · doi:10.1002/chem.201102880 · Cited by 57

Highly Stereoselective Synthesis of Natural‐Product‐Like Hybrids by an Organocatalytic/Multicomponent Reaction Sequence

Echemendía, R., de la Torre, A. F., Monteiro, J. L., Pila, M., Corrêa, A. G., Westermann, B., Rivera, D. G., & Paixão, M. W. (2015) · Angewandte Chemie International Edition · doi:10.1002/anie.201412074 · Cited by 57

Milde Rhodium(III)‐katalysierte Cyclisierung von Amiden mit α,β‐ungesättigten Aldehyden und Ketonen zu Azepinonen: Anwendung in der Synthese des Homoprotoberberin‐Gerüsts

Shi, Z., Grohmann, C., & Glorius, F. (2013) · Angewandte Chemie · doi:10.1002/ange.201301426 · Cited by 57

Computer-Aided Drug Discovery and Design: Recent Advances and Future Prospects

Talevi, A. (2023) · Methods in molecular biology · doi:10.1007/978-1-0716-3441-7_1 · Cited by 58

Design, synthesis and biological evaluation of 3-substituted 2,5-dimethyl-N-(3-(1H-tetrazol-5-yl)phenyl)pyrroles as novel potential HIV-1 gp41 inhibitors

He, X., Zou, P., Qiu, J., Hou, L., Jiang, S., Liu, S., & Xie, L. (2011) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2011.09.047 · Cited by 56

Perturbing pro-survival proteins using quinoxaline derivatives: A structure–activity relationship study

Rajule, R. N., Bryant, V. C., López-Bertoni, H., Luo, X., & Natarajan, A. (2012) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2012.02.022 · Cited by 56

Antifibrotic and anticancer action of 5-ene amino/iminothiazolidinones

Kaminskyy, D. V., den Hartog, G. J. M., Wojtyra, M., Lelyukh, M. I., Gzella, A. K., Bast, A., & Lesyk, R. (2016) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2016.02.011 · Cited by 56

Quinoline-based HIV Integrase Inhibitors

Musioł, R. (2013) · Current Pharmaceutical Design · doi:10.2174/1381612811319100008 · Cited by 57

A Short Review on Synthetic Advances toward the Synthesis of Rufinamide, an Antiepileptic Drug

Padmaja, R. D., & Chanda, K. (2018) · Organic Process Research & Development · doi:10.1021/acs.oprd.7b00373 · Cited by 55

Cycloisomerization of Olefins in Water

Matos, J. L. M., Green, S. A., Chun, Y., Dang, V. Q., Dushin, R. G., Richardson, P., Chen, J. S., Piotrowski, D. W., Paegel, B. M., & Shenvi, R. A. (2020) · Angewandte Chemie International Edition · doi:10.1002/anie.202003948 · Cited by 56

Deep Lead Optimization: Leveraging Generative AI for Structural Modification

Zhang, O., Lin, H., Zhang, H., Zhao, H., Huang, Y., Hsieh, C., Pan, P., & Hou, T. (2024) · Journal of the American Chemical Society · doi:10.1021/jacs.4c11686 · Cited by 64

Mechanism and Scope of Base‐Controlled Catalyst‐Free N‐Arylation of Amines with Unactivated Fluorobenzenes

Jacobsen, C. B., Meldal, M., & Diness, F. (2016) · Chemistry - A European Journal · doi:10.1002/chem.201604098 · Cited by 55

In vitro anticancer activity of pyrano[3, 2-c]chromene derivatives with both cell cycle arrest and apoptosis induction

El-Agrody, A. M., Fouda, A. M., Assiri, M. A., Mora, A., Tarik El-Sayed, A. L. I., Alam, M. M., & Alfaifi, M. Y. (2020) · Medicinal Chemistry Research · doi:10.1007/s00044-019-02494-3 · Cited by 55

Desulfonative photoredox alkylation of N -heteroaryl sulfones – an acid-free approach for substituted heteroarene synthesis

Wang, Z., Zheng, S., Matsui, J. K., Lu, Z., & Molander, G. A. (2019) · Chemical Science · doi:10.1039/c9sc00776h · Cited by 54

Linguistic measures of chemical diversity and the “keywords” of molecular collections

Woźniak, M., Wołos, A., Modrzyk, U., Górski, R. L., Winkowski, J., Bajczyk, M. D., Szymkuć, S., Grzybowski, B. A., & Eder, M. (2018) · Scientific Reports · doi:10.1038/s41598-018-25440-6 · Cited by 54

The piperazine scaffold for novel drug discovery efforts: the evidence to date

Romanelli, M. N., Manetti, D., Braconi, L., Dei, S., Gabellini, A., & Teodori, E. (2022) · Expert Opinion on Drug Discovery · doi:10.1080/17460441.2022.2103535 · Cited by 53

Discovery of Rezatapopt (PC14586), a First-in-Class, Small-Molecule Reactivator of p53 Y220C Mutant in Development

Vu, B. T., Dominique, R., Fahr, B. J., Li, H. H., Fry, D. C., Xu, L., Yang, H. Y., Puzio‐Kuter, A. M., Good, A. C., Liu, B., et al. (2024) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.4c00379 · Cited by 57

Design, synthesis and molecular modeling studies of novel thiazolidine-2,4-dione derivatives as potential anti-cancer agents

Asati, V., & Bharti, S. K. (2017) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2017.10.077 · Cited by 53

Catalytic Asymmetric Synthesis of α‐Arylpyrrolidines and Benzo‐fused Nitrogen Heterocycles

Dai, X., Engl, O. D., León, T., & Buchwald, S. L. (2019) · Angewandte Chemie International Edition · doi:10.1002/anie.201814331 · Cited by 53

Characterization of Drug-like Chemical Space for Cytotoxic Marine Metabolites Using Multivariate Methods

Jagannathan, R. (2019) · ACS Omega · doi:10.1021/acsomega.8b01764 · Cited by 53

Rational Development of Remote C−H Functionalization of Biphenyl: Experimental and Computational Studies

Fan, Z., Bay, K. L., Chen, X., Zhuang, Z., Park, H. S., Yeung, K., Houk, K. N., & Yu, J. (2020) · Angewandte Chemie International Edition · doi:10.1002/anie.201915624 · Cited by 53

Carboxyboronate: A Versatile C1 Building Block

Holownia, A., Tien, C., Diaz, D. B., Larson, R. T., & Yudin, A. K. (2019) · Angewandte Chemie International Edition · doi:10.1002/anie.201907486 · Cited by 52

Domino transformation of isoxazoles to 2,4-dicarbonylpyrroles under Fe/Ni relay catalysis

Galenko, E. E., Galenko, A. V., Khlebnikov, A. F., & Novikov, M. S. (2015) · RSC Advances · doi:10.1039/c5ra01889g · Cited by 52

Selective Kumada biaryl cross-coupling reaction enabled by an iron(iii) alkoxide–N-heterocyclic carbene catalyst system

Chua, Y., & Duong, H. A. (2014) · Chemical Communications · doi:10.1039/c4cc02930e · Cited by 52

Pyridine Based Antitumour Compounds Acting at the Colchicine Site

Álvarez, R., Aramburu, L., Puebla, P., Caballero, E., González, M., Vicente, A. A., Medarde, M., & Peláez, R. (2016) · Current Medicinal Chemistry · doi:10.2174/092986732311160420104823 · Cited by 52

An iron-catalysed C–C bond-forming spirocyclization cascade providing sustainable access to new 3D heterocyclic frameworks

Adams, K., Ball, A. K., Birkett, J., Brown, L., Chappell, B. G. N., Gill, D. M., Lo, P. K. T., Patmore, N. J., Rice, C. R., Ryan, J., et al. (2016) · Nature Chemistry · doi:10.1038/nchem.2670 · Cited by 52

Lewis Base–Boryl Radicals Enabled the Desulfurizative Reduction and Annulation of Thioamides

Yu, Y., Zhang, F., Cheng, J. L., Hei, J., Deng, W., & Wang, Y. (2017) · Organic Letters · doi:10.1021/acs.orglett.7b03201 · Cited by 52

Gold(I)-Catalyzed Enantioselective Annulations between Allenes and Alkene-Tethered Oxime Ethers: A Straight Entry to Highly Substituted Piperidines and aza -Bridged Medium-Sized Carbocycles

Marcote, D. C., Varela-Aneiros, I., Fernández-Casado, J., Mascarenas, J. L., & López, F. (2018) · Journal of the American Chemical Society · doi:10.1021/jacs.8b10388 · Cited by 52

Iridium‐Catalyzed Silylation of Five‐Membered Heteroarenes: High Sterically Derived Selectivity from a Pyridyl‐Imidazoline Ligand

Karmel, C., Rubel, C., Kharitonova, E. V., & Hartwig, J. F. (2020) · Angewandte Chemie International Edition · doi:10.1002/anie.201916015 · Cited by 52

Domino reactions in water: diastereoselective synthesis of densely functionalized indolyldihydrofuran derivatives

Gunasekaran, P., Balamurugan, K., Sivakumar, S., Perumal, S., Menéndez, J. C., & Almansour, A. I. (2012) · Green Chemistry · doi:10.1039/c2gc16517a · Cited by 51

Recent Advances on the C2-Functionalization of Indole via Umpolung

Deka, B., Deb, M. L., & Baruah, P. K. (2020) · Topics in Current Chemistry · doi:10.1007/s41061-020-0287-7 · Cited by 51

Exploring and mapping chemical space with molecular assembly trees

Liu, Y., Mathis, C., Bajczyk, M. D., Marshall, S. M., Wilbraham, L., & Cronin, L. (2021) · Science Advances · doi:10.1126/sciadv.abj2465 · Cited by 49

Solvent-free synthesis of new spiropyrroloindole compounds using Fe3O4/TiO2/MWCNTs MNCs via multicomponent reactions: assessment of new spiropyrroloindole antioxidant activity

Hezarcheshmeh, N. K., & Azizian, J. (2022) · Molecular Diversity · doi:10.1007/s11030-021-10311-6 · Cited by 51

A General and Practical Route to Functionalized Bicyclo[1.1.1]Pentane‐Heteroaryls Enabled by Photocatalytic Multicomponent Heteroarylation of [1.1.1]Propellane

Huang, W., Keeß, S., & Molander, G. A. (2023) · Angewandte Chemie International Edition · doi:10.1002/anie.202302223 · Cited by 51

2,3-Dihydrobenzofuran privileged structures as new bioinspired lead compounds for the design of mPGES-1 inhibitors

Micco, S. D., Spatafora, C., Cardullo, N., Riccio, R., Fischer, K., Pergola, C., Koeberle, A., Werz, O., Chalal, M., Fasseur, D., et al. (2016) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2016.01.002 · Cited by 50

Regiodivergent Intramolecular Nucleophilic Addition of Ketimines for the Diverse Synthesis of Azacycles

Wang, Y., Tian, J., Tan, P., Cao, Q., Zhang, X., Cao, Z., Zhou, F., Wang, X., & Zhou, J. E. (2019) · Angewandte Chemie International Edition · doi:10.1002/anie.201910864 · Cited by 51

Design, click conventional and microwave syntheses, DNA binding, docking and anticancer studies of benzotriazole-1,2,3-triazole molecular hybrids with different pharmacophores

Al‐Raqa, S. Y., Alharbi, K., Aljuhani, A., Rezki, N., Aouad, M. R., & Ali, I. (2020) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2020.129192 · Cited by 51

Facile Construction of Structurally Diverse Thiazolidinedione-Derived Compounds via Divergent Stereoselective Cascade Organocatalysis and Their Biological Exploratory Studies

Zhang, Y., Wang, S., Wu, S., Zhu, S., Dong, G., Miao, Z., Yao, J., Zhang, W., Sheng, C., & Wang, W. (2013) · ACS Combinatorial Science · doi:10.1021/co400022r · Cited by 51

1,2,3,4-Tetrahydroisoquinoline (THIQ) as privileged scaffold for anticancer de novo drug design

Faheem, F., Kumar, B. K., Sekhar, K. V. G. C., Chander, S., Kunjiappan, S., & Murugesan, S. (2021) · Expert Opinion on Drug Discovery · doi:10.1080/17460441.2021.1916464 · Cited by 52

Medium‐Ring Nitrogen Heterocycles through Migratory Ring Expansion of Metalated Ureas

Hall, J. E., Matlock, J. V., Ward, J. W., Gray, K. V., & Clayden, J. (2016) · Angewandte Chemie · doi:10.1002/ange.201605714 · Cited by 50

Pesticide Informatics Platform (PIP): An International Platform for Pesticide Discovery, Residue, and Risk Evaluation

Mei, L., Chen, H., Dong, A.-Y., Huang, G.-Y., Liu, Y.-W., Zhang, X., Wang, W., Hao, G., & Yang, G. (2022) · Journal of Agricultural and Food Chemistry · doi:10.1021/acs.jafc.2c02141 · Cited by 50

Scaffold Flatness: Reversing the Trend

Tajabadi, F. M., Campitelli, M. R., & Quinn, R. J. (2013) · Springer Science Reviews · doi:10.1007/s40362-013-0014-7 · Cited by 51

Discovery and verification of the potential targets from bioactive molecules by network pharmacology-based target prediction combined with high-throughput metabolomics

Zhang, A., Fang, H., Wang, Y., Yan, G., Sun, H. J., Zhou, X., Wang, Y., Liu, L., & Wang, X. (2017) · RSC Advances · doi:10.1039/c7ra09522h · Cited by 49

Oxidative Condensations To Form Benzimidazole-Substituted Potassium Organotrifluoroborates

Molander, G. A., & Ajayi, K. (2012) · Organic Letters · doi:10.1021/ol301956p · Cited by 49

Ligand specificity, privileged substructures and protein druggability from fragment-based screening

Barelier, S., & Krimm, I. (2011) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2011.02.020 · Cited by 49

Strategies of multi-objective optimization in drug discovery and development

Nicolotti, O., Giangreco, I., Introcaso, A., Leonetti, F., Stefanachi, A., & Carotti, A. (2011) · Expert Opinion on Drug Discovery · doi:10.1517/17460441.2011.588696 · Cited by 48

New Linearly and Angularly Fused Quinazolinones: Synthesis through Gold(I)‐Catalyzed Cascade Reactions and Anticancer Activities

Patil, N. T., Lakshmi, P. G. V. V., Sridhar, B., Patra, S., Bhadra, M. P., & Patra, C. R. (2012) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201101822 · Cited by 49

[Histamine release and cardiovascular reactions to implantation of bone cement during total hip replacement].

Tryba, M., Linde, I., Voshage, G., & Zenz, M. (1991) · PubMed · Cited by 49

Ruthenium(II)-Catalyzed Regioselective 1,2-Hydrosilylation of N-Heteroarenes and Tetrel Bonding Mechanism

Behera, D., Thiyagarajan, S., Anjalikrishna, P. K., Suresh, C. H., & Gunanathan, C. (2021) · ACS Catalysis · doi:10.1021/acscatal.1c01148 · Cited by 48

The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity

Robertson, M. J., Hadzic, G., Ambrus, J. I., Pomè, D. Y., Hyde, E. D. E. R., Whiting, A., Mariana, A., von Kleist, L., Chau, N., Haucke, V., et al. (2012) · ACS Medicinal Chemistry Letters · doi:10.1021/ml200284s · Cited by 48

Semi-synthesis of acylated triterpenes from olive-oil industry wastes for the development of anticancer and anti-HIV agents

Parra, A., Martin-Fonseca, S., Rivas, F., Reyes‐Zurita, F. J., Medina‐O’Donnell, M., Martı́nez, A., García‐Granados, A., Lupiáñez, J. A., & Alberício, F. (2014) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2013.12.049 · Cited by 48

Synthesis and biological activities of the respiratory chain inhibitor aurachin D and new ring versus chain analogues

Li, X., Herrmann, J. E., Zang, Y., Grellier, P., Prado, S., Müller, R., & Nay, B. (2013) · Beilstein Journal of Organic Chemistry · doi:10.3762/bjoc.9.176 · Cited by 48

Indanes—Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors

Vilums, M., Heuberger, J. A. A. C., Heitman, L. H., & IJzerman, A. P. (2015) · Medicinal Research Reviews · doi:10.1002/med.21352 · Cited by 49

Palladium‐Catalyzed Regioselective Synthesis of 1,2‐Fused Indole‐Diazepines via [5+2] Annulation of o‐Indoloanilines with Alkynes

Thikekar, T. U., & Sun, C. (2017) · Advanced Synthesis & Catalysis · doi:10.1002/adsc.201700741 · Cited by 48

Late‐Stage Alkylation of Heterocycles Using N‐(Acyloxy)phthalimides

Parida, S. K., Hota, S. K., Kumar, R., & Murarka, S. (2021) · Chemistry - An Asian Journal · doi:10.1002/asia.202100151 · Cited by 48

Electrochemical Dearomatization of Indoles: Access to Diversified Fluorine-Containing Spirocyclic Indolines

Mo, K., Zhou, X., Wu, J., & Zhao, Y. (2022) · Organic Letters · doi:10.1021/acs.orglett.2c00530 · Cited by 47

Catalyst-free visible-light-induced decarbonylative C–H alkylation of quinoxalin-2(1 H )-ones

Shi, X., Cao, Y., Liu, Y., Niu, K., Song, H., Zhang, J., & Wang, Q. (2023) · Organic Chemistry Frontiers · doi:10.1039/d2qo02019j · Cited by 47

Design and synthesis of 2-aminothiazole based antimicrobials targeting MRSA

Annadurai, S., Martinez, R. L., Canney, D. J., Eidem, T. M., Dunman, P. M., & Abou-Gharbia, M. A. (2012) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2012.09.095 · Cited by 47

Identification of a novel class of quinoline–oxadiazole hybrids as anti-tuberculosis agents

Jain, P. P., Degani, M. S., Raju, A., Anantram, A., Seervi, M., Sathaye, S. S., Ray, M., & Rajan, M. G. R. (2015) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2015.11.057 · Cited by 47

Amplification of Trichloroisocyanuric Acid (TCCA) Reactivity for Chlorination of Arenes and Heteroarenes via Catalytic Organic Dye Activation

Rogers, D. A., Bensalah, A. T., Espinosa, A. T., Hoerr, J. L., Refai, F. H., Pitzel, A. K., Alvarado, J. J., & Lamar, A. A. (2019) · Organic Letters · doi:10.1021/acs.orglett.9b01414 · Cited by 47

Zebrafish as an Emerging Model for Bioassay-Guided Natural Product Drug Discovery for Neurological Disorders

Pitchai, A., Rajaretinam, R. K., & Freeman, J. L. (2019) · Medicines · doi:10.3390/medicines6020061 · Cited by 49

Selectivity in the Elaboration of Bicyclic Borazarenes

Bhattacharjee, A., Davies, G. H. M., Saeednia, B., Wisniewski, S. R., & Molander, G. A. (2020) · Advanced Synthesis & Catalysis · doi:10.1002/adsc.202001384 · Cited by 46

Bridged bicyclic peptides as potential drug scaffolds: synthesis, structure, protein binding and stability

Bartoloni, M., Jin, X., Marcaida, M. J., Banha, J., Bonaventura, I. D., Bongoni, S., Bartho, K., Gräbner, O., Sefkow, M., Darbre, T., et al. (2015) · Chemical Science · doi:10.1039/c5sc01699a · Cited by 46

Catalytic Enantioselective Synthesis of a cis-β-Boronyl Cyclobutylcarboxyester Scaffold and Its Highly Diastereoselective Nickel/Photoredox Dual-Catalyzed Csp3–Csp2 Cross-Coupling to Access Elusive trans-β-Aryl/Heteroaryl Cyclobutylcarboxyesters

Nguyen, K., Clement, H. A., Bernier, L., Coe, J. W., Farrell, W. P., Helal, C. J., Reese, M. R., Sach, N. W., Lee, J. C., & Hall, D. G. (2020) · ACS Catalysis · doi:10.1021/acscatal.0c04520 · Cited by 46

Synthesis and characterization of nickel complex anchored onto MCM-41 as a novel and reusable nanocatalyst for the efficient synthesis of 2,3-dihydroquinazolin-4(1H)-ones

Havasi, F., Ghorbani‐Choghamarani, A., & Nikpour, F. (2015) · Microporous and Mesoporous Materials · doi:10.1016/j.micromeso.2015.10.036 · Cited by 45

The Purchasable Chemical Space: A Detailed Picture

Lucas, X., Grüning, B. A., Bleher, S., & Günther, S. (2015) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.5b00116 · Cited by 46

Mild Cobalt‐Catalyzed Negishi Cross‐Couplings of (Hetero)arylzinc Reagents with (Hetero)aryl Halides

Haas, D., Hammann, J. M., Lutter, F. H., & Knochel, P. (2016) · Angewandte Chemie International Edition · doi:10.1002/anie.201510665 · Cited by 45

Alkene Dioxygenation with Malonoyl Peroxides: Synthesis of γ-Lactones, Isobenzofuranones, and Tetrahydrofurans

Alamillo‐Ferrer, C., Karabourniotis‐Sotti, M., Kennedy, A. R., Campbell, M. J., & Tomkinson, N. C. O. (2016) · Organic Letters · doi:10.1021/acs.orglett.6b01253 · Cited by 45

Design, synthesis and DNA-binding study of some novel morpholine linked thiazolidinone derivatives

War, J. A., Srivastava, S. K., & Srivastava, S. K. (2016) · Spectrochimica Acta Part A Molecular and Biomolecular Spectroscopy · doi:10.1016/j.saa.2016.07.054 · Cited by 45

Organocatalytic, enantioselective synthesis of benzoxaboroles via Wittig/oxa-Michael reaction Cascade of α-formyl boronic acids

Hazra, G., Maity, S., Bhowmick, S., & Ghorai, P. (2017) · Chemical Science · doi:10.1039/c6sc04522g · Cited by 45

Synthesis of N -Fused Polycyclic Indoles via Ligand-Free Palladium-Catalyzed Annulation/Acyl Migration Reaction

Dong, Z., Zhang, X., Li, W., Li, Z., Wang, W., Zhang, Y., Liu, W., & Liu, W.-B. (2019) · Organic Letters · doi:10.1021/acs.orglett.8b04128 · Cited by 45

Synthesis of DNA-coupled isoquinolones and pyrrolidines by solid phase ytterbium- and silver-mediated imine chemistry

Potowski, M., Kunig, V. B. K., Losch, F., & Brunschweiger, A. (2019) · MedChemComm · doi:10.1039/c9md00042a · Cited by 45

Asymmetric Hydrogenation of Dibenzo[c,e]azepine Derivatives with Chiral Cationic Ruthenium Diamine Catalysts

Zhang, S., Chen, F., He, Y., & Fan, Q. (2019) · Organic Letters · doi:10.1021/acs.orglett.9b01859 · Cited by 45

The 2,11-Cyclized Cembranoids: Cladiellins, Asbestinins, and Briarellins (Period 1998–2010)

Welford, A. J., & Collins, I. (2011) · Journal of Natural Products · doi:10.1021/np200125v · Cited by 45

Synthesis of Alkyl Aryl(heteroaryl)acetates from N-Oxides, 1,1-Difluorostyrenes, and Alcohols

Loska, R., Szachowicz, K., & Szydlik, D. (2013) · Organic Letters · doi:10.1021/ol402735m · Cited by 45

Privileged heterocyclic scaffolds in chemical biology and drug discovery: synthesis and bioactivity

Altomare, C. (2017) · Chemistry of Heterocyclic Compounds · doi:10.1007/s10593-017-2046-4 · Cited by 8

Privileged Structures Revisited

Schneider, P., & Schneider, G. (2017) · Angewandte Chemie International Edition · doi:10.1002/anie.201702816 · Cited by 127

Privileged Structures and Motifs (Synthetic and Natural Scaffolds)

Jones, A. M. (2016) · Elsevier eBooks · doi:10.1016/b978-0-12-409547-2.12316-9 · Cited by 4

Privileged Structures: Applications in Drug Discovery

DeSimone, R., Currie, K., Mitchell, S. A., Darrow, J. W., & Pippin, D. A. (2004) · Combinatorial Chemistry & High Throughput Screening · doi:10.2174/1386207043328544 · Cited by 579

Scaffold composition and biological relevance of screening libraries

Shelat, A. A., & Guy, R. K. (2007) · Nature Chemical Biology · doi:10.1038/nchembio0807-442 · Cited by 170