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 C-3 chalcogenation (sulfenylation and selenylation) of 4 H -pyrido[1,2- a ]pyrimidin-4-ones

Ghosh, P., Chhetri, G., & Das, S. (2021) · RSC Advances · doi:10.1039/d1ra00834j · Cited by 26

Synthetic applications of α,α-difluoroarylacetic acids and salts via decarboxylative functionalization

Mei, W., Kong, Y., & Yan, G. (2021) · Organic Chemistry Frontiers · doi:10.1039/d1qo00775k · Cited by 26

Synthesis of oxindoles bearing a stereogenic 3-fluorinated carbon center from 3-fluorooxindoles

Liu, Y., Wang, X. P., Wei, J., & Li, Y. (2021) · Organic & Biomolecular Chemistry · doi:10.1039/d1ob01964c · Cited by 26

Recent advances in the tandem copper-catalyzed Ullmann–Goldberg N -arylation–cyclization strategies

Honnanayakanavar, J. M., Obulesu, O., & Suresh, S. (2022) · Organic & Biomolecular Chemistry · doi:10.1039/d2ob00082b · Cited by 26

Enzymatic and Chemoenzymatic Three‐Step Cascades for the Synthesis of Stereochemically Complementary Trisubstituted Tetrahydroisoquinolines

Erdmann, V., Lichman, B. R., Zhao, J., Simon, R. C., Kroutil, W., Ward, J. M., Hailes, H. C., & Rother, D. (2017) · Angewandte Chemie · doi:10.1002/ange.201705855 · Cited by 26

Carboxyboronate: A Versatile C1 Building Block

Holownia, A., Tien, C., Diaz, D. B., Larson, R. T., & Yudin, A. K. (2019) · Angewandte Chemie · doi:10.1002/ange.201907486 · Cited by 26

Diverse synthesis of α-tertiary amines and tertiary alcohols via desymmetric reduction of malonic esters

Liu, H., Lau, V. H. M., Xu, P., Chan, T. H., & Huang, Z. (2022) · Nature Communications · doi:10.1038/s41467-022-32560-1 · Cited by 26

Advances in Nickel-Catalyzed O-Arylation of Aliphatic Alcohols and Phenols with (Hetero)aryl Electrophiles

Stradiotto, M., & Morrison, K. M. (2023) · Synthesis · doi:10.1055/a-2134-0450 · Cited by 26

Green Synthesis and Theoretical Study of New Imidazopyrimidine Derivatives via One‐Pot Multicomponent Reactions

Ezzatzadeh, E., Mohammadi, M., Hossaini, Z., & Khandan, S. (2023) · ChemistrySelect · doi:10.1002/slct.202302491 · Cited by 26

Facile construction of 3-indolochromenes and 3-indoloxanthenes via EDDF catalyzed one-pot three component reactions

Thakur, A., Reddy, P. L., Tripathi, M., & Rawat, D. S. (2015) · New Journal of Chemistry · doi:10.1039/c5nj01288k · Cited by 26

Diverse synthesis of natural product inspired fused and spiro-heterocyclic scaffolds via ring distortion and ring construction strategies

Bathula, C., Dangi, P., Hati, S., Agarwal, R., Munshi, P., Singh, A., Singh, S., & Sen, S. (2015) · New Journal of Chemistry · doi:10.1039/c5nj01858g · Cited by 26

A chemo-centric view of human health and disease

Duran‐Frigola, M., Rossell, D., & Aloy, P. (2014) · Nature Communications · doi:10.1038/ncomms6676 · Cited by 28

Synthesis of Dibenzodiazepinones via Tandem Copper(I)‐ Catalyzed CN Bond Formation

Gawande, S. D., Kavala, V., Zanwar, M. R., Kuo, C., Huang, W., Kuo, T., Huang, H., He, C., & Yao, C. (2014) · Advanced Synthesis & Catalysis · doi:10.1002/adsc.201301020 · Cited by 26

A new, one-pot, multicomponent synthesis of 5-aza-9-deaza-adenines under microwave irradiation

Lim, F. P. L., Luna, G., & Dolzhenko, A. V. (2014) · Tetrahedron Letters · doi:10.1016/j.tetlet.2014.07.105 · Cited by 26

Regioselective dibromination of methyl indole-3-carboxylate and application in the synthesis of 5,6-dibromoindoles

Parsons, T. B., Ghellamallah, C., Male, L., Spencer, N., & Grainger, R. S. (2011) · Organic & Biomolecular Chemistry · doi:10.1039/c1ob05522d · Cited by 26

Solid-phase synthesis of tetrasubstituted pyrrolo[2,3-d]pyrimidines

Lee, J. H., & Lim, H. (2012) · Organic & Biomolecular Chemistry · doi:10.1039/c2ob06899k · Cited by 27

Cascade fluorofunctionalisation of 2,3-unsubstituted indoles by means of electrophilic fluorination

Nguyen, T. M., Duong, H. A., Richard, J., Johannes, C. W., Pincheng, F., Ye, D. K. J., & Shuying, E. L. (2013) · Chemical Communications · doi:10.1039/c3cc46564k · Cited by 26

A continuous-flow synthesis of 1,4-benzodiazepin-5-ones, privileged scaffolds for drug discovery

Viviano, M., Milite, C., Rescigno, D., Castellano, S., & Sbardella, G. (2014) · RSC Advances · doi:10.1039/c4ra13392g · Cited by 26

An Efficient One-Pot Synthesis of Densely Functionalized Fused-Quinolines via Sequential Ugi4CC and Acid-Mediated Povarov-Type Reaction

Ghoshal, A., Yugandhar, D., Nanubolu, J. B., & Srivastava, A. K. (2017) · ACS Combinatorial Science · doi:10.1021/acscombsci.7b00095 · Cited by 26

Synthesis of d -(+)-camphor-based N -acylhydrazones and their antiviral activity

Kovaleva, K. S., Zubkov, F. I., Бормотов, Н. И., Новиков, Р. А., Дороватовский, П. В., Khrustalev, V. N., Gatilov, Y. V., Zarubaev, V. V., Yarovaya, О. I., Николаевна, Ш. Л., et al. (2018) · MedChemComm · doi:10.1039/c8md00442k · Cited by 26

Au(I)-Catalyzed Synthesis of Trisubstituted Indolizines from 2-Propargyloxypyridines and Methyl Ketones

Rossler, M. D., Hartgerink, C., Zerull, E. E., Boss, B. L., Frndak, A. K., Mason, M. M., Nickerson, L. A., Romero, E. O., de Burg, J. E. V., Staples, R. J., et al. (2019) · Organic Letters · doi:10.1021/acs.orglett.9b01929 · Cited by 26

Construction of Polyheterocyclic Benzopyran Library with Diverse Core Skeletons through Diversity-Oriented Synthesis Pathway: Part II

Zhu, M., Lim, B. J., Koh, M., & Park, S. B. (2011) · ACS Combinatorial Science · doi:10.1021/co2001907 · Cited by 26

Green synthesis and theoretical study of new 1,3,4‐oxadiazoles: Application of Cu/Fe3O4@MWCNT magnetic nanocomposites

Ezzatzadeh, E., Mohammadi, M., Ghambarian, M., & Hossaini, Z. (2023) · Applied Organometallic Chemistry · doi:10.1002/aoc.7252 · Cited by 25

Synthesis and studies on gem-fluorinated 2-azabicyclo[n.1.0]alkanes

Kubyshkin, V., Kheylik, Y., & Mykhailiuk, P. K. (2015) · Journal of Fluorine Chemistry · doi:10.1016/j.jfluchem.2015.03.008 · Cited by 25

Green and Facile Assembly of Diverse Fused N-Heterocycles Using Gold-Catalyzed Cascade Reactions in Water

Jia, X., Li, P., Liu, X., Lin, J., Chu, Y., Yu, J., Wang, J., Liu, H., & Zhao, F. (2019) · Molecules · doi:10.3390/molecules24050988 · Cited by 25

Electrochemical synthesis of oxazoles via a phosphine-mediated deoxygenative [3 + 2] cycloaddition of carboxylic acids

Zhang, X., Yuan, Q., Zhang, H., Shen, Z., Zhao, L., Yang, C., Guo, L., & Xia, W. (2023) · Green Chemistry · doi:10.1039/d2gc04559a · Cited by 25

Sterically Constrained and Encumbered: An Approach to the Naturally Occurring Peptidomimetic Tetrahydropyrazino[1,2‐a]indole‐1,4‐dione Core

Golubev, P., & Krasavin, M. (2017) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201700152 · Cited by 25

A thiocyanopalladation/carbocyclization transformation identified through enzymatic screening: stereocontrolled tandem C–SCN and C–C bond formation

Malik, G., Swyka, R. A., Tiwari, V. K., Fei, X., Applegate, G. A., & Berkowitz, D. B. (2017) · Chemical Science · doi:10.1039/c7sc04083k · Cited by 25

Microwave Controlled Reductive Cyclization: A Selective Synthesis of Novel Benzimidazole-alkyloxypyrrolo[1,2-a]quinoxalinones

Dhole, S., Selvaraju, M., Maiti, B., Chanda, K., & Sun, C. (2015) · ACS Combinatorial Science · doi:10.1021/acscombsci.5b00010 · Cited by 24

Ugi-Based Approaches to Quinoxaline Libraries

Azuaje, J., Maatougui, A. E., Xerardo Garcia-mera, B., & Sotelo, E. (2014) · ACS Combinatorial Science · doi:10.1021/co500036n · Cited by 24

The Chan–Evans–Lam N-Arylation of 2-Imidazolines

Dar’in, D. V., & Krasavin, M. (2016) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.6b02404 · Cited by 24

Ligandenaktivierte enantioselektive C‐H‐Aktivierung von Tetrahydrochinolinen und gesättigten Aza‐Heterocyclen durch RhI

Greßies, S., Klauck, F. J. R., Kim, J. H., Daniliuc, C. G., & Glorius, F. (2018) · Angewandte Chemie · doi:10.1002/ange.201805680 · Cited by 24

Synthesis, structure elucidation and dft study of a new thiazole–pyridine anchored nnn donor and it's cobalt(II) complex: In-vitro antitumor activity against U937 cancer cells, dna binding property and molecular docking study

Bera, P., Aher, A., Brandão, P., Manna, S. K., Bhattacharyya, I., Pramanik, C., Mandal, B., Das, S., & Bera, P. (2020) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2020.129015 · Cited by 24

Catalytic Enantioselective Construction of Chiral Benzo-Fused N -Heterocycles through Friedel–Crafts-Type Electrophilic Chlorination

Luo, J., Zhang, Y., Zhong, F., & Zhao, X. (2021) · CCS Chemistry · doi:10.31635/ccschem.021.202100777 · Cited by 24

Recent Advances in N‐Heterocyclic Carbene Catalyzed Oxidative Cyclization for the Formation of Heterocycles

Pavithra, T., Devi, E. S., & Maheswari, C. U. (2021) · Asian Journal of Organic Chemistry · doi:10.1002/ajoc.202100289 · Cited by 24

Redox-Neutral Rhodium(III)-Catalyzed Chemospecific and Regiospecific [4+1] Annulation between Indoles and Alkenes for the Synthesis of Functionalized Imidazo[1,5-a]indoles

Zhao, F., Qiao, J., Lu, Y., Zhang, X., Dai, L., Liu, S., Ni, H., Jia, X., Wu, X., & Lu, S. (2021) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.1c01256 · Cited by 24

Recent Advances in the Synthesis of 5‐Membered N ‐Heterocycles via Rhodium Catalysed Cascade Reactions

Mishra, D. R., Panda, B. S., Nayak, S., Panda, J., & Mohapatra, S. (2022) · ChemistrySelect · doi:10.1002/slct.202200531 · Cited by 24

Cyclometalated Chiral-at-Ruthenium Catalyst for Enantioselective Ring-Closing C(sp 3 )–H Carbene Insertion to Access Chiral Flavanones

Han, F., Choi, P. H., Ye, C., Grell, Y., Xie, X., Ivlev, S. I., Chen, S., & Meggers, E. (2022) · ACS Catalysis · doi:10.1021/acscatal.2c02423 · Cited by 24

Manganese-Mediated Electrochemical Dearomatization of Indoles To Access 2-Azido Spirocyclic Indolines

Mo, K., Zhou, X., Wu, J., & Zhao, Y. (2022) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.2c02017 · Cited by 24

Recent Advances in the Synthesis of Quinoxalines. A Mini Review

Balakrishna, A., Reddivari, C. K. R., Muchumarri, R. M. R., Eraganaboyina, S., Zyryanov, G. V., & Nemallapudi, B. R. (2023) · Polycyclic aromatic compounds · doi:10.1080/10406638.2023.2167215 · Cited by 24

Nickel‐Catalyzed Chemoselective Arylation of Amino Alcohols

Morrison, K. M., Yeung, C. S., & Stradiotto, M. (2023) · Angewandte Chemie International Edition · doi:10.1002/anie.202300686 · Cited by 24

Biocatalytic Access to Chiral Benzazepines Using Imine Reductases

Rajput, A., Manna, T., Mondal, A., De, A., Mondal, J., & Husain, S. M. (2023) · ACS Catalysis · doi:10.1021/acscatal.3c00146 · Cited by 24

A new quinoxaline-containing peptide induces apoptosis in cancer cells by autophagy modulation

Zamudio-Vázquez, R., Ivanova, S., Moreno, M. R., Hernández‐Álvarez, M. I., Giralt, E., Bidon‐Chanal, A., Antonio Zorzano, A., Alberício, F., & Tulla‐Puche, J. (2015) · Chemical Science · doi:10.1039/c5sc00125k · Cited by 24

Novel diversely substituted 1-heteroaryl-2-imidazolines for fragment-based drug discovery

Krasavin, M. (2012) · Tetrahedron Letters · doi:10.1016/j.tetlet.2012.03.122 · Cited by 24

Synthesis of Stereochemically and Skeletally Diverse Fused Ring Systems from Functionalized C-Glycosides

Gerard, B., Lee, M. D., Dandapani, S., Duvall, J. R., Fitzgerald, M. E., Kesavan, S., Lowe, J. T., Marié, J., Pandya, B. A., Suh, B., et al. (2013) · The Journal of Organic Chemistry · doi:10.1021/jo4000916 · Cited by 24

Three-Component Bicyclization Providing an Expedient Access to Pyrano[2′,3′:5,6]pyrano[2,3- b ]pyridines and Its Derivatives

Tu, X., Fan, W., Hao, W., Jiang, B., & Tu, S. (2014) · ACS Combinatorial Science · doi:10.1021/co500100c · Cited by 24

Synthesis, spectroscopic characterization, X-ray structure, and in vivo neurotropic activity of new 1,5-benzodiazepin-2-ones

Gaponov, A. A., Zlenko, E. T., Shishkina, S. V., Шишкин, О. В., Antypenko, O., Tretiakov, S., & Palchikov, V. A. (2016) · Medicinal Chemistry Research · doi:10.1007/s00044-016-1605-z · Cited by 24

Transition‐Metal‐Free Oxidative Cross‐Coupling of Methylhetarenes with Imidazoheterocycles towards Efficient C(sp2)−H Carbonylation

Sultana, F., Shaik, S. P., AlArifi, A. S., Srivastava, A. K., & Kamal, A. (2017) · Asian Journal of Organic Chemistry · doi:10.1002/ajoc.201700173 · Cited by 24

Rational Design of Selective Adenine-Based Scaffolds for Inactivation of Bacterial Histidine Kinases

Goswami, M., Wilke, K. E., & Carlson, E. E. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01066 · Cited by 24

Isatin Derivatives Containing Sterically Hindered Phenolic Fragment and Water-Soluble Acyl Hydrazones on Their Basis: Synthesis and Antimicrobial Activity

Bogdanov, A. V., Zaripova, I. F., Voloshina, A. D., Strobykina, A. S., Kulik, N., Бухаров, С. В., & Mironov, V. F. (2018) · Russian Journal of General Chemistry · doi:10.1134/s1070363218010097 · Cited by 24

Sequential decarboxylative [3+2] cycloaddition and Staudinger/aza-Wittig reactions for diastereoselective synthesis of tetrahydro-pyrroloquinazolines and tetrahedro-pyrrolobenzodiazepines

Ma, X., Zhang, X., Awad, J. M., Xie, G., Qiu, W., Muriph, R. E., & Zhang, W. (2019) · Tetrahedron Letters · doi:10.1016/j.tetlet.2019.151392 · Cited by 24

Psychedelic-like Properties of Quipazine and Its Structural Analogues in Mice

Revenga, M. D. L. F., Shah, U. H., Nassehi, N., Jaster, A. M., Hemanth, P., Sierra, S., Dukat, M., & González‐Maeso, J. (2021) · ACS Chemical Neuroscience · doi:10.1021/acschemneuro.0c00291 · Cited by 23

Bridging chemical space and biological efficacy: advances and challenges in applying generative models in structural modification of natural products

Liu, C.-S., Yan, B., Sun, H., Lu, J., & Puno, P. (2025) · Natural Products and Bioprospecting · doi:10.1007/s13659-025-00521-y · Cited by 24

Facile access to a heterocyclic, sp 3 -rich chemical scaffold via a tandem condensation/intramolecular nitrone–alkene [3+2] cycloaddition strategy

Rawling, M. J., Storr, T. E., Bawazir, W. A., Cully, S. J., Lewis, W., Makki, M. S. I., Strutt, I. R., Jones, G., Hamza, D., & Stockman, R. A. (2015) · Chemical Communications · doi:10.1039/c5cc05070g · Cited by 23

One‐Pot Synthesis of 2‐Arylquinazolines and Tetracyclic Isoindolo[1,2‐a]quinazolines via Cyanation Followed by Rearrangement of ortho‐Substituted 2‐Halo‐N‐arylbenzamides

Gawande, S. D., Zanwar, M. R., Kavala, V., Kuo, C., Rajawinslin, R. R., & Yao, C. (2014) · Advanced Synthesis & Catalysis · doi:10.1002/adsc.201400505 · Cited by 23

Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters

Tosh, D. K., Janowsky, A. J., Eshleman, A. J., Warnick, E., Gao, Z.-G., Chen, Z., Gizewski, E. T., Auchampach, J. A., Salvemini, D., & Jacobson, K. A. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00141 · Cited by 23

Practical Metal‐Free C(sp3)H Functionalization: Construction of Structurally Diverse α‐Substituted N‐Benzyl and N‐Allyl Carbamates

Xie, Z., Liu, L., Chen, W., Zheng, H., Xu, Q., Yuan, H., & Lou, H. (2014) · Angewandte Chemie · doi:10.1002/ange.201310193 · Cited by 23

Diastereoselective congested β-amido ketone synthesis via NHC-catalyzed radical-radical coupling

Sato, Y., Miyamoto, Y., Matsui, T., Sumida, Y., & Ohmiya, H. (2023) · Chem Catalysis · doi:10.1016/j.checat.2023.100736 · Cited by 23

Functionalised isocoumarins as antifungal compounds: Synthesis and biological studies

Simić, M. R., Paunovic, N., Borić, I., Randjelović, J., Vojnović, S., Runic, J. N., Pekmezovic, M. G., & Savić, V. (2015) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2015.08.086 · Cited by 23

A Cycloisomerization/Friedel–Crafts Alkylation Strategy for the Synthesis of Pyrano[3,4-b]indoles

Medeiros, M. R., Schaus, S. E., & Porco, J. A. J. (2011) · Organic Letters · doi:10.1021/ol201532k · Cited by 23

Novel pyrrolobenzoxaboroles: Design, synthesis, and biological evaluation against Trypanosoma brucei

Wu, P., Zhang, J., Meng, Q., Nare, B., Jacobs, R. T., & Zhou, H. (2014) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2014.04.079 · Cited by 23

Cyclopropanations of Olefin-Containing Natural Products for Simultaneous Arming and Structure Activity Studies

Robles, O., Serna-Saldivar, S. O., Gutierrez-Uribe, J. A., & Romo, D. (2012) · Organic Letters · doi:10.1021/ol300105q · Cited by 23

Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT2B/5HT2CSerotonin Receptor Antagonists

Tosh, D. K., Ciancetta, A., Warnick, E., Crane, S., Gao, Z., & Jacobson, K. A. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01183 · Cited by 23

Polypharmacology of conformationally locked methanocarba nucleosides

Jacobson, K. A., Tosh, D. K., Toti, K. S., & Ciancetta, A. (2017) · Drug Discovery Today · doi:10.1016/j.drudis.2017.07.013 · Cited by 23

An Oxyboration Route to a Single Regioisomer of Borylated Dihydrofurans and Isochromenes

Tu, K. N., Gao, C., & Blum, S. A. (2018) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.8b01790 · Cited by 23

Indium-mediated difunctionalization of iodoalkyl-tethered unactivated alkenes via an intramolecular cyclization and an ensuing palladium-catalyzed cross-coupling reaction with aryl halides

Song, X., Li, X.-R., Wang, Y., Chu, X., Rao, W., Xu, H., Han, G., & Shen, Z. (2020) · Organic Chemistry Frontiers · doi:10.1039/d0qo00632g · Cited by 23

Palladium/GF-Phos-catalyzed asymmetric carbenylative amination to access chiral pyrrolidines and piperidines

Sun, Y., Ma, C., Li, Z., & Zhang, J. (2022) · Chemical Science · doi:10.1039/d2sc03999k · Cited by 22

Ring systems in medicinal chemistry: A cheminformatics analysis of ring popularity in drug discovery over time

Ertl, P., Altmann, E., & Wilcken, R. (2025) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2025.118178 · Cited by 24

Design, synthesis, and antimicrobial activity of novel 5-substituted indole-2-carboxamide derivatives

Mane, Y. D., Sarnikar, Y. P., Surwase, S. M., Biradar, D. O., Gorepatil, P. B., Shinde, V. S., & Khade, B. C. (2016) · Research on Chemical Intermediates · doi:10.1007/s11164-016-2696-3 · Cited by 22

Vibrational, structural and electronic properties investigation by DFT calculations and molecular docking studies with DNA topoisomerase II of strychnobrasiline type alkaloids: A theoretical approach for potentially bioactive molecules

Costa, R. A., de Oliveira, K. M. T., Costa, E. V., & Pinheiro, M. L. B. (2017) · Journal of Molecular Structure · doi:10.1016/j.molstruc.2017.05.087 · Cited by 22

Copper-catalyzed oxidative cross-dehydrogenative coupling of 2 H -chromenes and terminal alkynes

Yang, F., Li, Y., Floreancig, P. E., Li, X., & Liu, L. (2018) · Organic & Biomolecular Chemistry · doi:10.1039/c8ob00949j · Cited by 22

Styrylquinoline – A Versatile Scaffold in Medicinal Chemistry

Musioł, R. (2019) · Medicinal Chemistry · doi:10.2174/1573406415666190603103012 · Cited by 22

Pd-Catalyzed Sequential Arylation of 7-Azaindoles: Aggregate-Induced Emission of Tetra-Aryl 7-Azaindoles

Cardoza, S., Das, P., & Tandon, V. (2019) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.9b02187 · Cited by 22

Xanthine Derivatives Reveal an Allosteric Binding Site in Methylenetetrahydrofolate Dehydrogenase 2 (MTHFD2)

Lee, L.-C., Peng, Y., Chang, H.-H., Hsu, T., Lu, C., Huang, C., Hsueh, C.-C., Kung, F.-C., Kuo, C., Jiaang, W., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00663 · Cited by 22

Visible-light-mediated three-component Minisci reaction for heteroarylethyl alcohols synthesis

Dong, J., Yue, F., Liu, J., Song, H., Liu, Y., & Wang, Q. (2021) · Green Chemistry · doi:10.1039/d1gc02807c · Cited by 22

Direct Photoexcitation of Borate Enabling Minisci Reaction

Kemmochi, M., Miyamoto, Y., Sumida, Y., & Ohmiya, H. (2021) · Asian Journal of Organic Chemistry · doi:10.1002/ajoc.202100640 · Cited by 22

Imidazo[4,5-b]pyridine derived tubulin polymerization inhibitors: Design, synthesis, biological activity in vitro and computational analysis

Boček, I., Hok, L., Persoons, L., Daelemans, D., Vianello, R., & Hranjec, M. (2022) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2022.106032 · Cited by 22

Visible Light Assisted Direct C3–H Arylation of Pyrido[1,2-a]pyrimidin-4-ones and Thiazolo[3,2-a]pyrimidin-5-ones

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Electrosprayed poly(butylene succinate) microspheres loaded with indole derivatives: A system with anticancer activity

Murase, S. K., Rosiñol, M. A., Tarragona, A. C., del Valle, L. J., & Puiggalı́, J. (2015) · European Polymer Journal · doi:10.1016/j.eurpolymj.2015.07.047 · Cited by 22

N-bridged 5,6-bicyclic pyridines: Recent applications in central nervous system disorders

Delgado, Ó., Delgado, F., Vega, J. A., & Trabanco, A. A. (2014) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2014.12.034 · Cited by 22

Direct access to pyrazolo(benzo)thienoquinolines. Highly effective palladium catalysts for the intramolecular C–H heteroarylation of arenes

Churruca, F., Hernández, S., Perea, M., SanMartı́n, R., & Domı́nguez, E. (2013) · Chemical Communications · doi:10.1039/c2cc37905h · Cited by 22

DARC: Mapping Surface Topography by Ray-Casting for Effective Virtual Screening at Protein Interaction Sites

Gowthaman, R., Miller, S. A., Rogers, S. A., Khowsathit, J., Lan, L., Bai, N., Johnson, D. K., Liu, C., Xu, L., Anbanandam, A., et al. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b00150 · Cited by 23

Twelve‐membered macrolactones: privileged scaffolds for the development of new therapeutics

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Anticancer Pyrroloquinazoline LBL1 Targets Nuclear Lamins

Li, B. X., Chen, J., Chao, B., David, L. L., & Xiao, X. (2018) · ACS Chemical Biology · doi:10.1021/acschembio.8b00266 · Cited by 21

Selenocystine Peptides Performance in 5‐endo‐dig Reactions

Lapcinska, S., & Arsenyan, P. (2020) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201901548 · Cited by 22

Tandem Copper-Catalyzed Regioselective N-Arylation–Aza-Michael Addition: Synthesis of Tetracyclic 5H-Benzothiazolo[3,2-a]quinazoline Derivatives

Honnanayakanavar, J. M., Harish, B., Nanubolu, J. B., & Suresh, S. (2020) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.0c00275 · Cited by 22

LBVS: an online platform for ligand-based virtual screening using publicly accessible databases

Zheng, M., Liu, Z., Yan, X., Ding, Q., Gu, Q., & Xu, J. (2014) · Molecular Diversity · doi:10.1007/s11030-014-9545-3 · Cited by 24

A Short Asymmetric Synthesis of Octahydroindole Derivatives by Application of Catalytic C(sp3)–H Amination Reaction

Mazurais, M., Lescot, C., Retailleau, P., & Dauban, P. (2013) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201301174 · Cited by 21

Rhodium(III)‐Catalyzed Synthesis of Aryl Spirocycles by Aromatic CH Activation/Intramolecular Heck‐Type Reaction

Chabaud, L., Raynal, Q., Barré, E., & Guillou, C. (2015) · Advanced Synthesis & Catalysis · doi:10.1002/adsc.201500768 · Cited by 21

3′,4′-Dihydro-2′H-spiro[indoline-3,1′-isoquinolin]-2-ones as potential anti-cancer agents: synthesis and preliminary screening

Lobe, M. M. M., & Efange, S. M. N. (2020) · Royal Society Open Science · doi:10.1098/rsos.191316 · Cited by 21

Discovery of unusual dimeric piperazyl cyclopeptides encoded by a Lentzea flaviverrucosa DSM 44664 biosynthetic supercluster

Li, C., Hu, Y., Wu, X., Stumpf, S. D., Qi, Y., D’Alessandro, J. M., Nepal, K. K., Sarotti, A. M., Cao, S., & Blodgett, J. A. V. (2022) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2117941119 · Cited by 21

Ynones in dearomative spirocyclisation processes; a review

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Diversity‐Oriented Synthesis of Polycyclic Indoles: Brønsted or Lewis Acid Catalyzed Three‐Component Reaction for the Synthesis of α‐Carbolines and Pyrimidoindoles

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Targeting Oncogenic Protein-Protein Interactions by Diversity Oriented Synthesis and Combinatorial Chemistry Approaches

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Multicomponent assembling of salicylaldehydes, malononitrile and cyanoacetamides: A simple and efficient approach to medicinally relevant 2-amino-4H-chromene scaffold

Elinson, M. N., Ryzhkov, F. V., Vereshchagin, A. N., Gorbunov, S. V., & Egorov, M. P. (2015) · Comptes Rendus Chimie · doi:10.1016/j.crci.2014.09.005 · Cited by 21

Design, synthesis and biological evaluation of C(6)-indole celastrol derivatives as potential antitumor agents

Tang, K., Huang, J., Pan, J., Zhang, X., & Lu, W. P. (2015) · RSC Advances · doi:10.1039/c4ra15414b · Cited by 21

Development of a new cascade reaction for convergent synthesis of pyrazolo[1,5-a]quinoline derivatives under transition-metal-free conditions

Kato, J., Aoyama, H., & Yokomatsu, T. (2012) · Organic & Biomolecular Chemistry · doi:10.1039/c2ob27050a · Cited by 21

Three-component domino cyclization of novel carbazole and indole fused pyrano[2,3-c]pyridine derivatives

Zhang, W., Wang, J., Mao, J., Li, H., Wu, X., & Guo, C. (2016) · Tetrahedron Letters · doi:10.1016/j.tetlet.2016.03.081 · Cited by 21

Diastereoselective Synthesis of 2-Phenyl-3-(trifluoromethyl)piperazines as Building Blocks for Drug Discovery

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Disubstituted 1-Aryl-4-Aminopiperidine Library Synthesis Using Computational Drug Design and High-Throughput Batch and Flow Technologies

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

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Privileged Structures Revisited

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Privileged Structures: Applications in Drug Discovery

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Scaffold composition and biological relevance of screening libraries

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