Privileged scaffolds for library design and drug discovery

The evolving role of natural products in drug discovery

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

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Drugs for bad bugs: confronting the challenges of antibacterial discovery

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A Planning Strategy for Diversity‐Oriented Synthesis

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

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

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

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

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Privileged Structures: Applications in Drug Discovery

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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

Efficient synthesis of conformationally constrained, amino-triazoloazepinone-containing di- and tripeptides via a one-pot Ugi–Huisgen tandem reaction

Barlow, T. M. A., Jida, M., Tourwé, D. A., & Ballet, S. (2014) · Organic & Biomolecular Chemistry · doi:10.1039/c4ob01381f · Cited by 34

Organocatalytic asymmetric decarboxylative cyanomethylation of isatins using l-proline derived bifunctional thiourea

Gajulapalli, V. P. R., Vinayagam, P., & Kesavan, V. (2014) · Organic & Biomolecular Chemistry · doi:10.1039/c4ob00271g · Cited by 34

Novel Treatment for Mantle Cell Lymphoma Including Therapy-Resistant Tumor by NF-κB and mTOR Dual-Targeting Approach

Chaturvedi, N. K., Rajule, R. N., Shukla, A., Radhakrishnan, P., Todd, G. L., Natarajan, A., Vose, J. M., & Joshi, S. S. (2013) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-13-0239 · Cited by 34

Tuning of Copper-Catalyzed Multicomponent Reactions toward 3-Functionalized Oxindoles

Cheng, D. P., Ling, F., Zheng, C., & Ma, C. (2016) · Organic Letters · doi:10.1021/acs.orglett.6b00964 · Cited by 34

n Bu 4 NPF 6 promoted regioselective cascade synthesis of functionally embellished naphthofurans under acid, metal & solvent free conditions

Pareek, A., Dada, R., Rana, M., Sharma, A. K., & Yaragorla, S. (2016) · RSC Advances · doi:10.1039/c6ra17411f · Cited by 34

Method for Accessing Nitrogen-Containing, B -Heteroaryl-Substituted 2,1-Borazaronaphthalenes

Davies, G. H. M., Zhou, Z., Jouffroy, M., & Molander, G. A. (2016) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.6b02574 · Cited by 34

Enantioselective cross dehydrogenative coupling reaction catalyzed by Rose Bengal incorporated-Cu(I)-dimeric chiral complexes

Kumar, G., Verma, S. C., Ansari, A., Khan, N. H., & Kureshy, R. I. (2017) · Catalysis Communications · doi:10.1016/j.catcom.2017.05.026 · Cited by 34

Hydrazone Derivatives Enhance Antileishmanial Activity of Thiochroman-4-ones

Vargas, E., Echeverri, F., Upegui, Y., Robledo, S. M., & Quiñones, W. (2017) · Molecules · doi:10.3390/molecules23010070 · Cited by 34

Benzoxazoles as novel herbicidal agents

Sangi, D. P., Meira, Y. G., Moreira, N. M., Lopes, T. A., Leite, M. P., Pereira-Flores, M. E., & Alvarenga, E. S. (2018) · Pest Management Science · doi:10.1002/ps.5111 · Cited by 34

Rhodium(III)-Catalyzed C–H Activation: Ligand-Controlled Regioselective Synthesis of 4-Methyl-Substituted Dihydroisoquinolones

Barber, J. S., Scales, S. A., Tran‐Dubé, M., Wang, F., Sach, N. W., Bernier, L., Collins, M. R., Zhu, J., McAlpine, I., & Patman, R. L. (2019) · Organic Letters · doi:10.1021/acs.orglett.9b02029 · Cited by 34

Development of Novel Indole-Based Bifunctional Aldose Reductase Inhibitors/Antioxidants as Promising Drugs for the Treatment of Diabetic Complications

Kováčiková, L., Prnová, M. Š., Májeková, M., Boháč, A., Karasu, Ç., & Štefek, M. (2021) · Molecules · doi:10.3390/molecules26102867 · Cited by 34

Base-Mediated Direct C–H Germylation of Heteroarenes and Arenes

Dahiya, A., & Schoenebeck, F. (2021) · Organic Letters · doi:10.1021/acs.orglett.1c02079 · Cited by 34

Catalytic Stereoselective Multicomponent Reactions for the Synthesis of Spiro Derivatives: Recent Progress

Patel, D. M., Patel, P. J., & Patel, H. M. (2022) · European Journal of Organic Chemistry · doi:10.1002/ejoc.202201119 · Cited by 34

N-Heterocyclic (4-Phenylpiperazin-1-yl)methanones Derived from Phenoxazine and Phenothiazine as Highly Potent Inhibitors of Tubulin Polymerization

Prinz, H., Ridder, A.-K., Vogel, K., Böhm, K. J., Ivanov, I., Ghasemi, J. B., Aghaee, E., & Müller, K. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01591 · Cited by 34

Cheminformatic characterization of natural products from Panama

Olmedo, D. A., González-Medina, M., Gupta, M. P., & Medina‐Franco, J. L. (2017) · Molecular Diversity · doi:10.1007/s11030-017-9781-4 · Cited by 35

Catalyst-free [3 + 2] cyclization of dihydroisoquinoline imines and isatin-derived Morita–Baylis–Hillman carbonates via 1,5-electrocyclization: synthesis of tetrahydroisoquinoline-fused spirooxindoles

Xue Ming, T. A. N. G., Gao, Y.-J., Deng, H., Lei, J.-J., Liu, S., Zhou, L. P., Shi, Y., Liang, H., Qiao, J., Guo, L., et al. (2018) · Organic & Biomolecular Chemistry · doi:10.1039/c8ob00749g · Cited by 33

Metal-Free Denitrogenative C–C Couplings of Pyridotriazoles with Boronic Acids To Afford α-Secondary and α-Tertiary Pyridines

Dong, C., Wang, X., Pei, Z., & Shen, R. (2019) · Organic Letters · doi:10.1021/acs.orglett.9b01334 · Cited by 33

One-Pot Synthesis of Unsymmetrical Bis-Heterocycles: Benzimidazole-, Benzoxazole-, and Benzothiazole-Linked Thiazolidines

Lu, H.-Y., Barve, I. J., Selvaraju, M., & Sun, C. (2019) · ACS Combinatorial Science · doi:10.1021/acscombsci.9b00161 · Cited by 33

Promising 2,6,9-Trisubstituted Purine Derivatives for Anticancer Compounds: Synthesis, 3D-QSAR, and Preliminary Biological Assays

Salas, C. O., Zárate, A. M., Kryštof, V., Mella, J., Faúndez, M., Brea, J. M., Loza, M. I., Brito, I., Hendrychová, D., Jorda, R., et al. (2019) · International Journal of Molecular Sciences · doi:10.3390/ijms21010161 · Cited by 33

Direct Alkylation of Amines with Primary and Secondary Alcohols through Biocatalytic Hydrogen Borrowing

Montgomery, S. L., Mangas‐Sánchez, J., Thompson, M. P., Aleku, G. A., Domínguez, B., & Turner, N. J. (2017) · Angewandte Chemie · doi:10.1002/ange.201705848 · Cited by 33

Shape‐based virtual screening with volumetric aligned molecular shapes

Koes, D. R., & Camacho, C. J. (2014) · Journal of Computational Chemistry · doi:10.1002/jcc.23690 · Cited by 33

Direct N 9 -arylation of purines with aryl halides

Larsen, A. F., & Ulven, T. (2014) · Chemical Communications · doi:10.1039/c3cc48642g · Cited by 33

Identification, expression and characterization of an R-ω-transaminase from Capronia semiimmersa

Iglesias, C., Panizza, P., & Giordano, S. R. (2017) · Applied Microbiology and Biotechnology · doi:10.1007/s00253-017-8309-2 · Cited by 33

A Photo-Enzymatic Cascade to Transform Racemic Alcohols into Enantiomerically Pure Amines

Gacs, J., Zhang, W., Knaus, T., Mutti, F. G., Arends, I. W. C. E., & Hollmann, F. (2019) · Catalysts · doi:10.3390/catal9040305 · Cited by 33

Solid-Phase Library Synthesis of Bi-Functional Derivatives of Oleanolic and Maslinic Acids and Their Cytotoxicity on Three Cancer Cell Lines

Parra, A., Martin-Fonseca, S., Rivas, F., Reyes‐Zurita, F. J., Medina‐O’Donnell, M., Rufino‐Palomares, E. E., Martı́nez, A., García‐Granados, A., Lupiáñez, J. A., & Alberício, F. (2014) · ACS Combinatorial Science · doi:10.1021/co500051z · Cited by 31

Ir( iii )-catalyzed synthesis of isoquinolines from benzimidates and α-diazocarbonyl compounds

Yang, X., Jie, J., Li, H., & Piao, M. (2016) · RSC Advances · doi:10.1039/c6ra10045g · Cited by 32

Multiheterocyclic Motifs via Three-Component Reactions of Benzynes, Cyclic Amines, and Protic Nucleophiles

Ross, S. P., & Hoye, T. R. (2017) · Organic Letters · doi:10.1021/acs.orglett.7b03458 · Cited by 32

Diastereoselectivity in Passerini Reactions of Chiral Aldehydes and in Ugi Reactions of Chiral Cyclic Imines

Lambruschini, C., Moni, L., & Banfi, L. (2020) · European Journal of Organic Chemistry · doi:10.1002/ejoc.202000016 · Cited by 32

Access to Indole‐Fused Benzannulated Medium‐Sized Rings through a Gold(I)‐Catalyzed Cascade Cyclization of Azido‐Alkynes

Greiner, L. C., Inuki, S., Arichi, N., Oishi, S., Suzuki, R., Iwai, T., Sawamura, M., Hashmi, A. S. K., & Ohno, H. (2021) · Chemistry - A European Journal · doi:10.1002/chem.202101824 · Cited by 32

Synthesis and Pharmacophore Modelling of 2,6,9-Trisubstituted Purine Derivatives and Their Potential Role as Apoptosis-Inducing Agents in Cancer Cell Lines

Calderón-Arancibia, J., Espinosa‐Bustos, C., Cañete, Á., Tapia, R. A., Faúndez, M., Torres, M., Aguirre, A., Paulino, M., & Salas, C. O. (2015) · Molecules · doi:10.3390/molecules20046808 · Cited by 32

Cryptic indole hydroxylation by a non-canonical terpenoid cyclase parallels bacterial xenobiotic detoxification

Kugel, S., Baunach, M., Baer, P., Ishida‐Ito, M., Sundaram, S., Xu, Z., Groll, M., & Hertweck, C. (2017) · Nature Communications · doi:10.1038/ncomms15804 · Cited by 32

Expedient Synthesis of Norbenzomorphan Library via Multicomponent Assembly Process Coupled with Ring-Closing Reactions

Sahn, J. J., & Martin, S. F. (2012) · ACS Combinatorial Science · doi:10.1021/co300068a · Cited by 31

2P2Ichem: focused chemical libraries dedicated to orthosteric modulation of protein–protein interactions

Hamon, V., Brunel, J. M., Combes, S., Basse, M. J., Roche, P., & Morelli, X. (2013) · MedChemComm · doi:10.1039/c3md00018d · Cited by 31

A heavy metal- and oxidant-free, one-pot synthesis of pyridines and fused pyridines based on a Lewis acid-catalyzed multicomponent reaction

Raja, V. P. A., Tenti, G., Perumal, S., & Menéndez, J. C. (2014) · Chemical Communications · doi:10.1039/c4cc01791a · Cited by 31

The transition-metal-catalyzed stereoselective ring-expansion of vinylaziridines and vinyloxiranes

Sarkar, T., Talukdar, K., Das, B. K., Shah, T. A., Debnath, B., & Punniyamurthy, T. (2021) · Organic & Biomolecular Chemistry · doi:10.1039/d1ob00259g · Cited by 31

Artificial Intelligent Deep Learning Molecular Generative Modeling of Scaffold-Focused and Cannabinoid CB2 Target-Specific Small-Molecule Sublibraries

Bian, Y., & Xie, X. (2022) · Cells · doi:10.3390/cells11050915 · Cited by 32

Total Syntheses of Dalesconol A and B

Snyder, S. A., Sherwood, T. C., & Ross, A. G. (2010) · Angewandte Chemie · doi:10.1002/ange.201002264 · Cited by 31

Asymmetric Construction of α,α‐Disubstituted Piperazinones Enabled by Benzilic Amide Rearrangement

He, Y., Quan, R., Li, X., Zhu, J., & Wu, H. Y. (2023) · Angewandte Chemie International Edition · doi:10.1002/anie.202217954 · Cited by 31

Cyclosulfamide-based derivatives as inhibitors of noroviruses

Dou, D., Mandadapu, S. R., Alliston, K. R., Kim, Y., Chang, K., & Groutas, W. C. (2011) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2011.10.019 · Cited by 31

Friedländer synthesis of polysubstituted quinolines and naphthyridines promoted by propylphosphonic anhydride (T3P®) under mild conditions

Jida, M., & Deprez, B. P. (2012) · New Journal of Chemistry · doi:10.1039/c2nj21043f · Cited by 31

Solid-Phase Parallel Synthesis of Drug-Like Artificial 2H-Benzopyran Libraries

Lee, T., & Gong, Y. (2012) · Molecules · doi:10.3390/molecules17055467 · Cited by 31

Heterocycles fused on a 6,7-coumarin framework: an in-depth review of their structural and pharmacological diversity

Jibroo, R. N., Mustafa, Y. F., & Al-Shakarchi, W. (2024) · Chemical Papers · doi:10.1007/s11696-024-03613-0 · Cited by 30

Scalable Synthesis of Piperazines Enabled by Visible‐Light Irradiation and Aluminum Organometallics

Suárez‐Pantiga, S., Colas, K., Johansson, M. J., & Mendoza, A. (2015) · Angewandte Chemie International Edition · doi:10.1002/anie.201505608 · Cited by 30

Skeletal Fusion of Small Heterocycles with Amphoteric Molecules

Cheung, L. L. W., He, Z., Decker, S., & Yudin, A. K. (2011) · Angewandte Chemie International Edition · doi:10.1002/anie.201106024 · Cited by 30

A chemical family-based strategy for uncovering hidden bioactive molecules and multicomponent interactions in herbal medicines

Song, H., Wu, S., Hao, H., Chen, J., Lu, J., Xu, X., Li, P., & Yang, H. Q. (2016) · Scientific Reports · doi:10.1038/srep23840 · Cited by 30

Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer

Zhu, W., Chen, H., Wang, Y., Wang, J., Xia, P., Chen, X., Gao, Y., Li, C., He, Y., Ai, J., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00076 · Cited by 30

Structure activity relationship studies on rhodanines and derived enethiol inhibitors of metallo-β-lactamases

Zhang, D., Markoulides, M. S., Stepanovs, D., Rydzik, A. M., El‐Hussein, A., Bon, C., Kamps, J. J. A. G., Umland, K., Collins, P. M., Cahill, S. T., et al. (2018) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2018.02.043 · Cited by 30

Multi-component synthesis of 3-substituted indoles and their cyclisation to α-carbolines via I 2 -promoted intramolecular C2 oxidative amination/aromatisation at room temperature

Deka, B., Baruah, P. K., & Deb, M. L. (2018) · Organic & Biomolecular Chemistry · doi:10.1039/c8ob02362j · Cited by 30

Multicomponent Assembly Processes for the Synthesis of Diverse Yohimbine and Corynanthe Alkaloid Analogues

Granger, B. A., Wang, Z., Kaneda, K., Fang, Z., & Martin, S. F. (2013) · ACS Combinatorial Science · doi:10.1021/co400055b · Cited by 30

Organocatalytic cascade reactions: diversity-oriented synthesis for the construction of hydroisoquinoline scaffolds

Gómez, C. V., Cruz, D. C., Mose, R., & Jørgensen, K. A. (2014) · Chemical Communications · doi:10.1039/c4cc01231c · Cited by 30

From Natural Product‐Inspired Pyrrolidine Scaffolds to the Development of New Human Golgi α‐Mannosidase II Inhibitors

Cheng, T.-J. R., Chan, T., Tsou, E., Chang, S.-Y., Yun, W., Yang, P., Wu, Y., & Cheng, W. (2013) · Chemistry - An Asian Journal · doi:10.1002/asia.201300680 · Cited by 30

Identification of 4,6-diaryl-1,4-dihydropyridines as a new class of neuroprotective agents

Tenti, G., Egea, J., Villarroya, M., Leon, R. M., Fernández, J. C., Padín, J. F., Sridharan, V., Ramos, M. T., & Menéndez, J. C. (2013) · MedChemComm · doi:10.1039/c3md20345j · Cited by 30

Lead Optimization of 2-Phenylindolylglyoxylyldipeptide Murine Double Minute (MDM)2/Translocator Protein (TSPO) Dual Inhibitors for the Treatment of Gliomas

Daniele, S., Pietra, V. L., Barresi, E., Maro, S. D., Pozzo, E. D., Robello, M., Motta, C. L., Cosconati, S., Taliani, S., Marinelli, L., et al. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01767 · Cited by 32

Preparation of Substituted Tetrahydroisoquinolines by Pd(II)-Catalyzed NH2-Directed Insertion of Michael Acceptors into C–H Bonds Followed by NH2-Conjugated Addition

Mancinelli, A., Alamillo‐Ferrer, C., Albert, J., Ariza, X., Etxabe, H., Farràs, J., García, J., Granell, J., & Quijada, F. J. (2017) · Organometallics · doi:10.1021/acs.organomet.6b00944 · Cited by 30

Rapid identification of urokinase plasminogen activator inhibitors from Traditional Chinese Medicines based on ultrafiltration, LC–MS and in silico docking

Li, L., Kong, J., Yao, C.-H., Liu, X., & Liu, J.-H. (2018) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/j.jpba.2018.10.036 · Cited by 32

Copper-Catalyzed Multicomponent Domino Reaction of 2-Bromobenzaldehydes, Aryl Methyl Ketones, and Sodium Azide: Access to 1H-[1,2,3]Triazolo[4,5-c]quinoline Derivatives

Cheng, X., Jiang, S., Wu, Y., Jia, F., & Wu, A. (2018) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.8b02476 · Cited by 30

Catalytic S N Ar Hexafluoroisopropoxylation of Aryl Chlorides and Bromides

Su, J., Chen, K., Kang, Q., & Shi, H. (2023) · Angewandte Chemie International Edition · doi:10.1002/anie.202302908 · Cited by 29

N‐Heterocycle‐Editing to Access Fused‐BN‐Heterocycles via Ring‐Opening/C−H Borylation/Reductive C−B Bond Formation

Zhang, X., Su, W., Guo, H., Fang, P., Yang, K. H., & Song, Q. (2024) · Angewandte Chemie International Edition · doi:10.1002/anie.202318613 · Cited by 29

anti-Selective aminofluorination of alkenes with amidines mediated by hypervalent iodine( iii ) reagents

Chen, H., Kaga, A., & Chiba, S. (2015) · Organic & Biomolecular Chemistry · doi:10.1039/c5ob01854d · Cited by 29

Expanding the Scope of Human DNA Polymerase λ and β Inhibitors

Strittmatter, T., Brockmann, A., Pott, M., Hantusch, A., Brunner, T., & Marx, A. (2013) · ACS Chemical Biology · doi:10.1021/cb4007562 · Cited by 28

Enantioselective Synthesis of 1‐Aryl‐Substituted Tetrahydroisoquinolines Through Ru‐Catalyzed Asymmetric Transfer Hydrogenation

Perez, M., Wu, Z. P., Scalone, M., Ayad, T., & Ratovelomanana‐Vidal, V. (2015) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201500951 · Cited by 29

Structure-Based Screening of Uncharted Chemical Space for Atypical Adenosine Receptor Agonists

Rodriguez, D. J., Chakraborty, S., Warnick, E., Crane, S., Gao, Z., O'Connor, R. A., Jacobson, K. A., & Carlsson, J. (2016) · ACS Chemical Biology · doi:10.1021/acschembio.6b00357 · Cited by 29

Reductive amination of ketones catalyzed by whole cell biocatalysts containing imine reductases (IREDs)

Maugeri, Z., & Rother, D. (2017) · Journal of Biotechnology · doi:10.1016/j.jbiotec.2017.05.015 · Cited by 29

Palladium oxide nanoparticles intercalated mesoporous silica for solvent free acceptorless dehydrogenation reactions of alcohols

Samanta, P. K., Ray, S., Das, T., Gage, S. H., Nandi, M., Richards, R. M., & Biswas, P. (2019) · Microporous and Mesoporous Materials · doi:10.1016/j.micromeso.2019.04.034 · Cited by 29

Approaches for the isolation and identification of hydrophilic, light-sensitive, volatile and minor natural products

Berlinck, R. G. S., Monteiro, A. F. M., Bertonha, A. F., Bernardi, D. I., Gubiani, J. R., Slivinski, J., Michaliski, L. F., Tonon, L. A. C., Venancio, V. A., & Freire, V. F. (2019) · Natural Product Reports · doi:10.1039/c9np00009g · Cited by 30

N,N,N’,N’-Tetramethylethylenediamine-Enabled Photoredox-Catalyzed C–H Methylation of N-Heteroarenes

Liu, F., Ye, Z., Hu, Y., Gao, J., Zheng, L., Chen, K., Xiang, H., Chen, X., & Yang, H. (2021) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.1c01325 · Cited by 29

Stereoselective hydrogen atom transfer to acyclic radicals: a switch enabling diastereodivergent borylative radical cascades

Tian, Y., Zhang, F., Xia, H.-M., Zhou, X., Yu, Z., & Wang, Y. (2022) · Nature Communications · doi:10.1038/s41467-022-28071-8 · Cited by 29

trans‐Selective Aryldifluoroalkylation of Endocyclic Enecarbamates and Enamides by Nickel Catalysis

Xu, C., Cheng, R., Luo, Y., Wang, M., & Zhang, X. (2020) · Angewandte Chemie · doi:10.1002/ange.202008498 · Cited by 29

New molecular hybrids containing benzimidazole, thiazolidine-2,4-dione and 1,2,4-oxadiazole as EGFR directing cytotoxic agents

Kudapa, V., Saritha, B., & Sailaja, B. B. V. (2022) · Tetrahedron · doi:10.1016/j.tet.2022.132991 · Cited by 29

meta-Selective O-Arylation of Cyclic Diaryliodonium Salts with Phenols via Aryne Intermediates

Liu, M., Jiang, H., Tang, J., Ye, Z., Zhang, F., & Wu, Y. (2023) · Organic Letters · doi:10.1021/acs.orglett.3c00600 · Cited by 30

Rational drug design based synthesis of novel arylquinolines as anti-tuberculosis agents

Jain, P. P., Degani, M. S., Raju, A., Ray, M., & Rajan, M. G. R. (2013) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2013.09.027 · Cited by 29

The first solvent-free synthesis of privileged γ- and δ-lactams via the Castagnoli–Cushman reaction

Lepikhina, A., Bakulina, O., Dar’in, D. V., & Krasavin, M. (2016) · RSC Advances · doi:10.1039/c6ra19196g · Cited by 29

PtCl4-catalyzed cyclization of N-acetyl-2-alkynylanilines: A mild and efficient synthesis of N-acetyl-2-substituted indoles

Chaisan, N., Kaewsri, W., Thongsornkleeb, C., Tummatorn, J., & Ruchirawat, S. (2018) · Tetrahedron Letters · doi:10.1016/j.tetlet.2018.01.014 · Cited by 29

Copper-catalyzed regioselective alkylation of heteroarenes with functionalized alkyl halides

Li, D., & Yang, W. (2019) · Tetrahedron Letters · doi:10.1016/j.tetlet.2019.06.005 · Cited by 29

A new method for the preparation of 5-acylidene and 5-imino substituted rhodanine derivatives and their antioxidant and antimicrobial activities

Üngören, Ş. H., Albayrak, S., Günay, A., Yurtseven, L., & Yurttaş, N. (2015) · Tetrahedron · doi:10.1016/j.tet.2015.04.069 · Cited by 29

Pd-Catalyzed Ag(I)-Promoted C3-Arylation of Pyrido[1,2-a]pyrimidin-4-ones with Bromo/Iodo-Arenes

Guchhait, S. K., & Priyadarshani, G. (2015) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.5b01573 · Cited by 28

Pd-Catalyzed Regioselective 1,2-Dicarbofunctionalization of Unactivated Olefins by a Heck Reaction/Enolate Cyclization Cascade

Dhungana, R. K., Shrestha, B. L., Magar, R. T., Basnet, P., & Giri, R. (2017) · Organic Letters · doi:10.1021/acs.orglett.7b00794 · Cited by 28

Synthesis of Highly Substituted 2-Arylindoles via Copper-Catalyzed Coupling of Isocyanides and Arylboronic Acids

Heckman, L. M., He, Z., & Jamison, T. F. (2018) · Organic Letters · doi:10.1021/acs.orglett.8b01132 · Cited by 28

Diversity of small molecule HIV‐1 latency reversing agents identified in low‐ and high‐throughput small molecule screens

Hashemi, P., & Sadowski, I. (2019) · Medicinal Research Reviews · doi:10.1002/med.21638 · Cited by 30

Developing Metal-Binding Isosteres of 8-Hydroxyquinoline as Metalloenzyme Inhibitor Scaffolds

Seo, H., Jackl, M. K., Kalaj, M., & Cohen, S. M. (2022) · Inorganic Chemistry · doi:10.1021/acs.inorgchem.2c00891 · Cited by 28

Combinatorial Aid for Underprivileged Scaffolds: Solution and Solid-phase Strategies for a Rapid and Efficient Access To Novel Aza-diketopiperazines (Aza-DKP)

Bonnet, D., Margathe, J., Radford, S. K., Pflimlin, E., Riché, S., Doman, P., Hibert, M., & Ganesan, A. (2012) · ACS Combinatorial Science · doi:10.1021/co300015k · Cited by 28

Lewis Acid‐Catalyzed Generation of CC and CN Bonds on π‐Deficient Heterocyclic Substrates

Staderini, M., Bolognesi, M. L., & Menéndez, J. C. (2014) · Advanced Synthesis & Catalysis · doi:10.1002/adsc.201400674 · Cited by 28

Synthesis of functionalized 2-salicyloylfurans, furo[3,2-b]chromen-9-ones and 2-benzoyl-8H-thieno[2,3-b]indoles by one-pot cyclizations of 3-halochromones with β-ketoamides and 1,3-dihydroindole-2-thiones

Savych, I., Gläsel, T., Villinger, A., Sosnovskikh, V. Y., Iaroshenko, V. O., & Langer, P. (2014) · Organic & Biomolecular Chemistry · doi:10.1039/c4ob01730g · Cited by 28

Diversity-oriented synthesis of 1,3-benzodiazepines

Wang, G., Liu, C., Li, B., Wang, Y., Hecke, K. V., der Eycken, E. V. V., Pereshivko, O. P., & Peshkov, V. A. (2017) · Tetrahedron · doi:10.1016/j.tet.2017.09.034 · Cited by 28

Synthesis and evaluation of 1-(1H-indol-3-yl)ethanamine derivatives as new antibacterial agents

Burchak, O. Ν., Pihive, E. L., Maigre, L., Guinchard, X., Bouhours, P., Jolivalt, C., Schneider, D., Maurin, M., Giglione, C., Meinnel, T., et al. (2011) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2011.03.060 · Cited by 28

Recent Advances in the Multifunctionalization Reactions of Indoles

Zhang, X., Dai, M., Zhang, P., Lu, X., & Liang, T. (2025) · Chinese Journal of Chemistry · doi:10.1002/cjoc.70176 · Cited by 27

Antiparasitic Lead Discovery: Toward Optimization of a Chemotype with Activity Against Multiple Protozoan Parasites

Devine, W. G., Thomas, S. M., Erath, J., Bachovchin, K. A., Lee, P. J., Leed, S. E., Rodrı́guez, A., Sciotti, R. J., Mensa‐Wilmot, K., & Pollastri, M. P. (2017) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.7b00011 · Cited by 27

Chemoproteomics of an Indole-Based Quinone Epoxide Identifies Druggable Vulnerabilities in Vancomycin-Resistant Staphylococcus aureus

Kulkarni, A., Soni, I., Kelkar, D. S., Allimuthu, D., Rathinam, S., Beniwal, G., Rajendran, A., Tamhankar, S., Chopra, S., Kamat, S. S., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00774 · Cited by 27

Ag-Catalyzed minisci C–H difluoromethylarylation of N-heteroarenes

Xie, X., Zhang, Y., Hao, J., & Wan, W. (2019) · Organic & Biomolecular Chemistry · doi:10.1039/c9ob02586c · Cited by 27

Intermediates, Isolation and Mechanistic Insights into Zinc Hydride-Catalyzed 1,2-Regioselective Hydrofunctionalization of N-Heteroarenes

Sahoo, R. K., Sarkar, N., & Nembenna, S. (2022) · Inorganic Chemistry · doi:10.1021/acs.inorgchem.2c03389 · Cited by 27

Rare‐Earth Metal Chlorides Catalyzed One‐pot Syntheses of Quinolines under Solvent‐free Microwave Irradiation Conditions

Zhang, L., Wu, B., Zhou, Y., Xia, J., Zhou, S., & Wang, S. (2013) · Chinese Journal of Chemistry · doi:10.1002/cjoc.201300047 · Cited by 27

Novel fluorinated benzimidazole-based scaffolds and their anticancer activity in vitro

Bhambra, A. S., Edgar, M. A., Elsegood, M. R. J., Horsburgh, L., Kryštof, V., Lucas, P. D., Mojally, M., Teat, S. J., Warwick, T. G., Weaver, G. W., et al. (2016) · Journal of Fluorine Chemistry · doi:10.1016/j.jfluchem.2016.06.009 · Cited by 27

Stereoselective, solvent free, highly efficient synthesis of aldo- and keto-N-acylhydrazones applying grindstone chemistry

Filho, J. M. D. S., & Pinheiro, S. M. (2017) · Green Chemistry · doi:10.1039/c7gc00730b · Cited by 27

One-Pot Synthesis of spiro(indoline-3,4′-pyrazolo[3,4-b]pyridine)-5′-carbonitriles As p53-MDM2 Interaction Inhibitors

Ibrahim, H. S., Eldehna, W. M., Fallacara, A. L., Ahmed, E. R., Ghabbour, H. A., Elaasser, M. M., Botta, M., Abou‐Seri, S. M., & Abdel‐Aziz, H. A. (2018) · Future Medicinal Chemistry · doi:10.4155/fmc-2018-0288 · Cited by 27

Synthesis of Chiral γ-Lactones by One-Pot Sequential Enantioselective Organocatalytic Michael Addition of Boronic Acids and Diastereoselective Intramolecular Passerini Reaction

Bos, M., & Riguet, E. (2014) · The Journal of Organic Chemistry · doi:10.1021/jo501908z · Cited by 27

A facile, one pot method for the synthesis of 4-acyl-1,2-dihydro-3-benzazepines, based on the ring expansion of natural and synthetic 3,4-dihydroisoquinoline pseudo bases

Карцев, В. Г., Zubenko, A. A., Морковник, А. С., & Диваева, Л. Н. (2015) · Tetrahedron Letters · doi:10.1016/j.tetlet.2015.10.103 · Cited by 27

Metal-free sequential reaction via a propargylation, annulation and isomerization sequence for the one-pot synthesis of 2,3-disubstituted benzofurans

Li, W.-T., Nan, W., & Luo, Q. (2014) · RSC Advances · doi:10.1039/c4ra05503a · Cited by 26

Design and Enantioselective Synthesis of β-Vinyl Tryptamine Building Blocks for Construction of Privileged Chiral Indole Scaffolds

Lin, T., Wu, H., Feng, J., & Zhang, J. (2017) · ACS Catalysis · doi:10.1021/acscatal.7b00870 · Cited by 26

Bicyclic Heterocycles from Levulinic Acid through a Fast and Operationally Simple Diversity‐Oriented Multicomponent Approach

Lambruschini, C., Basso, A., Moni, L., Pinna, A., Riva, R., & Banfi, L. (2018) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201801129 · Cited by 26

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 · doi:10.1002/ange.201916015 · Cited by 26

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