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

A novel, flexible strategy to construct privileged dibenzo[ b,f ][1,4,5]oxathiazepine 5,5-dioxides and their heterocyclic isosteres

Sapegin, A., Panova, V. A., Reutskaya, E., Смирнов, А. В., & Krasavin, M. (2016) · Tetrahedron · doi:10.1016/j.tet.2016.10.008 · Cited by 10

Synthesis of a novel fused pyrrolodiazepine-based library with anti-cancer activity

Malik, N., Iyamu, I. D., Scheidt, K. A., & Schiltz, G. E. (2018) · Tetrahedron Letters · doi:10.1016/j.tetlet.2018.03.021 · Cited by 10

Acetic anhydride to the rescue: Facile access to privileged 1,2,3,4-tetrahydropyrazino[1,2-a]indole core via the Castagnoli-Cushman reaction

Chizhova, M., Khoroshilova, O. V., Dar’in, D. V., & Krasavin, M. (2018) · Tetrahedron Letters · doi:10.1016/j.tetlet.2018.08.049 · Cited by 10

Stereoselective synthesis of 1,3-disubstituted dihydroisoquinolines via l -phenylalanine-derived dihydroisoquinoline N -oxides

Flores‐Ferrándiz, J., Carter, N., González‐Soria, M. J., Wąsińska-Kałwa, M., Gill, D. M., Maciá, B., & Caprio, V. E. (2018) · Organic & Biomolecular Chemistry · doi:10.1039/c8ob02007h · Cited by 10

In vitro Antifungal Activity of Dihydropyrimidinones/Thiones Against Candida albicans and Cryptococcus neoformans

de Azambuja, G. O., Svetaz, L. A., Gonçalves, I. L., Corbelini, P. F., von Poser, G. L., Kawano, D. F., Zacchino, S. A., & Eifler-Lima, V. L. (2018) · Current Bioactive Compounds · doi:10.2174/1573407214666180926115745 · Cited by 10

Probing 2H‐Indazoles as Templates for SGK1, Tie2, and SRC Kinase Inhibitors

Schoene, J., Gazzi, T., Lindemann, P., Christmann, M., Volkamer, A., & Nazaré, M. (2019) · ChemMedChem · doi:10.1002/cmdc.201900328 · Cited by 10

Regioselective Reversal Cyclization To Access either Eight-Membered Sulfur-Containing Heterocycle-Fused γ-Pyrones or 2-(1,4-Dithianyl)-4-pyrones from the Same Precursors

Tang, L., Yang, Q., Zhang, J., & Deng, G. (2020) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.9b03303 · Cited by 10

Synthesis of Chiral Propargylamines, Chiral 1,2‐Dihydronaphtho[2,1‐b]furans and Naphtho[2,1‐b]furans with C‐Alkynyl N,N′‐di‐(tert‐butoxycarbonyl)‐aminals and β‐Naphthols

Man, N., Li, Y., Jie, J., Li, H., Yang, H., Zhao, Y., & Fu, H. (2021) · Chemistry - A European Journal · doi:10.1002/chem.202102040 · Cited by 10

Synthesis of Coumarin‐Thiazolidine‐2,4‐dione‐Pyrazole Hybrids as Epidermal Growth Factor Receptor (EGFR)‐Targeted Agents

Gangadhar, K. H., Benarjee, V., & Ratnamala, A. (2022) · ChemistrySelect · doi:10.1002/slct.202200270 · Cited by 10

Information-Rich, Dual-Function 13C/2H-Isotopic Crosstalk NMR Assay for Human Serine Racemase (hSR) Provides a PLP-Enzyme “Partitioning Fingerprint” and Reveals Disparate Chemotypes for hSR Inhibition

de Dios, S. M. R., Hass, J. L., Graham, D. L., Kumar, N., Antony, A. E., Morton, M., & Berkowitz, D. B. (2023) · Journal of the American Chemical Society · doi:10.1021/jacs.2c12774 · Cited by 10

Manufacturing synthesis of 5-hydroxy-2-methyl-1H-indole

Huang, Y., Zhang, W., Zhang, X., & Wang, J. (2010) · Research on Chemical Intermediates · doi:10.1007/s11164-010-0210-x · Cited by 10

Chemoenzymatic Approach to (S)‐1,2,3,4‐Tetrahydroisoquinoline Carboxylic Acids Employing D‐Amino Acid Oxidase

Ju, S., Qian, M., Xu, G., Yang, L., & Wu, J. (2019) · Advanced Synthesis & Catalysis · doi:10.1002/adsc.201900178 · Cited by 10

Natural Products as Enzyme Inhibitors

Pereira, D. M., Andrade, C., Valentão, P., & Andrade, P. B. (2017) · Wiley eBooks · doi:10.1002/9783527805921.ch1 · Cited by 10

Recent trends for chemoselectivity modulation in one-pot organic transformations

Chaudhary, H. R., & Patel, D. M. (2024) · RSC Advances · doi:10.1039/d4ra05495d · Cited by 9

Single-Site Palladium “Microreactor” for Carbon Dioxide Coupling/Cyclization Reactions

Ren, S., Lin, S., Ren, Z., Wang, M., Yang, Y., Tang, H., Chen, P., Zhou, L., & Pan, Y. (2025) · ACS Sustainable Chemistry & Engineering · doi:10.1021/acssuschemeng.4c07745 · Cited by 9

Microwave‐Assisted Synthesis of New Molecular Hybrids of Benzoimidazole Containing Thiazolidine‐2,4‐diones: Design, Theoretical, In Silico, and In Vitro Antimicrobial Studies

Khiratkar, N. M., Patil, R. C., Alotaibi, B. S., Bhat, A. R., Fahelelbom, K. M., Hadda, T. B., Ahmed, S., & Tătărîngă, G. (2025) · ChemistrySelect · doi:10.1002/slct.202502553 · Cited by 9

Unravelling the Functional Diversity of Type III Polyketide Synthases in Fungi

Sokolova, N., Denisov, S. S., Hackl, T., & Haslinger, K. (2025) · Angewandte Chemie International Edition · doi:10.1002/anie.202514786 · Cited by 9

Doebner-type pyrazolopyridine carboxylic acids in an Ugi four-component reaction

Murlykina, M. V., Kolomiiets, O., Kornet, M. N., Sakhno, Y. I., Desenko, S. M., Dyakonenko, V. V., Shishkina, S. V., Brazhko, O. A., Мусатов, В. И., Tsygankov, A. V., et al. (2019) · Beilstein Journal of Organic Chemistry · doi:10.3762/bjoc.15.126 · Cited by 9

On the Effect of the Nature of Substituents on the Antimicrobial Activity of Water-Soluble Acylhydrazones on the Isatin Scaffold

Av, B., Voloshina, A. D., Khamatgalimov, A. R., Terekhova, N. V., & Mironov, V. F. (2020) · Doklady Chemistry · doi:10.1134/s0012500820090013 · Cited by 9

Design and Synthesis of Tetrahydroisoquinoline Derivatives as Anti-Angiogenesis and Anti-Cancer Agents

Gangapuram, M., Eyunni, S., Zhang, W., & Redda, K. K. (2021) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/1871520621666210112122913 · Cited by 9

Tandem copper catalyzed regioselective N -arylation–amidation: synthesis of angularly fused dihydroimidazoquinazolinones and the anticancer agent TIC10/ONC201

Honnanayakanavar, J. M., Nanubolu, J. B., & Suresh, S. (2021) · Organic & Biomolecular Chemistry · doi:10.1039/d1ob01561c · Cited by 9

Contrasteric coupling of allenes and tetrahydroisoquinolines by iron-catalysed allenic C(sp 2 )–H functionalisation

Xia, Y. Y., Wade, N. W., Palermo, P. N., Wang, Y., & Wang, Y. (2021) · Chemical Communications · doi:10.1039/d1cc05949a · Cited by 9

Antibacterial and antibiofilm activities of thiazolidine-2,4-dione and 4-thioxo-thiazolidin-2-one derivatives against multidrug-resistant Staphylococcus aureus clinical isolates

Sena, K. X. F. R., Mendes, R. F. V., Bôtelho, E. X., Melo, R. D. O. A., Silva, C. J. A., Júnior, H. N. P. C., Amorim-Carmo, B., Damasceno, I. Z., Fernandes‐Pedrosa, M. D. F., Aguiar, J. D. S., et al. (2022) · Journal of Applied Microbiology · doi:10.1111/jam.15790 · Cited by 9

Rhodium( iii )-catalyzed mild and regioselective dearomative spirocyclization of 2-aryl-3-nitrosoindoles with alkynes

Li, C., Zhao, B., Mao, G., & Deng, G. (2023) · Chemical Communications · doi:10.1039/d3cc01940c · Cited by 9

Design, Synthesis, and Insecticidal Evaluation of N-Pyridylpyrazole Amide Derivatives Containing 4,5-Dihydroisoxazole Amide as Potential Ryanodine Receptor Activators

Pang, X., Li, H., Zhou, C., Li, Y., Xu, X., Shao, X., & Li, Z. (2023) · Journal of Agricultural and Food Chemistry · doi:10.1021/acs.jafc.3c03199 · Cited by 9

Ionic liquid-catalysed regioselective oxygenation of quinoxalin-2(1 H )-ones under visible-light conditions

Badhani, G., Biramya, V. M., & Adimurthy, S. (2023) · New Journal of Chemistry · doi:10.1039/d3nj04496c · Cited by 9

Nickel-Based Catalysts for the Selective Monoarylation of Dichloropyridines: Ligand Effects and Mechanistic Insights

Duran-Camacho, G., Bland, D. C., Li, F., Neufeldt, S. R., & Sanford, M. S. (2024) · ACS Catalysis · doi:10.1021/acscatal.4c00648 · Cited by 9

Design and synthesis of novel indole-quinoxaline hybrids to target phosphodiesterase 4 (PDE4)

Luther, B. J., Rani, C. S., Suresh, N., Rao, M. V. B., Kapavarapu, R., Suresh, C., Babu, P. V., & Pal, M. (2015) · Arabian Journal of Chemistry · doi:10.1016/j.arabjc.2015.08.009 · Cited by 9

Synthesis of a hexahydropyrrolo indole (HPI) compound library

Nickel, S., Nickel, P., Hellmert, M., Ernst, S., Jewell, R., Pearce, C. A., Jones, G., Hamza, D., & Kaiser, M. (2015) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2015.04.003 · Cited by 9

Data-mining patent literature for novel chemical reagents for use in medicinal chemistry design

Kettle, J. G., Ward, R. A., & Griffen, E. (2010) · MedChemComm · doi:10.1039/c0md00148a · Cited by 9

Synthesis of 6-aryl/heteroaryl-4-oxo-4 H -chromene-2-carboxylic ethyl ester derivatives

Fernandes, C., Soares, P., Gaspar, A., Martins, D., Gomes, L. R., Low, J. N., & Borges, F. (2016) · Tetrahedron Letters · doi:10.1016/j.tetlet.2016.05.096 · Cited by 9

Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ) Inhibitors

Schwehm, C., Kellam, B., Garces, A. E., Hill, S. J., Kindon, N. D., Bradshaw, T. D., Li, J., Macdonald, S. J. F., Rowedder, J. E., Stoddart, L. A., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01801 · Cited by 9

Diversifying Complexity by Domino Benzannulation of Polycyclic Natural Products

Tejedor, D., Delgado‐Hernández, S., Carballo, R. M., Dapueto, R., Mena‐Rejón, G. J., & García‐Tellado, F. (2017) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.7b00654 · Cited by 9

Synthesis and Reactions of Benzannulated Spiroaminals: Tetrahydrospirobiquinolines

Almond-Thynne, J., White, A. J. P., Polyzos, A., Rzepa, H. S., Parsons, P. J., & Barrett, A. G. M. (2017) · ACS Omega · doi:10.1021/acsomega.7b00482 · Cited by 9

Mixed carboxylic–sulfonic anhydride in reaction with imines: a straightforward route to water-soluble β-lactams via a Staudinger-type reaction

Bakulina, O., Dar’in, D. V., & Krasavin, M. (2018) · Organic & Biomolecular Chemistry · doi:10.1039/c8ob00768c · Cited by 9

Design and synthesis of 2,6-disubstituted-8-amino imidazo[1,2a]pyridines, a promising privileged structure

Boulahjar, R., Arias, A. R., Bolteau, R., Renault, N., Coevoet, M., Barczyk, A., Duroux, R., Yous, S., Melnyk, P., & Agouridas, L. (2018) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2018.04.057 · Cited by 9

Synthesis of Chiral cis-Cyclopropane Bearing Indole and Chromone as Potential TNFα Inhibitors

Kanada, R., Tanabe, M., Muromoto, R., Sato, Y., Kuwahara, T., Fukuda, H., Arisawa, M., Matsuda, T., Watanabe, M., & Shuto, S. (2018) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.8b00466 · Cited by 9

Multitargeting Heterocycles

Singh, P. K., & Silakari, O. (2018) · Elsevier eBooks · doi:10.1016/b978-0-08-102083-8.00001-7 · Cited by 9

An Efficient Ugi‐Azide Four‐Component Approach for the Preparation of Novel 1‐(1H‐tetrazol‐5‐yl)‐10‐chloro‐1,2,3,4‐tetrahydropyrazino[1,2‐a] Indoles

Salahi, S., Ghandi, M., & Abbasi, A. (2019) · Journal of Heterocyclic Chemistry · doi:10.1002/jhet.3499 · Cited by 9

Site-Resolved and Quantitative Characterization of Very Weak Protein–Ligand Interactions

Fuglestad, B., Kerstetter, N. E., & Wand, A. J. (2019) · ACS Chemical Biology · doi:10.1021/acschembio.9b00353 · Cited by 9

Rapid construction of tetrahydropyridine scaffolds via formal imino Diels–Alder reactions of Schiff bases and Nazarov reagents

Wu, Y., & Rawal, V. H. (2019) · Organic & Biomolecular Chemistry · doi:10.1039/c9ob01880h · Cited by 9

Cluster analysis to identify prominent patterns of anti-hypertensives: A three-tiered unsupervised learning approach

Sharma, R. (2020) · Informatics in Medicine Unlocked · doi:10.1016/j.imu.2020.100303 · Cited by 9

Allosteric Modulators

Lu, S., & Zhang, J. (2016) · Elsevier eBooks · doi:10.1016/b978-0-12-409547-2.12324-8 · Cited by 9

Chemoproteomic Profiling of a Pharmacophore-Focused Chemical Library

Punzalan, L. L., Jiang, L., Mao, D., Mahapatra, A. D., Sato, S., Takemoto, Y., Tsujimura, M., Kusamori, K., Nishikawa, M., Zhou, L., et al. (2020) · Cell chemical biology · doi:10.1016/j.chembiol.2020.04.007 · Cited by 9

Synthesis and biological properties of a series of aryl alkyl disulfide derivatives

Joondan, N., Inassee, M. A. T., Bhowon, M. G., & Laulloo, S. J. (2020) · Heliyon · doi:10.1016/j.heliyon.2020.e05368 · Cited by 9

Fluorocyclization of Vinyl Azides for the Formation of 3‐Azido Heterocycles

Bai, D., Li, L., Li, X., Lü, Y., Wu, Y. Q., Reddy, B. R. P., & Ning, Y. (2020) · Chemistry - An Asian Journal · doi:10.1002/asia.202001175 · Cited by 9

CH-Diazomethane Sulfonamides Generated in Situ for Intramolecular [3+2] Cycloaddition of Alkynes: An Entry into Novel Pyrazole-Fused Five-Membered Sultams

Dar’in, D. V., Krasavin, M., Bubyrev, A. I., & Kantin, G. P. (2020) · Synthesis · doi:10.1055/a-1336-6857 · Cited by 9

Palladium Nanocatalysts for Cascade C−N Cross‐Coupling/Heck Reaction

Rodriguez‐Oliva, I., Losada‐Garcia, N., Santos, A. S., Marques, M. M. B., & Palomo, J. M. (2021) · Asian Journal of Organic Chemistry · doi:10.1002/ajoc.202100077 · Cited by 9

Copper-catalyzed synthesis of 1-(2-benzofuryl)-N-heteroarenes from o -hydroxy- gem -(dibromovinyl)benzenes and N-heteroarenes

Rao, M. L. N., & Islam, S. S. (2021) · Organic & Biomolecular Chemistry · doi:10.1039/d1ob01765a · Cited by 9

Transition‐Metal‐Free Catalyzed Dehydrative Coupling of Quinoline and Isoquinoline N‐Oxides with Propargylic Alcohols

Cai, Z., Feng, X., Zhang, Y., Lu, C., Han, Y., & Zhao, J. (2021) · Chinese Journal of Chemistry · doi:10.1002/cjoc.202100687 · Cited by 9

Decoding the Mechanism of Drugs of Heterocyclic Nature against Hepatocellular Carcinoma

Sugunan, S., Nath, L. R., Kumar, A. R., Anitha, L., Nair, B., & Mathew, B. (2022) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/1871520622666220418115310 · Cited by 9

Iridium-Catalyzed Borylation of 6-Fluoroquinolines: Access to 6-Fluoroquinolones

Hickey, A., Merz, J., Mamari, H. H. A., Friedrich, A., Marder, T. B., & McGlacken, G. P. (2022) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.2c00973 · Cited by 9

Identification of Small Molecules with Improved Potency against Orthopoxviruses from Vaccinia to Smallpox

Brown, L. E., Seitz, S., Kondas, A. V., Marcyk, P. T., Filone, C. M., Hossain, M. M., Schaus, S. E., Olson, V. A., & Connor, J. H. (2022) · Antimicrobial Agents and Chemotherapy · doi:10.1128/aac.00841-22 · Cited by 9

Synthesis and Conformational Analysis of Hydantoin-Based Universal Peptidomimetics

Caramiello, A. M., Bellucci, M. C., Cristina, G., Castellano, C., Meneghetti, F., Mori, M., Secundo, F., Viani, F., Sacchetti, A., & Volonterio, A. (2022) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.2c01903 · Cited by 9

Synthesis of structurally diverse silicon-incorporated indolines via silyl radical-triggered radical cascade reactions

Tian, Y., Zhao, J., Zheng, W.-X., Zhang, J., Wang, Z., & Zhang, F. (2023) · Organic Chemistry Frontiers · doi:10.1039/d3qo00153a · Cited by 9

Evidences of noncovalent interactions between indole and dichloromethane under different solvent conditions

Al-Otaibi, J. S., Mary, Y. S., Mary, Y. S., & Thomas, R. (2023) · Journal of Molecular Modeling · doi:10.1007/s00894-023-05623-3 · Cited by 9

Harnessing the Potential of Electron Donor–Acceptor Complexes and N-Centered Radicals: Expanding the Frontiers of Isoquinoline Derivative Synthesis

Yuan, Y., Faure, C., Berthelot, M., Belmont, P., & Brachet, E. (2024) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.4c00086 · Cited by 9

Solid phase synthesis of functionalized indazoles using triazenes – scope and limitations

Garcia, A. M., Jung, N., Gil, C., Nieger, M., & Bräse, S. (2015) · RSC Advances · doi:10.1039/c5ra09705c · Cited by 9

Synthesis and biological evaluation of new quinazolinone derivatives

Askar, F. W., Abbas, S. A. R., Al-Bayati, R. I., & Al-Tamemi, H. A. (2014) · European Journal of Chemistry · doi:10.5155/eurjchem.5.4.628-634.1120 · Cited by 9

The Design and Synthesis of 1,4-Substituted Piperazine Derivatives as Triple Reuptake Inhibitors

Han, M., Han, Y.-H., Song, C., & Hahn, H. (2012) · Bulletin of the Korean Chemical Society · doi:10.5012/bkcs.2012.33.8.2597 · Cited by 9

Synthesis and antiproliferative activity of 6-phenylaminopurines

Canela, M., Liekens, S., Camarasa, M., Priego, E., & Pérez‐Pérez, M. (2014) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2014.09.093 · Cited by 9

Synthesis of Molecular Frameworks Containing Two Distinct Heterocycles Connected in a Single Molecule with Enhanced Three‐Dimensional Shape Diversity

Lim, D., & Park, S. B. (2013) · Chemistry - A European Journal · doi:10.1002/chem.201204293 · Cited by 9

Gold(I)‐Catalyzed and Nucleophile‐Guided Ligand‐Directed Divergent Synthesis

Lee, Y., Knauer, L., Louven, K., Golz, C., Carsten Strohmann, B., Waldmann, H., & Kumar, K. (2018) · European Journal of Organic Chemistry · doi:10.1002/ejoc.201801080 · Cited by 9

Catalytic, selective, and stereocontrolled construction of C4 quaternary and homobenzylic dihydroisoquinolones by sp 3 C–H benzylation

Beng, T. K., & Moreno, A. (2020) · RSC Advances · doi:10.1039/c9ra10888b · Cited by 9

Data set of competitive and allosteric protein kinase inhibitors confirmed by X-ray crystallography

Hu, H., Laufkötter, O., Miljković, F. N., & Bajorath, J. (2021) · Data in Brief · doi:10.1016/j.dib.2021.106816 · Cited by 9

Techniques and Strategies in Drug Design and Discovery

Nițulescu, G. M. (2024) · International Journal of Molecular Sciences · doi:10.3390/ijms25031364 · Cited by 9

Chemoenzymatic One-Pot Process for the Synthesis of Tetrahydroisoquinolines

Klein, A., Albrecht, A. C., & Pietruszka, J. (2021) · Catalysts · doi:10.3390/catal11111389 · Cited by 8

Redox Relay-Induced C–S Radical Cross-Coupling Strategy: Application in Nontraditional Site-Selective Thiocyanation of Quinoxalinones

Shi, S., Li, H., Liu, H., Tian, R., & Zhu, H. (2024) · The Journal of Organic Chemistry · doi:10.1021/acs.joc.4c00215 · Cited by 8

The Chromenopyridine Scaffold: A Privileged Platform in Drug Design

de Lima, F. P., Costa, M. F., Sousa, A. R., & Proença, M. F. R. P. (2024) · Molecules · doi:10.3390/molecules29133004 · Cited by 8

Investigation on molecular and biomolecular spectroscopy of the novel 2BCA molecule to analyse its biological activities and binding interaction with nipah viral protein

Manogaran, K., Tamilmani, S., Sengeny, P., Venkatachalapathy, V. S. K., Mahadevan, M., Elangovan, K., Armaković, S., Armaković, S. J., & Abramović, B. (2024) · Spectrochimica Acta Part A Molecular and Biomolecular Spectroscopy · doi:10.1016/j.saa.2024.124737 · Cited by 8

Cooperative NHC and Photoredox Catalyzed Radical Aminoacylation of Alkenes to Tetrahydropyridazines

Liu, W., Gao, J., Mo, J., Zhou, Y., & Zhao, J. (2024) · Chemistry - A European Journal · doi:10.1002/chem.202402288 · Cited by 8

Going beyond SMILES enumeration for data augmentation in generative drug discovery

Brinkmann, H., Argante, A., ter Steege, H., & Grisoni, F. (2025) · Digital Discovery · doi:10.1039/d5dd00028a · Cited by 13

Chemoselective cyclodesulfurization vs. dehydration enabled by aqueous microdroplet chemistry

Jana, M., Saha, M., & Cooks, R. G. (2025) · Chemical Science · doi:10.1039/d5sc05557a · Cited by 8

Design and synthesis of [1,2,4]-triazolo isoquinoline derivatives via 1, 3-dipolar [3 + 2] cycloaddition: Reaction of azomethine imine with ethyl cyanoformate as unknown protocol

Swapnaja, K. J. M., Yennam, S., & Chavali, M. S. (2019) · Tetrahedron Letters · doi:10.1016/j.tetlet.2019.01.033 · Cited by 8

Novel substituted triazolo benzodiazepine scaffolds to explore chemical space

Abeykoon, G. A., Sahn, J. J., & Martin, S. F. (2021) · Tetrahedron Letters · doi:10.1016/j.tetlet.2021.152828 · Cited by 8

Photoinduced Copper‐Catalyzed Asymmetric C(sp 3 )−H Alkynylation of Cyclic Amines by Intramolecular 1,5‐Hydrogen Atom Transfer

Guo, R., Xiao, H., Li, S., Luo, Y., Bai, J., Zhang, M., Guo, Y., Qi, X., & Zhang, G. (2022) · Angewandte Chemie · doi:10.1002/ange.202208232 · Cited by 8

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Synthesis of novel 2H-spiro[1-benzofuran-3,4′-piperidin]ol scaffolds

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Microwave‐Assisted Expedite Synthesis of 2‐Phenylimidazo[1,2‐a]pyridylquinoxalin‐2(1H)‐ones

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New route to bioactive 2-(hetero)arylethylamines via nucleophilic ring opening in fused 7-acyl-2,3-dihydroazepines

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Arylhydrazono/Aryldiazenyl Pyrazoles: Green One-Pot Solvent-Free Synthesis and Anticancer Evaluation

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A review on synthetic procedures and applications of phosphorus oxychloride (POCl3) in the last biennial period (2018–19)

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Global Assessment of Substituents on the Basis of Analogue Series

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Fragment‐based screening and hit‐based substructure search: Rapid discovery of 8‐hydroxyquinoline‐7‐carboxylic acid as a low‐cytotoxic, nanomolar metallo β‐lactamase inhibitor

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Spectroscopic characterization, DFT calculations, and microbiological activity of 5-iodoindole

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

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Catalyst-free and atom-economical [4+3] cycloaddition of azadienes with cyclic azomethine imines for facile synthesis of 1,2,4-triazepines

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Reductive Buchwald‐Hartwig Amination of Nitroarenes with Aryl (pseudo)Halides

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A simple one-pot 2-step N-1-alkylation of indoles with α-iminoketones toward the expeditious 3-step synthesis of N-1-quinoxaline-indoles

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Facile Pd-catalyzed amination of imidazolin-1-yl chloroazines under microwave irradiation: toward a new kinase-inhibitory chemotype

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ASDB: a resource for probing protein functions with small molecules

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Pd‐Catalyzed Reductive Carbonylation‐Ring Closure of Aryl Halides: A Direct Approach for Synthesis of Benzimidazoles

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Identification of spirocyclic or phosphate substituted quinolizine derivatives as novel HIV-1 integrase inhibitors: a patent evaluation of WO2016094197A1, WO2016094198A1 and WO2016154527A1

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The synthesis of 2-amino-4(3H)-quinazolinones and related heterocycles via a mild electrocyclization of aryl guanidines

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

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Scaffold composition and biological relevance of screening libraries

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