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

Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis

Dixon, S. J., Patel, D. N., Welsch, M., Skouta, R., Lee, E. D., Hayano, M., Thomas, A. G., Gleason, C. E., Tatonetti, N. P., Slusher, B. S., et al. (2014) · eLife · doi:10.7554/elife.02523 · Cited by 2,088

Click Chemistry for Drug Development and Diverse Chemical–Biology Applications

Prakasam, T., Matosiuk, D., & Jóźwiak, K. (2013) · Chemical Reviews · doi:10.1021/cr200409f · Cited by 1,933

Chalcone: A Privileged Structure in Medicinal Chemistry

Zhuang, C., Zhang, W., Sheng, C., Zhang, W., Xing, C., & Miao, Z. (2017) · Chemical Reviews · doi:10.1021/acs.chemrev.7b00020 · Cited by 1,538

Deep reinforcement learning for de novo drug design

Popova, M., Isayev, O., & Tropsha, A. (2018) · Science Advances · doi:10.1126/sciadv.aap7885 · Cited by 1,433

Single-electron transmetalation in organoboron cross-coupling by photoredox/nickel dual catalysis

Tellis, J. C., Primer, D. N., & Molander, G. A. (2014) · Science · doi:10.1126/science.1253647 · Cited by 1,295

A review on recent developments of indole-containing antiviral agents

Zhang, M., Chen, Q., & Yang, G. (2014) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2014.10.065 · Cited by 892

Medicinal attributes of 1,2,3-triazoles: Current developments

Dheer, D., Singh, V., & Shankar, R. (2017) · Bioorganic Chemistry · doi:10.1016/j.bioorg.2017.01.010 · Cited by 884

Tetrazoles via Multicomponent Reactions

Neochoritis, C. G., Zhao, T. K., & Dömling, A. S. S. (2019) · Chemical Reviews · doi:10.1021/acs.chemrev.8b00564 · Cited by 610

Recent developments in solvent-free multicomponent reactions: a perfect synergy for eco-compatible organic synthesis

Singh, M. S., & Chowdhury, S. (2012) · RSC Advances · doi:10.1039/c2ra01056a · Cited by 506

When Light Meets Nitrogen-Centered Radicals: From Reagents to Catalysts

Yu, X., Zhao, Q., Chen, J., Xiao, W., & Chen, J. (2020) · Accounts of Chemical Research · doi:10.1021/acs.accounts.0c00090 · Cited by 508

Rings in Clinical Trials and Drugs: Present and Future

Shearer, J., Castro, J. L., Lawson, A. D. G., MacCoss, M., & Taylor, R. D. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c00473 · Cited by 499

Ligand and Target Discovery by Fragment-Based Screening in Human Cells

Parker, C. G., Galmozzi, A., Wang, Y., Correia, B. E., Sasaki, K., Joslyn, C. M., Kim, A. S., Cavallaro, C. L., Lawrence, R. M., Johnson, S. R., et al. (2017) · Cell · doi:10.1016/j.cell.2016.12.029 · Cited by 439

Recent advances in spirocyclization of indole derivatives

Bariwal, J. B., Voskressensky, L. G., & der Eycken, E. V. V. (2018) · Chemical Society Reviews · doi:10.1039/c7cs00508c · Cited by 426

Visible‐Light‐Mediated Generation of Nitrogen‐Centered Radicals: Metal‐Free Hydroimination and Iminohydroxylation Cyclization Reactions

Davies, J., Booth, S. G., Labouille, S., Dryfe, R. A. W., & Leonori, D. (2015) · Angewandte Chemie International Edition · doi:10.1002/anie.201507641 · Cited by 426

Iridium-Catalyzed C–H Borylation of Heteroarenes: Scope, Regioselectivity, Application to Late-Stage Functionalization, and Mechanism

Larsen, M. A., & Hartwig, J. F. (2014) · Journal of the American Chemical Society · doi:10.1021/ja412563e · Cited by 418

Asymmetric organocatalysis: an enabling technology for medicinal chemistry

Han, B., He, X., Liu, Y., He, G., Peng, C. Y., & Li, J. (2021) · Chemical Society Reviews · doi:10.1039/d0cs00196a · Cited by 409

Synergistic Dual Transition Metal Catalysis

Kim, U. B., Jung, D. J., Jeon, H. J., Rathwell, K., & Lee, S. (2020) · Chemical Reviews · doi:10.1021/acs.chemrev.0c00245 · Cited by 405

Discovery and Characterization of Sulfoxaflor, a Novel Insecticide Targeting Sap-Feeding Pests

Zhu, Y., Loso, M. R., Watson, G. B., Sparks, T. C., Rogers, R. B., Huang, J. X., Gerwick, B. C., Babcock, J. M., Kelley, D. R., Hegde, V. B., et al. (2010) · Journal of Agricultural and Food Chemistry · doi:10.1021/jf102765x · Cited by 382

Electrochemically Driven, Ni-Catalyzed Aryl Amination: Scope, Mechanism, and Applications

Kawamata, Y., Vantourout, J. C., Hickey, D. P., Bai, P., Chen, L., Hou, Q., Qiao, W., Barman, K., Edwards, M. A., Garrido‐Castro, A. F., et al. (2019) · Journal of the American Chemical Society · doi:10.1021/jacs.9b01886 · Cited by 375

Liquid‐Assisted Grinding Mechanochemistry in the Synthesis of Pharmaceuticals

Ying, P., Yu, J., & Su, W. (2021) · Advanced Synthesis & Catalysis · doi:10.1002/adsc.202001245 · Cited by 374

The Open Access Malaria Box: A Drug Discovery Catalyst for Neglected Diseases

Spangenberg, T., Burrows, J. N., Kowalczyk, P., McDonald, S., Wells, T. N. C., & Willis, P. A. (2013) · PLoS ONE · doi:10.1371/journal.pone.0062906 · Cited by 345

Synthesis of Spirocyclic Indolenines

James, M. J., O’Brien, P., Taylor, R. J. K., & Unsworth, W. P. (2015) · Chemistry - A European Journal · doi:10.1002/chem.201503835 · Cited by 339

Visible-Light-Mediated Synthesis of Amidyl Radicals: Transition-Metal-Free Hydroamination and N -Arylation Reactions

Davies, J., Svejstrup, T. D., Reina, D. F., Sheikh, N. S., & Leonori, D. (2016) · Journal of the American Chemical Society · doi:10.1021/jacs.6b04920 · Cited by 338

Photoredox-mediated Minisci C–H alkylation of N-heteroarenes using boronic acids and hypervalent iodine

Li, G., Morales-Rivera, C. A., Wang, Y., Gao, F., He, G., Liu, P., & Chen, G. (2016) · Chemical Science · doi:10.1039/c6sc02653b · Cited by 331

Catalytic Enantioselective Construction of Spiro Quaternary Carbon Stereocenters

Xu, P., Yu, J., Chen, C., Cao, Z., Zhou, F., & Zhou, J. E. (2019) · ACS Catalysis · doi:10.1021/acscatal.8b03694 · Cited by 322

Single-Electron Transmetalation: An Enabling Technology for Secondary Alkylboron Cross-Coupling

Primer, D. N., Karakaya, İ., Tellis, J. C., & Molander, G. A. (2015) · Journal of the American Chemical Society · doi:10.1021/ja512946e · Cited by 323

Iminosugars as Therapeutic Agents: Recent Advances and Promising Trends

Nash, R. J., Kato, A., Yu, C.-Y., & Fleet, G. W. J. (2011) · Future Medicinal Chemistry · doi:10.4155/fmc.11.117 · Cited by 302

Recent Developments in Ruthenium-Catalyzed C–H Arylation: Array of Mechanistic Manifolds

Nareddy, P. R., Jordan, F., & Szostak, M. (2017) · ACS Catalysis · doi:10.1021/acscatal.7b01645 · Cited by 291

Base-Free Photoredox/Nickel Dual-Catalytic Cross-Coupling of Ammonium Alkylsilicates

Jouffroy, M., Primer, D. N., & Molander, G. A. (2015) · Journal of the American Chemical Society · doi:10.1021/jacs.5b10963 · Cited by 292

Metal-free C–H alkylation of heteroarenes with alkyltrifluoroborates: a general protocol for 1°, 2° and 3° alkylation

Matsui, J. K., Primer, D. N., & Molander, G. A. (2017) · Chemical Science · doi:10.1039/c7sc00283a · Cited by 284

Nicotinic Acetylcholine Receptor Agonists: A Milestone for Modern Crop Protection

Jeschke, P., Nauen, R., & Beck, M. E. (2013) · Angewandte Chemie International Edition · doi:10.1002/anie.201302550 · Cited by 269

Recent advances in catalyst-free photochemical reactions via electron-donor-acceptor (EDA) complex process

Yuan, Y., Majumder, S., Yang, M., & Guo, S. (2019) · Tetrahedron Letters · doi:10.1016/j.tetlet.2019.151506 · Cited by 263

Unique motifs and hydrophobic interactions shape the binding of modified DNA ligands to protein targets

Davies, D. R., Gelinas, A. D., Zhang, C., Rohloff, J. C., Carter, J. D., O’Connell, D., Waugh, S. M., Wolk, S. K., Mayfield, W. S., Burgin, A. B., et al. (2012) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1213933109 · Cited by 257

Late-Stage C–H Alkylation of Heterocycles and 1,4-Quinones via Oxidative Homolysis of 1,4-Dihydropyridines

Gutiérrez‐Bonet, Á., Remeur, C., Matsui, J. K., & Molander, G. A. (2017) · Journal of the American Chemical Society · doi:10.1021/jacs.7b05899 · Cited by 255

An overview of quinoline as a privileged scaffold in cancer drug discovery

Musioł, R. (2017) · Expert Opinion on Drug Discovery · doi:10.1080/17460441.2017.1319357 · Cited by 255

Natural product derived privileged scaffolds in drug discovery

Davison, E. K., & Brimble, M. A. (2019) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2018.12.007 · Cited by 249

Bioengineering of plant (tri)terpenoids: from metabolic engineering of plants to synthetic biology in vivo and in vitro

Moses, T., Pollier, J., Thevelein, J. M., & Goossens, A. (2013) · New Phytologist · doi:10.1111/nph.12325 · Cited by 245

Palladium‐Catalyzed Synthesis of Benzofurans and Coumarins from Phenols and Olefins

Sharma, U. K., Naveen, T., Maji, A., Manna, S., & Maiti, D. (2013) · Angewandte Chemie International Edition · doi:10.1002/anie.201305326 · Cited by 224

Heteroatom–Heteroatom Bond Formation in Natural Product Biosynthesis

Waldman, A. J., Ng, T. L., Wang, P., & Balskus, E. P. (2017) · Chemical Reviews · doi:10.1021/acs.chemrev.6b00621 · Cited by 227

Natural products as starting points for the synthesis of complex and diverse compounds

Morrison, K. C., & Hergenrother, P. J. (2013) · Natural Product Reports · doi:10.1039/c3np70063a · Cited by 222

Redox-Neutral Indole Annulation Cascades

Haibach, M. C., Deb, I., De, C. K., & Seidel, D. (2011) · Journal of the American Chemical Society · doi:10.1021/ja110713k · Cited by 211

A Versatile Approach to Ullmann C–N Couplings at Room Temperature: New Families of Nucleophiles and Electrophiles for Photoinduced, Copper-Catalyzed Processes

Ziegler, D. T., Choi, J., Muñoz‐Molina, J. M., Bissember, A. C., Peters, J. C., & Fu, G. C. (2013) · Journal of the American Chemical Society · doi:10.1021/ja4060806 · Cited by 202

Deaminative Reductive Arylation Enabled by Nickel/Photoredox Dual Catalysis

Yi, J., Badir, S. O., Kammer, L. M., Ribagorda, M., & Molander, G. A. (2019) · Organic Letters · doi:10.1021/acs.orglett.9b01097 · Cited by 199

DCAF11 Supports Targeted Protein Degradation by Electrophilic Proteolysis-Targeting Chimeras

Zhang, X., Luukkonen, L. M., Eissler, C. L., Crowley, V. M., Yamashita, Y., Schafroth, M. A., Kikuchi, S., Weinstein, D. S., Symons, K. T., Nordin, B. E., et al. (2021) · Journal of the American Chemical Society · doi:10.1021/jacs.1c00990 · Cited by 199

Mild Rhodium(III)‐Catalyzed Cyclization of Amides with α,β‐Unsaturated Aldehydes and Ketones to Azepinones: Application to the Synthesis of the Homoprotoberberine Framework

Shi, Z., Grohmann, C., & Glorius, F. (2013) · Angewandte Chemie International Edition · doi:10.1002/anie.201301426 · Cited by 195

5-Ene-4-thiazolidinones – An efficient tool in medicinal chemistry

Kaminskyy, D. V., Kryshchyshyn‐Dylevych, A., & Lesyk, R. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.09.031 · Cited by 195

Site-selective Suzuki–Miyaura coupling of heteroaryl halides – understanding the trends for pharmaceutically important classes

Almond-Thynne, J., Blakemore, D. C., Pryde, D. C., & Spivey, A. C. (2016) · Chemical Science · doi:10.1039/c6sc02118b · Cited by 185

Copper-Catalyzed Aerobic [3+2]-Annulation of N-Alkenyl Amidines

Wang, Y., Zhu, X. H., & Chiba, S. (2012) · Journal of the American Chemical Society · doi:10.1021/ja2120629 · Cited by 184

The Azaindole Framework in the Design of Kinase Inhibitors

MEROUR, J. Y., Buron, F., Plé, K., Bonnet, P., & Routier, S. (2014) · Molecules · doi:10.3390/molecules191219935 · Cited by 180

Expedited mapping of the ligandable proteome using fully functionalized enantiomeric probe pairs

Wang, Y., Dix, M. M., Bianco, G., Remsberg, J. R., Lee, H.-Y., Kalocsay, M., Gygi, S. P., Forli, S., Vite, G., Lawrence, R. M., et al. (2019) · Nature Chemistry · doi:10.1038/s41557-019-0351-5 · Cited by 179

Informatics and Computational Methods in Natural Product Drug Discovery: A Review and Perspectives

Romano, J. D., & Tatonetti, N. P. (2019) · Frontiers in Genetics · doi:10.3389/fgene.2019.00368 · Cited by 183

Chiral Amine Synthesis Using ω‐Transaminases: An Amine Donor that Displaces Equilibria and Enables High‐Throughput Screening

Green, A. P., Turner, N. J., & O’Reilly, E. (2014) · Angewandte Chemie International Edition · doi:10.1002/anie.201406571 · Cited by 180

Applications of visible light photoredox catalysis to the synthesis of natural products and related compounds

Nicholls, T. P., Leonori, D., & Bissember, A. C. (2016) · Natural Product Reports · doi:10.1039/c6np00070c · Cited by 181

The Symbiotic Relationship Between Drug Discovery and Organic Chemistry

Grygorenko, O. O., Volochnyuk, D. M., Ryabukhin, S. V., & Judd, D. B. (2019) · Chemistry - A European Journal · doi:10.1002/chem.201903232 · Cited by 174

Scaffold-based molecular design with a graph generative model

Lim, J., Hwang, S.-Y., Moon, S., Kim, S., & Kim, W. Y. (2019) · Chemical Science · doi:10.1039/c9sc04503a · Cited by 180

Discovery of orally active anticancer candidate CFI-400945 derived from biologically promising spirooxindoles: Success and challenges

Yu, B., Yu, Z., Qi, P., Yu, D., & Liu, H. (2015) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2015.03.020 · Cited by 171

Current strategies for diversity-oriented synthesis

Dandapani, S., & Marcaurelle, L. A. (2010) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2010.03.018 · Cited by 172

Computational Exploration of Molecular Scaffolds in Medicinal Chemistry

Hu, Y., Stumpfe, D., & Bajorath, J. (2016) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01746 · Cited by 163

Treatment of opioid use disorder with ibogaine: detoxification and drug use outcomes

Brown, T. K., & Alper, K. (2017) · The American Journal of Drug and Alcohol Abuse · doi:10.1080/00952990.2017.1320802 · Cited by 164

Mushroom-Derived Indole Alkaloids

Homer, J. A., & Sperry, J. (2017) · Journal of Natural Products · doi:10.1021/acs.jnatprod.7b00390 · Cited by 160

Heterocyclic N-Oxides - An Emerging Class of Therapeutic Agents

Mfuh, A. M., & Larionov, O. V. (2015) · Current Medicinal Chemistry · doi:10.2174/0929867322666150619104007 · Cited by 159

Bayesian semi-supervised learning for uncertainty-calibrated prediction of molecular properties and active learning

Zhang, Y., & Lee, A. A. (2019) · Chemical Science · doi:10.1039/c9sc00616h · Cited by 162

An (R)‐Imine Reductase Biocatalyst for the Asymmetric Reduction of Cyclic Imines

Hussain, S., Leipold, F., Man, H., Wells, E., France, S. P., Mulholland, K. R., Grogan, G., & Turner, N. J. (2015) · ChemCatChem · doi:10.1002/cctc.201402797 · Cited by 155

Visible-light-mediated Minisci C–H alkylation of heteroarenes with unactivated alkyl halides using O 2 as an oxidant

Dong, J., Lyu, X., Wang, Z., Wang, X., Song, H., Liu, Y., & Wang, Q. (2018) · Chemical Science · doi:10.1039/c8sc04892d · Cited by 152

A Practical Lewis Base Catalyzed Electrophilic Chlorination of Arenes and Heterocycles

Maddox, S. M., Nalbandian, C. J., Smith, D. E., & Gustafson, J. L. (2015) · Organic Letters · doi:10.1021/acs.orglett.5b00186 · Cited by 147

Regioselective Metal-Free Cross-Coupling of Quinoline N-Oxides with Boronic Acids

Bering, L., & Antonchick, A. P. (2015) · Organic Letters · doi:10.1021/acs.orglett.5b01456 · Cited by 144

Direct, Catalytic, and Regioselective Synthesis of 2-Alkyl-, Aryl-, and Alkenyl-Substituted N-Heterocycles from N-Oxides

Larionov, O. V., Stephens, D. E., Mfuh, A. M., & Chavez, G. (2014) · Organic Letters · doi:10.1021/ol403631k · Cited by 143

Synthesis of Arylamines via Aminium Radicals

Svejstrup, T. D., Ruffoni, A., Juliá, F., Aubert, V. M., & Leonori, D. (2017) · Angewandte Chemie International Edition · doi:10.1002/anie.201708693 · Cited by 144

Skeletal Editing of (Hetero)Arenes Using Carbenes

Liu, Z., Sivaguru, P., Ning, Y., Wu, Y. Q., & Bi, X. (2023) · Chemistry - A European Journal · doi:10.1002/chem.202301227 · Cited by 143

Reversible modulation of interlayer stacking in 2D copper-organic frameworks for tailoring porosity and photocatalytic activity

You, P., Mo, K., Wang, Y., Gao, Q., Lin, X., Lin, J., Xie, M., Wei, R., Ning, G., & Li, D. (2024) · Nature Communications · doi:10.1038/s41467-023-44552-w · Cited by 142

Site-Selective Cross-Coupling of Polyhalogenated Arenes and Heteroarenes with Identical Halogen Groups

Palani, V., Perea, M. A., & Sarpong, R. (2021) · Chemical Reviews · doi:10.1021/acs.chemrev.1c00513 · Cited by 141

On the origins of drug polypharmacology

Jalencas, X., & Mestres, J. (2012) · MedChemComm · doi:10.1039/c2md20242e · Cited by 142

Carbazole Derivatives as Antiviral Agents: An Overview

Caruso, A., Ceramella, J., Iacopetta, D., Saturnino, C., Mauro, M. V., Bruno, R., Aquaro, S., & Sinicropi, M. S. (2019) · Molecules · doi:10.3390/molecules24101912 · Cited by 132

Novel Pyrrolopyrimidine-Based α-Helix Mimetics: Cell-Permeable Inhibitors of Protein−Protein Interactions

Lee, J. H., Zhang, Q., Jo, S., Chai, S. C., Oh, M., Im, W., Lu, H., & Lim, H. (2010) · Journal of the American Chemical Society · doi:10.1021/ja108230s · Cited by 126

Neurotrophic Natural Products: Chemistry and Biology

Xu, J., Lacoske, M. H., & Theodorakis, E. A. (2013) · Angewandte Chemie International Edition · doi:10.1002/anie.201302268 · Cited by 124

Privileged Structures Revisited

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

Nitrogen atom insertion into indenes to access isoquinolines

Finkelstein, P., Reisenbauer, J. C., Botlik, B. B., Green, O., Florin, A., & Morandi, B. (2023) · Chemical Science · doi:10.1039/d2sc06952k · Cited by 127

Extending the small-molecule similarity principle to all levels of biology with the Chemical Checker

Duran-Frigola, M., Pauls, E., Guitart-Pla, O., Bertoni, M., Alcalde, V., Amat, D., Juan-Blanco, T., & Aloy, P. (2020) · Nature Biotechnology · doi:10.1038/s41587-020-0502-7 · Cited by 126

Rhodanine hydrolysis leads to potent thioenolate mediated metallo-β-lactamase inhibition

Brem, J., van Berkel, S. S., Aik, W. S., Rydzik, A. M., Avison, M. B., Pettinati, I., Umland, K., Kawamura, A., SPENCER, J. M., Claridge, T. D. W., et al. (2014) · Nature Chemistry · doi:10.1038/nchem.2110 · Cited by 125

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 International Edition · doi:10.1002/anie.201310193 · Cited by 125

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 International Edition · doi:10.1002/anie.201605714 · Cited by 125

Site-selective remote C(sp3)–H heteroarylation of amides via organic photoredox catalysis

Chen, H., Fan, W., Yuan, X., & Yu, S. (2019) · Nature Communications · doi:10.1038/s41467-019-12722-4 · Cited by 123

Visible‐Light‐Mediated Generation of Nitrogen‐Centered Radicals: Metal‐Free Hydroimination and Iminohydroxylation Cyclization Reactions

Davies, J., Booth, S. G., Labouille, S., Dryfe, R. A. W., & Leonori, D. (2015) · Angewandte Chemie · doi:10.1002/ange.201507641 · Cited by 121

Catalytic asymmetric synthesis of polysubstituted spirocyclopropyl oxindoles: organocatalysis versus transition metal catalysis

Cao, Z., & Zhou, J. E. (2015) · Organic Chemistry Frontiers · doi:10.1039/c5qo00092k · Cited by 120

BET bromodomain inhibitors: a patent review

Garnier, J., Sharp, P. P., & Burns, C. J. (2013) · Expert Opinion on Therapeutic Patents · doi:10.1517/13543776.2014.859244 · Cited by 122

Oxidative Geminal Functionalization of Organoboron Compounds

He, Z., Trinchera, P., Adachi, S., Denis, J. D. S., & Yudin, A. K. (2012) · Angewandte Chemie International Edition · doi:10.1002/anie.201206501 · Cited by 120

Metal-, Photocatalyst-, and Light-Free, Late-Stage C–H Alkylation of Heteroarenes and 1,4-Quinones Using Carboxylic Acids

Sutherland, D. R., Veguillas, M., Oates, C. L., & Lee, A. (2018) · Organic Letters · doi:10.1021/acs.orglett.8b02988 · Cited by 118

Copper-Catalyzed Aliphatic C–H Amination with an Amidine Moiety

Chen, H., Sanjaya, S., Wang, Y., & Chiba, S. (2012) · Organic Letters · doi:10.1021/ol303302r · Cited by 117

Iridium-Catalyzed Enantioselective α-C(sp3)–H Borylation of Azacycles

Chen, L., Yang, Y., Liu, L., Gao, Q., & Xu, S. (2020) · Journal of the American Chemical Society · doi:10.1021/jacs.0c06756 · Cited by 117

Visible-Light-Induced C(sp3)–H Oxidative Arylation with Heteroarenes

Liang, X., Niu, L., Wang, S., Liu, J., & Lei, A. (2019) · Organic Letters · doi:10.1021/acs.orglett.9b00744 · Cited by 115

Visible Light-Mediated Decarboxylative Alkylation of Pharmaceutically Relevant Heterocycles

Sun, A. C., McClain, E. J., Beatty, J. W., & Stephenson, C. R. J. (2018) · Organic Letters · doi:10.1021/acs.orglett.8b01250 · Cited by 114

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 International Edition · doi:10.1002/anie.201705855 · Cited by 113

Photocatalytic Cross-Dehydrogenative Amination Reactions between Phenols and Diarylamines

Zhao, Y., Huang, B., Yang, C., Li, B., Gou, B., & Xia, W. (2017) · ACS Catalysis · doi:10.1021/acscatal.7b00192 · Cited by 112

Ligand‐Enabled Enantioselective C–H Activation of Tetrahydroquinolines and Saturated Aza‐Heterocycles by RhI

Greßies, S., Klauck, F. J. R., Kim, J. H., Daniliuc, C. G., & Glorius, F. (2018) · Angewandte Chemie International Edition · doi:10.1002/anie.201805680 · Cited by 112

Detection of Parasitic Plant Suicide Germination Compounds Using a High-Throughput Arabidopsis HTL/KAI2 Strigolactone Perception System

Toh, S., Holbrook‐Smith, D., Stokes, M. E., Tsuchiya, Y., & McCourt, P. (2014) · Chemistry & Biology · doi:10.1016/j.chembiol.2014.07.005 · Cited by 111

Aminoboration: Addition of B–N σ Bonds across C–C π Bonds

Chong, E., & Blum, S. A. (2015) · Journal of the American Chemical Society · doi:10.1021/jacs.5b06678 · Cited by 109

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 International Edition · doi:10.1002/anie.201705848 · Cited by 109

Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents

Camacho, J., Barazarte, A. R., Gamboa, N., Rodrigues, J. R., Rojas, R., Vaisberg, A., Gilman, R., & Charris, J. (2011) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2011.01.050 · Cited by 109

Copper-Catalyzed Dicarbofunctionalization of Unactivated Olefins by Tandem Cyclization/Cross-Coupling

Thapa, S., Basnet, P., & Giri, R. (2017) · Journal of the American Chemical Society · doi:10.1021/jacs.7b01922 · Cited by 108

Building better bioorthogonal reactions

Shih, H., Kamber, D. N., & Prescher, J. A. (2014) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2014.07.002 · Cited by 107

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