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Organic Synthesis Toward Small-Molecule Probes and Drugs Special Feature


  • Stuart L. Schreiber
  • From the Cover: Organic synthesis toward small-molecule probes and drugs
  • PNAS 2011 108:6699-6702; doi:10.1073/pnas.1103205108
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  • Nicolas Lecomte, Jon T. Njardarson, Pavel Nagorny, Guangli Yang, Robert Downey, Ouathek Ouerfelli, Malcolm A. S. Moore, and Samuel J. Danishefsky
  • Emergence of potent inhibitors of metastasis in lung cancer via syntheses based on migrastatin
  • PNAS 2011 108:15074-15078; doi:10.1073/pnas.1015247108
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  • K. C. Nicolaou, Silvano Sanchini, David Sarlah, Gang Lu, T. Robert Wu, Daniel K. Nomura, Benjamin F. Cravatt, Beatrice Cubitt, Juan C. de la Torre, Ann J. Hessell, and Dennis R. Burton
  • Design, synthesis, and biological evaluation of a biyouyanagin compound library
  • PNAS 2011 108:6703-6708; doi:10.1073/pnas.1015252108
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  • Paul A. Wender, Jeremy L. Baryza, Stacey E. Brenner, Brian A. DeChristopher, Brian A. Loy, Adam J. Schrier, and Vishal A. Verma
  • Design, synthesis, and evaluation of potent bryostatin analogs that modulate PKC translocation selectivity
  • PNAS 2011 108:6703-6708; doi:10.1073/pnas.1015252108
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  • Kevin J. Frankowski, Vincent Setola, Jon M. Evans, Ben Neuenswander, Bryan L. Roth, and Jeffrey Aubé
  • Synthesis and receptor profiling of Stemona alkaloid analogues reveal a potent class of sigma ligands
  • PNAS 2011 108:6727-6732; doi:10.1073/pnas.1016558108
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  • Daniel S. Palacios, Ian Dailey, David M. Siebert, Brandon C. Wilcock, and Martin D. Burke
  • Synthesis-enabled functional group deletions reveal key underpinnings of amphotericin B ion channel and antifungal activities
  • PNAS 2011 108:6733-6738; doi:10.1073/pnas.1015023108
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  • Aurelio Bonavia, Michael Franti, Erin Pusateri Keaney, Kelli Kuhen, Mohindra Seepersaud, Branko Radetich, Jian Shao, Ayako Honda, Janetta Dewhurst, Kara Balabanis, James Monroe, Karen Wolff, Colin Osborne, Leanne Lanieri, Keith Hoffmaster, Jakal Amin, Judit Markovits, Michelle Broome, Elizabeth Skuba, Ivan Cornella-Taracido, Gerard Joberty, Tewis Bouwmeester, Lawrence Hamann, John A. Tallarico, Ruben Tommasi, Teresa Compton, and Simon M. Bushell
  • Identification of broad-spectrum antiviral compounds and assessment of the druggability of their target for efficacy against respiratory syncytial virus (RSV)
  • PNAS 2011 108:6739-6744; doi:10.1073/pnas.1017142108
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  • Gustavo Moura-Letts, Christine M. DiBlasi, Renato A. Bauer, and Derek S. Tan
  • Solid-phase synthesis and chemical space analysis of a 190-membered alkaloid/terpenoid-like library
  • PNAS 2011 108:6745-6750; doi:10.1073/pnas.1015268108
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  • Eamon Comer, Haibo Liu, Adrien Joliton, Alexandre Clabaut, Christopher Johnson, Lakshmi B. Akella, and Lisa A. Marcaurelle
  • Fragment-based domain shuffling approach for the synthesis of pyran-based macrocycles
  • PNAS 2011 108:6751-6756; doi:10.1073/pnas.1015255108
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  • Donna M. Huryn, Jeffrey L. Brodsky, Kay M. Brummond, Peter G. Chambers, Benjamin Eyer, Alex W. Ireland, Masaoki Kawasumi, Matthew G. LaPorte, Kayla Lloyd, Baptiste Manteau, Paul Nghiem, Bettina Quade, Sandlin P. Seguin, and Peter Wipf
  • Chemical methodology as a source of small-molecule checkpoint inhibitors and heat shock protein 70 (Hsp70) modulators
  • PNAS 2011 108:6757-6762; doi:10.1073/pnas.1015251108
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  • Jiayue Cui, Jason Hao, Olesya A. Ulanovskaya, Joseph Dundas, Jie Liang, and Sergey A. Kozmin
  • Creation and manipulation of common functional groups en route to a skeletally diverse chemical library
  • PNAS 2011 108:6763-6768; doi:10.1073/pnas.1015253108
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  • Daniel Cruz, Zhiming Wang, Jon Kibbie, Robert Modlin, and Ohyun Kwon
  • Diversity through phosphine catalysis identifies octahydro-1,6-naphthyridin-4-ones as activators of endothelium-driven immunity
  • PNAS 2011 108:6769-6774; doi:10.1073/pnas.1015254108
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  • Lauren E. Brown, Ken Chih-Chien Cheng, Wan-Guo Wei, Pingwei Yuan, Peng Dai, Richard Trilles, Feng Ni, Jing Yuan, Ryan MacArthur, Rajarshi Guha, Ronald L. Johnson, Xin-zhuan Su, Melissa M. Dominguez, John K. Snyder, Aaron B. Beeler, Scott E. Schaus, James Inglese, and John A. Porco, Jr.
  • Discovery of new antimalarial chemotypes through chemical methodology and library development
  • PNAS 2011 108:6775-6780; doi:10.1073/pnas.1017666108
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  • Amos B. Smith, III, and Won-Suk Kim
  • Diversity-oriented synthesis leads to an effective class of bifunctional linchpins uniting anion relay chemistry (ARC) with benzyne reactivity
  • PNAS 2011 108:6787-6792; doi:10.1073/pnas.1015265108
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  • Albert Isidro-Llobet, Tiffanie Murillo, Paula Bello, Agostino Cilibrizzi, James T. Hodgkinson, Warren R. J. D. Galloway, Andreas Bender, Martin Welch, and David R. Spring
  • Diversity-oriented synthesis of macrocyclic peptidomimetics
  • PNAS 2011 108:6793-6798; doi:10.1073/pnas.1015267108
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  • Alvin W. Hung, Alex Ramek, Yikai Wang, Taner Kaya, J. Anthony Wilson, Paul A. Clemons, and Damian W. Young
  • Route to three-dimensional fragments using diversity-oriented synthesis
  • PNAS 2011 108:6727-6732; doi:10.1073/pnas.1016558108
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  • Sudipta Basu, Bernhard Ellinger, Stefano Rizzo, Céline Deraeve, Markus Schürmann, Hans Preut, Hans-Dieter Arndt, and Herbert Waldmann
  • Biology-oriented synthesis of a natural-product inspired oxepane collection yields a small-molecule activator of the Wnt-pathway
  • PNAS 2011 108:6805-6810; doi:10.1073/pnas.1015269108
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  • Daniel A. Bachovchin, Justin T. Mohr, Anna E. Speers, Chu Wang, Jacob M. Berlin, Timothy P. Spicer, Virneliz Fernandez-Vega, Peter Chase, Peter S. Hodder, Stephan C. Schürer, Daniel K. Nomura, Hugh Rosen, Gregory C. Fu, and Benjamin F. Cravatt
  • Academic cross-fertilization by public screening yields a remarkable class of protein phosphatase methylesterase-1 inhibitors
  • PNAS 2011 108:6811-6816; doi:10.1073/pnas.1015248108
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  • Paul A. Clemons, J. Anthony Wilson, Vlado Dancík, Sandrine Muller, Hyman A. Carrinski, Bridget K. Wagner, Angela N. Koehler, and Stuart L. Schreiber
  • Quantifying structure and performance diversity for sets of small molecules comprising small-molecule screening collections
  • PNAS 2011 108:6817-6822; doi:10.1073/pnas.1015024108
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