Literature DB >> 20189383

Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres.

Frederick Cohen1, Michael F T Koehler, Philippe Bergeron, Linda O Elliott, John A Flygare, Matthew C Franklin, Lewis Gazzard, Stephen F Keteltas, Kevin Lau, Cuong Q Ly, Vickie Tsui, Wayne J Fairbrother.   

Abstract

A series of IAP antagonists based on thiazole or benzothiazole amide isosteres was designed and synthesized. These compounds were tested for binding to the XIAP-BIR3 and ML-IAP BIR using a fluorescence polarization assay. The most potent of these compounds, 19a and 33b, were found to have K(i)'s of 20-30 nM against ML-IAP and 50-60 nM against XIAP-BIR3. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20189383     DOI： 10.1016/j.bmcl.2010.02.021

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  7 in total

1.  Synthesis of sansalvamide A peptidomimetics: triazole, oxazole, thiazole, and pseudoproline containing compounds.

Authors:  Melinda R Davis; Erinprit K Singh; Hendra Wahyudi; Leslie D Alexander; Joseph B Kunicki; Lidia A Nazarova; Kelly A Fairweather; Andrew M Giltrap; Katrina A Jolliffe; Shelli R McAlpine
Journal:  Tetrahedron       Date:  2012-01-28       Impact factor: 2.457

2.  Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).

Authors:  John A Flygare; Maureen Beresini; Nageshwar Budha; Helen Chan; Iris T Chan; Sravanthi Cheeti; Frederick Cohen; Kurt Deshayes; Karl Doerner; S Gail Eckhardt; Linda O Elliott; Bainian Feng; Matthew C Franklin; Stacy Frankovitz Reisner; Lewis Gazzard; Jason Halladay; Sarah G Hymowitz; Hank La; Patricia LoRusso; Brigitte Maurer; Lesley Murray; Emile Plise; Clifford Quan; Jean-Philippe Stephan; Shin G Young; Jeffrey Tom; Vickie Tsui; Joanne Um; Eugene Varfolomeev; Domagoj Vucic; Andrew J Wagner; Heidi J A Wallweber; Lan Wang; Joseph Ware; Zhaoyang Wen; Harvey Wong; Jonathan M Wong; Melisa Wong; Susan Wong; Ron Yu; Kerry Zobel; Wayne J Fairbrother
Journal:  J Med Chem       Date:  2012-03-28       Impact factor: 7.446

3.  Recognition of Smac-mimetic compounds by the BIR domain of cIAP1.

Authors:  Federica Cossu; Francesca Malvezzi; Giulia Canevari; Eloise Mastrangelo; Daniele Lecis; Domenico Delia; Pierfausto Seneci; Carlo Scolastico; Martino Bolognesi; Mario Milani
Journal:  Protein Sci       Date:  2010-12       Impact factor: 6.725

4.  Expedient synthesis of highly potent antagonists of inhibitor of apoptosis proteins (IAPs) with unique selectivity for ML-IAP.

Authors:  Mitchell Vamos; Kate Welsh; Darren Finlay; Pooi San Lee; Peter D Mace; Scott J Snipas; Monica L Gonzalez; Santhi Reddy Ganji; Robert J Ardecky; Stefan J Riedl; Guy S Salvesen; Kristiina Vuori; John C Reed; Nicholas D P Cosford
Journal:  ACS Chem Biol       Date:  2013-02-05       Impact factor: 5.100

5.  Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation.

Authors:  Nobumichi Ohoka; Yoko Morita; Katsunori Nagai; Kenichiro Shimokawa; Osamu Ujikawa; Ikuo Fujimori; Masahiro Ito; Youji Hayase; Keiichiro Okuhira; Norihito Shibata; Takayuki Hattori; Tomoya Sameshima; Osamu Sano; Ryokichi Koyama; Yasuhiro Imaeda; Hiroshi Nara; Nobuo Cho; Mikihiko Naito
Journal:  J Biol Chem       Date:  2018-03-15       Impact factor: 5.157

6.  2-(4-Bromo-phen-yl)-5-dodec-yloxy-1,3-thia-zole.

Authors:  Hugo Gallardo; Deise M P O Santos; Adailton J Bortoluzzi
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-08-21

Review 7.  Pharmacological Potential and Synthetic Approaches of Imidazo[4,5-b]pyridine and Imidazo[4,5-c]pyridine Derivatives.

Authors:  Malwina Krause; Henryk Foks; Katarzyna Gobis
Journal:  Molecules       Date:  2017-03-04       Impact factor: 4.411
  7 in total

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