Literature DB >> 20541934

Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.

Xianming Deng1, Sang Min Lim, Jianming Zhang, Nathanael S Gray.   

Abstract

A series of alkyne-containing type II inhibitors with potent inhibitory activity of T315I Bcr-Abl has been identified. The most active compound 4 exhibits an EC(50) of less than 1 nM against wild-type Bcr-Abl and an EC(50) of 10 nM against T315I mutant but is broadly active against a number of other kinases. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20541934      PMCID： PMC2901992          DOI： 10.1016/j.bmcl.2010.05.043

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


  18 in total

1.  Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants.

Authors:  Ellen Weisberg; Hwan Geun Choi; Arghya Ray; Rosemary Barrett; Jianming Zhang; Taebo Sim; Wenjun Zhou; Markus Seeliger; Michael Cameron; Mohammed Azam; Jonathan A Fletcher; Maria Debiec-Rychter; Mark Mayeda; Daisy Moreno; Andrew L Kung; Pasi Antero Janne; Roya Khosravi-Far; Junia V Melo; Paul W Manley; Sophia Adamia; Catherine Wu; Nathanael Gray; James D Griffin
Journal:  Blood       Date:  2010-03-18       Impact factor: 22.113

2.  A quantitative analysis of kinase inhibitor selectivity.

Authors:  Mazen W Karaman; Sanna Herrgard; Daniel K Treiber; Paul Gallant; Corey E Atteridge; Brian T Campbell; Katrina W Chan; Pietro Ciceri; Mindy I Davis; Philip T Edeen; Raffaella Faraoni; Mark Floyd; Jeremy P Hunt; Daniel J Lockhart; Zdravko V Milanov; Michael J Morrison; Gabriel Pallares; Hitesh K Patel; Stephanie Pritchard; Lisa M Wodicka; Patrick P Zarrinkar
Journal:  Nat Biotechnol       Date:  2008-01       Impact factor: 54.908

3.  Structural mechanism for STI-571 inhibition of abelson tyrosine kinase.

Authors:  T Schindler; W Bornmann; P Pellicena; W T Miller; B Clarkson; J Kuriyan
Journal:  Science       Date:  2000-09-15       Impact factor: 47.728

4.  The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants.

Authors:  John S Tokarski; John A Newitt; Chieh Ying J Chang; Janet D Cheng; Michael Wittekind; Susan E Kiefer; Kevin Kish; Francis Y F Lee; Robert Borzillerri; Louis J Lombardo; Dianlin Xie; Yaqun Zhang; Herbert E Klei
Journal:  Cancer Res       Date:  2006-06-01       Impact factor: 12.701

5.  Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia.

Authors:  B J Druker; M Talpaz; D J Resta; B Peng; E Buchdunger; J M Ford; N B Lydon; H Kantarjian; R Capdeville; S Ohno-Jones; C L Sawyers
Journal:  N Engl J Med       Date:  2001-04-05       Impact factor: 91.245

6.  Overriding imatinib resistance with a novel ABL kinase inhibitor.

Authors:  Neil P Shah; Chris Tran; Francis Y Lee; Ping Chen; Derek Norris; Charles L Sawyers
Journal:  Science       Date:  2004-07-16       Impact factor: 47.728

7.  A phase 2 study of imatinib in patients with relapsed or refractory Philadelphia chromosome-positive acute lymphoid leukemias.

Authors:  Oliver G Ottmann; Brian J Druker; Charles L Sawyers; John M Goldman; Jose Reiffers; Richard T Silver; Sante Tura; Thomas Fischer; Michael W Deininger; Charles A Schiffer; Michele Baccarani; Alois Gratwohl; Andreas Hochhaus; Dieter Hoelzer; Sofia Fernandes-Reese; Insa Gathmann; Renaud Capdeville; Stephen G O'Brien
Journal:  Blood       Date:  2002-09-15       Impact factor: 22.113

8.  9-(Arenethenyl)purines as dual Src/Abl kinase inhibitors targeting the inactive conformation: design, synthesis, and biological evaluation.

Authors:  Wei-Sheng Huang; Xiaotian Zhu; Yihan Wang; Mohammad Azam; David Wen; Raji Sundaramoorthi; R Mathew Thomas; Shuangying Liu; Geetha Banda; Scott P Lentini; Sasmita Das; Qihong Xu; Jeff Keats; Frank Wang; Scott Wardwell; Yaoyu Ning; Joseph T Snodgrass; Marc I Broudy; Karin Russian; George Q Daley; John Iuliucci; David C Dalgarno; Tim Clackson; Tomi K Sawyer; William C Shakespeare
Journal:  J Med Chem       Date:  2009-08-13       Impact factor: 7.446

9.  Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

Authors:  Ellen Weisberg; Paul W Manley; Werner Breitenstein; Josef Brüggen; Sandra W Cowan-Jacob; Arghya Ray; Brian Huntly; Doriano Fabbro; Gabriele Fendrich; Elizabeth Hall-Meyers; Andrew L Kung; Jürgen Mestan; George Q Daley; Linda Callahan; Laurie Catley; Cara Cavazza; Mohammad Azam; Azam Mohammed; Donna Neuberg; Renee D Wright; D Gary Gilliland; James D Griffin
Journal:  Cancer Cell       Date:  2005-02       Impact factor: 31.743

10.  Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations.

Authors:  Markus A Seeliger; Pratistha Ranjitkar; Corynn Kasap; Yibing Shan; David E Shaw; Neil P Shah; John Kuriyan; Dustin J Maly
Journal:  Cancer Res       Date:  2009-03-10       Impact factor: 12.701
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  3 in total

1.  Development of 'DFG-out' inhibitors of gatekeeper mutant kinases.

Authors:  Hwan Geun Choi; Jianming Zhang; Ellen Weisberg; James D Griffin; Taebo Sim; Nathanael S Gray
Journal:  Bioorg Med Chem Lett       Date:  2012-06-23       Impact factor: 2.823

2.  Identification of common inhibitors of wild-type and T315I mutant of BCR-ABL through the parallel structure-based virtual screening.

Authors:  Hwangseo Park; Seunghee Hong; Sungwoo Hong
Journal:  J Comput Aided Mol Des       Date:  2012-08-11       Impact factor: 3.686

3.  Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase.

Authors:  Marialuisa Moccia; Qingsong Liu; Teresa Guida; Giorgia Federico; Annalisa Brescia; Zheng Zhao; Hwan Geun Choi; Xianming Deng; Li Tan; Jinhua Wang; Marc Billaud; Nathanael S Gray; Francesca Carlomagno; Massimo Santoro
Journal:  PLoS One       Date:  2015-06-05       Impact factor: 3.240
  3 in total

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