Literature DB >> 22727638

An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFRα and kit.

Xianming Deng1, Wenjun Zhou, Ellen Weisberg, Jinhua Wang, Jianming Zhang, Takaaki Sasaki, Erik Nelson, James D Griffin, Pasi A Jänne, Nathanael S Gray.   

Abstract

Here we describe the synthesis and characterization of a number of 3-amino-1H-indazol-6-yl-benzamides that were designed to target the 'DFG-out' conformation of the kinase activation loop. Several compounds such as 4 and 11 exhibit single-digit nanomolar EC(50)s against FLT3, c-Kit and the gatekeeper T674M mutant of PDGFRα.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 22727638      PMCID： PMC3547541          DOI： 10.1016/j.bmcl.2012.05.107

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


  14 in total

1.  An efficient rapid system for profiling the cellular activities of molecular libraries.

Authors:  Jonathan S Melnick; Jeff Janes; Sungjoon Kim; Jim Y Chang; Daniel G Sipes; Drew Gunderson; Laura Jarnes; Jason T Matzen; Michael E Garcia; Tami L Hood; Ronak Beigi; Gang Xia; Richard A Harig; Hayk Asatryan; S Frank Yan; Yingyao Zhou; Xiang-Ju Gu; Alham Saadat; Vicki Zhou; Frederick J King; Christopher M Shaw; Andrew I Su; Robert Downs; Nathanael S Gray; Peter G Schultz; Markus Warmuth; Jeremy S Caldwell
Journal:  Proc Natl Acad Sci U S A       Date:  2006-02-21       Impact factor: 11.205

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

Review 3.  Targeting cancer with small molecule kinase inhibitors.

Authors:  Jianming Zhang; Priscilla L Yang; Nathanael S Gray
Journal:  Nat Rev Cancer       Date:  2009-01       Impact factor: 60.716

4.  Structure-based design of potent and selective 3-phosphoinositide-dependent kinase-1 (PDK1) inhibitors.

Authors:  Jesús R Medina; Christopher J Becker; Charles W Blackledge; Celine Duquenne; Yanhong Feng; Seth W Grant; Dirk Heerding; William H Li; William H Miller; Stuart P Romeril; Daryl Scherzer; Arthur Shu; Mark A Bobko; Antony R Chadderton; Melissa Dumble; Christine M Gardiner; Seth Gilbert; Qi Liu; Sridhar K Rabindran; Valery Sudakin; Hong Xiang; Pat G Brady; Nino Campobasso; Paris Ward; Jeffrey M Axten
Journal:  J Med Chem       Date:  2011-02-22       Impact factor: 7.446

5.  Rational design of inhibitors that bind to inactive kinase conformations.

Authors:  Yi Liu; Nathanael S Gray
Journal:  Nat Chem Biol       Date:  2006-07       Impact factor: 15.040

6.  c-Src binds to the cancer drug imatinib with an inactive Abl/c-Kit conformation and a distributed thermodynamic penalty.

Authors:  Markus A Seeliger; Bhushan Nagar; Filipp Frank; Xiaoxian Cao; M Nidanie Henderson; John Kuriyan
Journal:  Structure       Date:  2007-03       Impact factor: 5.006

7.  PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer.

Authors:  Patrizia Carpinelli; Roberta Ceruti; Maria Laura Giorgini; Paolo Cappella; Laura Gianellini; Valter Croci; Anna Degrassi; Gemma Texido; Maurizio Rocchetti; Paola Vianello; Luisa Rusconi; Paola Storici; Paola Zugnoni; Claudio Arrigoni; Chiara Soncini; Cristina Alli; Veronica Patton; Aurelio Marsiglio; Dario Ballinari; Enrico Pesenti; Daniele Fancelli; Jürgen Moll
Journal:  Mol Cancer Ther       Date:  2007-12       Impact factor: 6.261

8.  AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.

Authors:  Thomas O'Hare; William C Shakespeare; Xiaotian Zhu; Christopher A Eide; Victor M Rivera; Frank Wang; Lauren T Adrian; Tianjun Zhou; Wei-Sheng Huang; Qihong Xu; Chester A Metcalf; Jeffrey W Tyner; Marc M Loriaux; Amie S Corbin; Scott Wardwell; Yaoyu Ning; Jeffrey A Keats; Yihan Wang; Raji Sundaramoorthi; Mathew Thomas; Dong Zhou; Joseph Snodgrass; Lois Commodore; Tomi K Sawyer; David C Dalgarno; Michael W N Deininger; Brian J Druker; Tim Clackson
Journal:  Cancer Cell       Date:  2009-11-06       Impact factor: 31.743

9.  Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.

Authors:  Yujia Dai; Kresna Hartandi; Zhiqin Ji; Asma A Ahmed; Daniel H Albert; Joy L Bauch; Jennifer J Bouska; Peter F Bousquet; George A Cunha; Keith B Glaser; Christopher M Harris; Dean Hickman; Jun Guo; Junling Li; Patrick A Marcotte; Kennan C Marsh; Maria D Moskey; Ruth L Martin; Amanda M Olson; Donald J Osterling; Lori J Pease; Niru B Soni; Kent D Stewart; Vincent S Stoll; Paul Tapang; David R Reuter; Steven K Davidsen; Michael R Michaelides
Journal:  J Med Chem       Date:  2007-03-08       Impact factor: 7.446

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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  1 in total

1.  Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.

Authors:  Aurélie Mallinger; Kai Schiemann; Christian Rink; Frank Stieber; Michel Calderini; Simon Crumpler; Mark Stubbs; Olajumoke Adeniji-Popoola; Oliver Poeschke; Michael Busch; Paul Czodrowski; Djordje Musil; Daniel Schwarz; Maria-Jesus Ortiz-Ruiz; Richard Schneider; Ching Thai; Melanie Valenti; Alexis de Haven Brandon; Rosemary Burke; Paul Workman; Trevor Dale; Dirk Wienke; Paul A Clarke; Christina Esdar; Florence I Raynaud; Suzanne A Eccles; Felix Rohdich; Julian Blagg
Journal:  J Med Chem       Date:  2016-01-21       Impact factor: 7.446
  1 in total

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