Literature DB >> 25221654

Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.

Sharadha Subramanian1, Abran Costales1, Teresa E Williams1, Barry Levine1, Christopher M McBride1, Daniel Poon1, Payman Amiri1, Paul A Renhowe1, Cynthia M Shafer1, Darrin Stuart1, Joelle Verhagen1, Savithri Ramurthy1.   

Abstract

Benzimidazole reverse amides were designed and synthesized as Pan RAF kinase inhibitors. Investigation of the structure-activity relationship of the compounds revealed that they were potent in vitro and exhibited desirable in vivo properties.

Entities:  

Keywords:  CSF1R; MAP; RTKs; STKs; TKs; VEGF; colony stimulating factor-1 receptor; ras-mitogen activated protein kinase; receptor tyrosine kinases; serine threonine kinases; tyrosine kinases; vascular endothelial growth factor receptor

Year:  2014        PMID： 25221654      PMCID： PMC4160747          DOI： 10.1021/ml5002272

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  5 in total

1.  Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors.

Authors:  Savithri Ramurthy; Sharadha Subramanian; Mina Aikawa; Payman Amiri; Abran Costales; Jeff Dove; Susan Fong; Johanna M Jansen; Barry Levine; Sylvia Ma; Christopher M McBride; Jonah Michaelian; Teresa Pick; Daniel J Poon; Sandhya Girish; Cynthia M Shafer; Darrin Stuart; Leonard Sung; Paul A Renhowe
Journal:  J Med Chem       Date:  2008-11-27       Impact factor: 7.446

2.  Design and synthesis of 5,6-fused heterocyclic amides as Raf kinase inhibitors.

Authors:  Savithri Ramurthy; Mina Aikawa; Payman Amiri; Abran Costales; Ahmad Hashash; Johanna M Jansen; Song Lin; Sylvia Ma; Paul A Renhowe; Cynthia M Shafer; Sharadha Subramanian; Leonard Sung; Joelle Verhagen
Journal:  Bioorg Med Chem Lett       Date:  2011-04-14       Impact factor: 2.823

3.  Inhibition of mutated, activated BRAF in metastatic melanoma.

Authors:  Keith T Flaherty; Igor Puzanov; Kevin B Kim; Antoni Ribas; Grant A McArthur; Jeffrey A Sosman; Peter J O'Dwyer; Richard J Lee; Joseph F Grippo; Keith Nolop; Paul B Chapman
Journal:  N Engl J Med       Date:  2010-08-26       Impact factor: 91.245

Review 4.  ras oncogenes in human cancer: a review.

Authors:  J L Bos
Journal:  Cancer Res       Date:  1989-09-01       Impact factor: 12.701

5.  Mutations of the BRAF gene in human cancer.

Authors:  Helen Davies; Graham R Bignell; Charles Cox; Philip Stephens; Sarah Edkins; Sheila Clegg; Jon Teague; Hayley Woffendin; Mathew J Garnett; William Bottomley; Neil Davis; Ed Dicks; Rebecca Ewing; Yvonne Floyd; Kristian Gray; Sarah Hall; Rachel Hawes; Jaime Hughes; Vivian Kosmidou; Andrew Menzies; Catherine Mould; Adrian Parker; Claire Stevens; Stephen Watt; Steven Hooper; Rebecca Wilson; Hiran Jayatilake; Barry A Gusterson; Colin Cooper; Janet Shipley; Darren Hargrave; Katherine Pritchard-Jones; Norman Maitland; Georgia Chenevix-Trench; Gregory J Riggins; Darell D Bigner; Giuseppe Palmieri; Antonio Cossu; Adrienne Flanagan; Andrew Nicholson; Judy W C Ho; Suet Y Leung; Siu T Yuen; Barbara L Weber; Hilliard F Seigler; Timothy L Darrow; Hugh Paterson; Richard Marais; Christopher J Marshall; Richard Wooster; Michael R Stratton; P Andrew Futreal
Journal:  Nature       Date:  2002-06-09       Impact factor: 49.962
  5 in total
  2 in total

1.  Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.

Authors:  Teresa E Williams; Sharadha Subramanian; Joelle Verhagen; Christopher M McBride; Abran Costales; Leonard Sung; William Antonios-McCrea; Maureen McKenna; Alicia K Louie; Savithri Ramurthy; Barry Levine; Cynthia M Shafer; Timothy Machajewski; Paul A Renhowe; Brent A Appleton; Payman Amiri; James Chou; Darrin Stuart; Kimberly Aardalen; Daniel Poon
Journal:  ACS Med Chem Lett       Date:  2015-08-03       Impact factor: 4.345

2.  Synthesis, Bioactivity Assessment, and Molecular Docking of Non-sulfonamide Benzimidazole-Derived N-Acylhydrazone Scaffolds as Carbonic Anhydrase-II Inhibitors.

Authors:  Muhammad Saadiq; Ghias Uddin; Abdul Latif; Mumtaz Ali; Nazia Akbar; Sardar Ali; Manzoor Ahmad; Mohammad Zahoor; Ajmal Khan; Ahmed Al-Harrasi
Journal:  ACS Omega       Date:  2021-12-20
  2 in total

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