Literature DB >> 18942827

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

Savithri Ramurthy1, 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.   

Abstract

A series of arylaminobenzimidazoles was designed and synthesized as Raf kinase inhibitors. Exploration of the structure-activity relationship resulted in compounds that are potent in vitro and show desirable in vivo properties.

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Year:  2008        PMID: 18942827     DOI: 10.1021/jm801050k

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  12 in total

1.  RAF265, a dual BRAF and VEGFR2 inhibitor, prevents osteoclast formation and resorption. Therapeutic implications.

Authors:  Antonio Garcia-Gomez; Enrique M Ocio; Atanasio Pandiella; Jesús F San Miguel; Mercedes Garayoa
Journal:  Invest New Drugs       Date:  2012-07-07       Impact factor: 3.850

2.  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

Review 3.  Targeting the mitogen-activated protein kinase pathway: physiological feedback and drug response.

Authors:  Christine A Pratilas; David B Solit
Journal:  Clin Cancer Res       Date:  2010-05-14       Impact factor: 12.531

4.  Development of a novel class of B-Raf(V600E)-selective inhibitors through virtual screening and hierarchical hit optimization.

Authors:  Xiangqian Kong; Jie Qin; Zeng Li; Adina Vultur; Linjiang Tong; Enguang Feng; Geena Rajan; Shien Liu; Junyan Lu; Zhongjie Liang; Mingyue Zheng; Weiliang Zhu; Hualiang Jiang; Meenhard Herlyn; Hong Liu; Ronen Marmorstein; Cheng Luo
Journal:  Org Biomol Chem       Date:  2012-09-28       Impact factor: 3.876

5.  Physicochemical property-driven optimization of diarylaniline compounds as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.

Authors:  Na Liu; Bingjie Qin; Lian-Qi Sun; Fei Yu; Lu Lu; Shibo Jiang; Kuo-Hsiung Lee; Lan Xie
Journal:  Bioorg Med Chem Lett       Date:  2014-07-11       Impact factor: 2.823

6.  RAF265 inhibits the growth of advanced human melanoma tumors.

Authors:  Yingjun Su; Anna E Vilgelm; Mark C Kelley; Oriana E Hawkins; Yan Liu; Kelli L Boyd; Sara Kantrow; Ryan C Splittgerber; Sarah P Short; Tammy Sobolik; Snjezana Zaja-Milatovic; Kimberly Brown Dahlman; Katayoun I Amiri; Aixiang Jiang; Pengcheng Lu; Yu Shyr; Darrin D Stuart; Shawn Levy; Jeffrey A Sosman; Ann Richmond
Journal:  Clin Cancer Res       Date:  2012-02-20       Impact factor: 12.531

7.  Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors.

Authors:  Sung Hee Hwang; Aaron T Wecksler; Guodong Zhang; Christophe Morisseau; Long V Nguyen; Samuel H Fu; Bruce D Hammock
Journal:  Bioorg Med Chem Lett       Date:  2013-05-15       Impact factor: 2.823

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

Authors:  Sharadha Subramanian; Abran Costales; Teresa E Williams; Barry Levine; Christopher M McBride; Daniel Poon; Payman Amiri; Paul A Renhowe; Cynthia M Shafer; Darrin Stuart; Joelle Verhagen; Savithri Ramurthy
Journal:  ACS Med Chem Lett       Date:  2014-07-17       Impact factor: 4.345

9.  A novel, selective, and efficacious nanomolar pyridopyrazinone inhibitor of V600EBRAF.

Authors:  Steven Whittaker; Delphine Ménard; Ruth Kirk; Lesley Ogilvie; Douglas Hedley; Alfonso Zambon; Filipa Lopes; Natasha Preece; Helen Manne; Sareena Rana; Maryou Lambros; Jorge S Reis-Filho; Richard Marais; Caroline J Springer
Journal:  Cancer Res       Date:  2010-08-31       Impact factor: 12.701

10.  Synthesis and characterization of some novel diaryl urea derivatives bearing quinoxalindione moiety.

Authors:  Sedighe Sadeghian-Rizi; Ghadamali Khodarahmi; Amirhossein Sakhteman; Ali Jahanian-Najafabadi; Mahboubeh Rostami; Mahmoud Mirzaei; Farshid Hassanzadeh
Journal:  Res Pharm Sci       Date:  2018-02
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