Design and Discovery of N-(2-Methyl-5′-morpholino-6′-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers-Reference-Cited by-同舟云学术

Design and Discovery of N-(2-Methyl-5′-morpholino-6′-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3′-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers

Published:2017-06-08 Issue:12 Volume:60 Page:4869-4881
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Nishiguchi Gisele A.¹,Rico Alice²,Tanner Huw²,Aversa Robert J.¹^ORCID,Taft Benjamin R.²,Subramanian Sharadha²,Setti Lina²,Burger Matthew T.¹,Wan Lifeng²,Tamez Victoriano¹,Smith Aaron²,Lou Yan²,Barsanti Paul A.²,Appleton Brent A.²,Mamo Mulugeta²,Tandeske Laura³,Dix Ina⁴,Tellew John E.⁵,Huang Shenlin⁵,Mathews Griner Lesley A.⁶,Cooke Vesselina G.⁶,Van Abbema Anne³,Merritt Hanne³,Ma Sylvia³,Gampa Kalyani⁶,Feng Fei⁶,Yuan Jing⁶,Wang Yingyun³,Haling Jacob R.⁵,Vaziri Sepideh⁵,Hekmat-Nejad Mohammad³,Jansen Johanna M.²,Polyakov Valery²,Zang Richard²,Sethuraman Vijay³,Amiri Payman³,Singh Mallika³,Lees Emma⁶,Shao Wenlin⁶,Stuart Darrin D.⁶,Dillon Michael P.¹,Ramurthy Savithri²^ORCID

Affiliation:

1. Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States

2. Global Discovery Chemistry, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States

3. Oncology, Novartis Institutes for BioMedical Research, 5300 Chiron Way, Emeryville, California 94608, United States

4. Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Novartis Pharma AG, Werk Klybeck, Postfach, CH-4002 Basel, Switzerland

5. Genomics Institute of the Novartis Research Foundation, 10675 John Hopkins Drive, San Diego, California 92121, United States

6. Oncology, Novartis Institutes for BioMedical Research, 250 Massachusetts Avenue, Cambridge, Massachusetts 02139, United States

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.6b01862

Reference25 articles.

1. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

2. Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism

3. Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State

4. C-Raf Is Required for the Initiation of Lung Cancer by K-RasG12D

5. c-Raf, but Not B-Raf, Is Essential for Development of K-Ras Oncogene-Driven Non-Small Cell Lung Carcinoma

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