Literature DB >> 14741289

Omega-carboxypyridyl substituted ureas as Raf kinase inhibitors: SAR of the amide substituent.

Uday R Khire1, Donald Bankston, James Barbosa, David R Brittelli, Yolanda Caringal, Robert Carlson, Jacques Dumas, Todd Gane, Sarah L Heald, Barbara Hibner, Jeffrey S Johnson, Michael E Katz, Nancy Kennure, Jill Kingery-Wood, Wendy Lee, Xiao-Gao Liu, Timothy B Lowinger, Ian McAlexander, Mary-Katherine Monahan, Reina Natero, Joel Renick, Bernd Riedl, Hong Rong, Robert N Sibley, Roger A Smith, Donald Wolanin.   

Abstract

Bis-aryl ureas have been disclosed previously as a potent class of Raf kinase inhibitors. Modifications in the amide portion led to an improvement in aqueous solubility, an important characteristic for an oral drug. Based on this finding, we hypothesize that this portion of the molecule is directed towards the solvent in Raf-1.

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Year:  2004        PMID: 14741289     DOI: 10.1016/j.bmcl.2003.11.041

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


  10 in total

1.  In vitro inhibition of translation initiation by N,N'-diarylureas--potential anti-cancer agents.

Authors:  Séverine Denoyelle; Ting Chen; Limo Chen; Yibo Wang; Edvin Klosi; José A Halperin; Bertal H Aktas; Michael Chorev
Journal:  Bioorg Med Chem Lett       Date:  2011-11-16       Impact factor: 2.823

Review 2.  Small-molecule inhibitors of the ERK signaling pathway: Towards novel anticancer therapeutics.

Authors:  Jeremy L Yap; Shilpa Worlikar; Alexander D MacKerell; Paul Shapiro; Steven Fletcher
Journal:  ChemMedChem       Date:  2011-01-03       Impact factor: 3.466

3.  4-[4-(3-Methoxy-benzamido)phen-oxy]-N-methyl-picolinamide.

Authors:  Na-Na Meng; Ting-Ting Huang; De-Kuan Li; Wen-Xin Zhang; Luo-Ting Yu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-01-30

4.  The crystal structure of BRAF in complex with an organoruthenium inhibitor reveals a mechanism for inhibition of an active form of BRAF kinase.

Authors:  Peng Xie; Craig Streu; Jie Qin; Howard Bregman; Nicholas Pagano; Eric Meggers; Ronen Marmorstein
Journal:  Biochemistry       Date:  2009-06-16       Impact factor: 3.162

5.  4-{[4-(3,5-Dimeth-oxy-benzamido)-phen-yl]sulfan-yl}-N-methyl-pyridine-2-carboxamide.

Authors:  Ting-Ting Huang; Na-Na Meng; Xiao-Yu Qing; Luo-Ting Yu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-03-12

6.  N,N'-Bis(4-fluoro-phen-yl)urea.

Authors:  Wan-Sin Loh; Hoong-Kun Fun; S Sarveswari; V Vijayakumar; R Venkat Ragavan
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-05-12

7.  N-Methyl-4-(4-pivalamido-phenyl-sulfan-yl)picolinamide hemihydrate.

Authors:  Ting-Hong Ye; Ting-Ting Huang; Yao-Jie Shi; Ying Xiong; Luo-Ting Yu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-04-13

8.  Personalizing colon cancer therapeutics: targeting old and new mechanisms of action.

Authors:  Christina Leah B Kline; Wafik S El-Deiry
Journal:  Pharmaceuticals (Basel)       Date:  2013-08-21

9.  A general approach for retrosynthetic molecular core analysis.

Authors:  J Jesús Naveja; B Angélica Pilón-Jiménez; Jürgen Bajorath; José L Medina-Franco
Journal:  J Cheminform       Date:  2019-09-24       Impact factor: 5.514

10.  The RAS/mitogen activated protein (MAP) kinase pathway in melanoma biology and therapeutics.

Authors:  Abel D Jarell; Donald Lawrence; Hensin Tsao
Journal:  Biologics       Date:  2007-12
  10 in total

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