1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives: A novel type II Raf kinase inhibitors

Bioorganic & Medicinal Chemistry Letters
2010.0

Abstract

The synthesis of a novel series of 1,4-dihydropyrazolo[4,3-d]imidazole phenyl derivatives 1a-b, 2a-v and their antiproliferative activities against A375P and WM3629 human melanoma cell line were described. Most compounds showed competitive antiproliferative activities to sorafenib, the reference standard. Among them, pyrazoloimidazole phenyl urea compounds 2a, 2d, 2g, 2i, 2t exhibited potent activities on WM3629 cell lines (IC(50)=0.56-0.86 microM). Especially, 2t was found to be a potent and selective C-Raf inhibitor, showing a possibility as melanoma therapeutics.

Knowledge Graph

Similar Paper

1,4-Dihydropyrazolo[4,3-d]imidazole phenyl derivatives: A novel type II Raf kinase inhibitors
Bioorganic & Medicinal Chemistry Letters 2010.0
Discovery and initial SAR of pyrimidin-4-yl-1H-imidazole derivatives with antiproliferative activity against melanoma cell lines
Bioorganic & Medicinal Chemistry Letters 2010.0
Structure based design and syntheses of amino-1H-pyrazole amide derivatives as selective Raf kinase inhibitors in melanoma cells
Bioorganic & Medicinal Chemistry 2011.0
Design, synthesis and biological evaluation of benzyl 2-(1H-imidazole-1-yl) pyrimidine analogues as selective and potent Raf inhibitors
Bioorganic & Medicinal Chemistry Letters 2014.0
Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells
Bioorganic & Medicinal Chemistry 2011.0
Design, synthesis and antitumor activities of novel bis-aryl ureas derivatives as Raf kinase inhibitors
Bioorganic & Medicinal Chemistry 2012.0
Discovery of New Imidazo[2,1-b]thiazole Derivatives as Potent Pan-RAF Inhibitors with Promising In Vitro and In Vivo Anti-melanoma Activity
Journal of Medicinal Chemistry 2021.0
3,3-Dimethyl-1H-pyrrolo[3,2-g]quinolin-2(3H)-one derivatives as novel Raf kinase inhibitors
Med. Chem. Commun. 2012.0
Synthesis of pyrrolo[2,3-d]pyrimidine derivatives and their antiproliferative activity against melanoma cell line
Bioorganic & Medicinal Chemistry Letters 2009.0
New diarylureas and diarylamides containing 1,3,4-triarylpyrazole scaffold: Synthesis, antiproliferative evaluation against melanoma cell lines, ERK kinase inhibition, and molecular docking studies
European Journal of Medicinal Chemistry 2011.0