946125-91-3Relevant articles and documents
MEK INHIBITORS AND THERAPEUTIC USES THEREOF
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Paragraph 0352; 0394; 0402; 0561, (2021/07/17)
The present disclosure provides compounds, compositions containing such compounds, and methods of designing, developing, producing and preparing compounds represented by general Formula (I), including pharmaceutically acceptable salts thereof or a synthetic intermediate thereof. The compounds act as MEK inhibitors and are capable of displaying one or more beneficial therapeutic effects, including treating cancer.
The sulfamide moiety affords higher inhibitory activity and oral bioavailability to a series of coumarin dual selective RAF/MEK inhibitors
Aoki, Toshihiro,Hyohdoh, Ikumi,Furuichi, Noriyuki,Ozawa, Sawako,Watanabe, Fumio,Matsushita, Masayuki,Sakaitani, Masahiro,Ori, Kazutomo,Takanashi, Kenji,Harada, Naoki,Tomii, Yasushi,Tabo, Mitsuyasu,Yoshinari, Kiyoshi,Aoki, Yuko,Shimma, Nobuo,Iikura, Hitoshi
, p. 6223 - 6227 (2013/11/19)
Introducing a sulfamide moiety to our coumarin derivatives afforded enhanced Raf/MEK inhibitory activity concomitantly with an acceptable PK profile. Novel sulfamide 17 showed potent HCT116 cell growth inhibition (IC 50 = 8 nM) and good PK prof
