… : Synthesis and Structure-Activity Relationships of 7-[3-(Cyclohexylmethyl) ureido]-3-{1-methyl-1H-pyrrolo [2, 3-b] pyridin-3-yl} quinoxalin-2 (1H)-one Derivatives

…, K Niitsu, S Takeda, M Aburada, K Miyamoto

文献索引：Aoki, Katsuyuki; Obata, Tatsuhiro; Yamazaki, Yosuke; Mori, Yoshikazu; Hirokawa, Hiroko; Koseki, Jun-Ichi; Hattori, Tomohisa; Niitsu, Kazuaki; Takeda, Shuichi; Aburada, Masaki; Miyamoto, Ken-Ichi Chemical and Pharmaceutical Bulletin, 2007 , vol. 55, # 2 p. 255 - 267

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被引用次数: 14

摘要

We found previously that 7-[3-(cyclohexylmethyl) ureido]-3-{1-methyl-1H-pyrrolo [2, 3-b] pyridin-3-yl} quinoxalin-2 (1H)-one (7d-6) has considerable potency as a PDGF inhibitor. This compound showed potent inhibitory activity in a PDGF-induced CPA (Cell Proliferation Assay) and APA (Auto-Phosphorylation Assay)(IC 50= 0.05 μmol/l in CPA, 0.03 μmol/l in APA). Therefore, we tried to develop a novel and effective PDGF-βR inhibitor by ...