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Design,synthesis and biological evaluation of indole derivatives as novel inhibitors targeting B-Raf kinase
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作者 Zeng Wu Ming Yan +8 位作者 Shi-He Hu Zhi-Cheng Yu Yong Zhu Ya-Dong Cheng Hai-Chun Liu Yan-Min Zhang Si-Hui Yao Wei-Fang Tang Tao Lu 《Chinese Chemical Letters》 SCIE CAS CSCD 2014年第2期351-354,共4页
A series of novel indole derivatives were designed and synthesized and their inhibitory activity against B-Raf and HepG2 cell were also described. Among them, compounds 7a and 7b exhibited excellent potency, which sho... A series of novel indole derivatives were designed and synthesized and their inhibitory activity against B-Raf and HepG2 cell were also described. Among them, compounds 7a and 7b exhibited excellent potency, which showed the potential for further research as lead compounds. 展开更多
关键词 b-raf kinase inhibitors Receptor-based drug discovery Indole derivatives biological evaluation
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SB-590885的合成工艺研究
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作者 黄朋越 朱雄 +2 位作者 赵永利 柴慧芳 赵春深 《化学研究与应用》 CAS CSCD 北大核心 2020年第6期1094-1099,共6页
SB-590885是一种新型的三芳基咪唑类B-Raf激酶抑制剂,已报道的合成方法收率较低且操作繁琐,不适合工业化生产。本文设计了一条新的合成路线,以4-溴吡啶盐酸盐为起始原料,经偶联、脱保护、加成、氧化、环合、水解等反应得到目标化合物,... SB-590885是一种新型的三芳基咪唑类B-Raf激酶抑制剂,已报道的合成方法收率较低且操作繁琐,不适合工业化生产。本文设计了一条新的合成路线,以4-溴吡啶盐酸盐为起始原料,经偶联、脱保护、加成、氧化、环合、水解等反应得到目标化合物,产物结构经1H NMR,13C NMR和MS确证,总收率为9.53%,该方法原料便宜易得、反应条件温和、操作简单且总收率较高,是一条适合工业化生产的合成路线。 展开更多
关键词 4-溴吡啶盐酸盐 Sb-590885 b-raf激酶抑制剂 合成
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