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新型法尼基转移酶抑制剂1-苄基-5-(3-联苯-2-基丙基)-1H-咪唑的合成与生物学评价

Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitor.

作者信息

Lin Nan-Horng, Wang Le, Wang Xilu, Wang Gary T, Cohen Jerry, Gu Wen-Zhen, Zhang Haiying, Rosenberg Saul H, Sham Hing L

机构信息

Cancer Research, R-47B, Global Pharmaceutical Products Division, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064-3500, USA.

出版信息

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5057-62. doi: 10.1016/j.bmcl.2004.07.083.

DOI:10.1016/j.bmcl.2004.07.083
PMID:15380198
Abstract

Farnesyltransferase inhibitors (FTIs) have emerged as a novel class of anti-cancer agents. Analogs of the potent FTI, 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole, were synthesized and tested in vitro for their inhibitory activities. The most promising compound identified from this series is analog 29 that possesses potent enzymatic and cellular activities.

摘要

法尼基转移酶抑制剂（FTIs）已成为一类新型抗癌药物。合成了强效FTI 1-苄基-5-（3-联苯-2-基丙基）-1H-咪唑的类似物，并在体外测试了它们的抑制活性。从该系列中鉴定出的最有前景的化合物是具有强效酶活性和细胞活性的类似物29。

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