Structural analogs of tylophora alkaloids may not be functional analogs

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:18

Article

Gao, Wenli¹  Chen, Annie Pei-Chun¹  Leung, Chung-Hang¹  Gullen, Elizabeth A.¹  Fuerstner, Alois²  Shi, Qian³  Wei, Linyi³  Lee, Kuo-Hslung³  Cheng, Yung-Chi¹ 

[1] Yale Univ, Sch Med, Dept Pharmacol, New Haven, CT 06510 USA

[2] Max Planck Inst Kohlenforsch, D-45470 Mulheim, Germany

[3] Univ N Carolina, Sch Pharm, Natl Prod Res Labs, Chapel Hill, NC 27599 USA

关键词: tylophora alkaloids;    structure-activity relationship;    protein;    DNA;    and RNA synthesis;   

DOI  :  10.1016/j.bmcl.2007.11.054

来源: Elsevier

【 摘 要 】

Phenanthroindolizidine-based tylophora alkaloids have been reported to have potential antitumor, anti-immuno and, anti-inflammatory activity. The structure-activity relationships of a series of tylophora alkaloids were studied to guide future drug design. Our results indicate that although these compounds are structural analogs, their potency of cytotoxicity, selectivity against NF-kappa B signaling pathway, and their inhibitory effects against protein and nucleic acid synthesis are different. Because they do not have an identical spectrum of targets, the studied compounds are structural, but may not be functional analogs. (c) 2007 Elsevier Ltd. All rights reserved.

【 授权许可】

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