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Structural analogs of tylophora alkaloids may not be functional analogs.


ABSTRACT: 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-kappaB 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.

SUBMITTER: Gao W 

PROVIDER: S-EPMC2701548 | biostudies-literature | 2008 Jan

REPOSITORIES: biostudies-literature

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Structural analogs of tylophora alkaloids may not be functional analogs.

Gao Wenli W   Chen Annie Pei-Chun AP   Leung Chung-Hang CH   Gullen Elizabeth A EA   Fürstner Alois A   Shi Qian Q   Wei Linyi L   Lee Kuo-Hsiung KH   Cheng Yung-Chi YC  

Bioorganic & medicinal chemistry letters 20071121 2


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-kappaB signaling pathway, and their inhibitory effects against protein and nucleic acid synthesis are different. Be  ...[more]

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