Dual-functional abeo-taxane derivatives destabilizing microtubule equilibrium and inhibiting NF-?B activation.
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ABSTRACT:
SUBMITTER: Zhao Y
PROVIDER: S-EPMC3755589 | biostudies-literature | 2013 Jun
REPOSITORIES: biostudies-literature
Publications
Dual-functional abeo-taxane derivatives destabilizing microtubule equilibrium and inhibiting NF-κB activation.
Zhao Yu Y Su Jia J Goto Masuo M Morris-Natschke Susan L SL Li Yan Y Zhao Qin-Shi QS Yao Zhu-Jun ZJ Lee Kuo-Hsiung KH
Journal of medicinal chemistry 20130531 11
Taxchinin A, with a 11(15→1)-abeo-taxane skeleton, is a major, but inactive taxoid contained in leaves of Taxus chinensis . In our design of dual-functional antitumor abeo-taxane derivatives, two fragments from antitumor agents with different molecular targets (the N-acyl-3'-phenylisoserine side chain from the antimitotic agent paclitaxel and an α,β-unsaturated carbonyl system from NF-κB inhibitors) were incorporated into the scaffold of taxchinin A. The resulting compounds displayed broad inhib ...[more]
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