Design, synthesis and biological evaluation of paclitaxel-mimics possessing only the oxetane D-ring and side chain structures.

Abstract:

:Two spiro paclitaxel-mimics consisting only of an oxetane D-ring and a C-13 side chain were designed and synthesized on the basis of analysis of structure-activity relationships (SAR) of paclitaxel. In vitro microtubule-stabilizing and antiproliferative assays indicated a moderate weaker activity of the mimics than paclitaxel, but which still represented the first example of simplified paclitaxel analogues with significant anti-tumor biological activity.

journal_name

Fitoterapia

journal_title

Fitoterapia

authors

Chen XX,Gao F,Wang Q,Huang X,Wang D

doi

10.1016/j.fitote.2013.10.015

subject

Has Abstract

pub_date

2014-01-01 00:00:00

pages

111-5

eissn

0367-326X

issn

1873-6971

pii

S0367-326X(13)00292-X

journal_volume

92

pub_type

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