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Preparation and biological activity of 13-substituted retinoic acids.

Abstract：

:13-Demethyl or 13-substituted all-E- and 9Z-retinoic acids were synthesized using a palladium-catalyzed coupling reaction of enol triflates and tributylstannylolefins. Their biological activities were then measured. The 13-ethyl analogs exhibited approximately one-half of the antiproliferative and differentiation-inducing activity of ATRA in HL-60 cells. In contrast, in the 9Z-derivatives, all analogs, except for the 13-butyl derivatives, showed apoptosis-inducing activity.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Wada A,Fukunaga K,Ito M,Mizuguchi Y,Nakagawa K,Okano T

doi

10.1016/j.bmc.2004.04.047

subject

Has Abstract

pub_date

2004-07-15 00:00:00

pages

3931-42

issue

14

eissn

0968-0896

issn

1464-3391

pii

S0968089604003682

journal_volume

12

pub_type

杂志文章

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