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New highly active taxoids from 9beta-dihydrobaccatin-9,10-acetals. Part 4.

Abstract：

:It was shown that a new taxane analogue 3, which exhibited both in vitro antitumor activity and in vivo efficacy by both i.v. and p.o. administration, was prone to be metabolized by human liver microsomes. We identified a major metabolite, M-1, generated by human liver microsomes as 20a, a hydroxylated compound at the pyridine ring of 3. To improve the metabolic stability of 3, we designed and synthesized new taxane analogues based on the structure of M-1, and obtained some compounds that maintained excellent antitumor activity and were scarcely metabolized by human liver microsomes.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Takeda Y,Uoto K,Chiba J,Horiuchi T,Iwahana M,Atsumi R,Ono C,Terasawa H,Soga T

doi

10.1016/s0968-0896(03)00454-1

subject

Has Abstract

pub_date

2003-10-01 00:00:00

pages

4431-47

issue

20

eissn

0968-0896

issn

1464-3391

pii

S0968089603004541

journal_volume

11

pub_type

杂志文章

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