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Synthesis and preliminary cytotoxicity study of glucuronide derivatives of CC-1065 analogues.

Abstract：

:Glucuronide derivatives of CBI-bearing CC-1065 analogues have been synthesized, and their cytotoxicities tested against U937 leukemia cells. The new compounds show potent antitumor activity in vitro. Compounds 1 and 2, and their corresponding glucuronides 3 and 4 have IC(50) values of 0.6, 0.1, 1.4 and 0.6 nM, respectively. Glucuronide 3 is approximately 2-fold less toxic than its hydroxyl counterpart 1, and glucuronide 4 is approximately 6-fold less toxic than its hydroxyl counterpart 2. Glucuronides 3 and 4 may have limited use in the ADEPT approach. However, they may be used as antitumor agents in a conventional way.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Wang Y,Yuan H,Wright SC,Wang H,Larrick JW

doi

10.1016/s0968-0896(02)00603-x

subject

Has Abstract

pub_date

2003-04-03 00:00:00

pages

1569-75

issue

7

eissn

0968-0896

issn

1464-3391

pii

S096808960200603X

journal_volume

11

pub_type

杂志文章

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