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11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents.

Abstract：

:Several 11-substituted benzo[i]phenanthridine derivatives were synthesized, and their TOP1-targeting activity and cytotoxicity were assessed. Comparative data indicate that TOP1-targeting was often the primary molecular target associated with their cytotoxicity. Several 11-aminoalkyl derivatives, 11-aminocarboxy derivatives as well as the 11-[(2-dimethylamino)ethyl]carboxamide of 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine were synthesized and did exhibit considerable cytotoxicity with IC(50) values ranging from 20 to 120 nM in the human lymphoblast tumor cell line RPMI8402.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Feng W,Satyanarayana M,Tsai YC,Liu AA,Liu LF,LaVoie EJ

doi

10.1016/j.bmc.2008.08.018

subject

Has Abstract

pub_date

2008-09-15 00:00:00

pages

8598-606

issue

18

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(08)00735-9

journal_volume

16

pub_type

杂志文章

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