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Oxo-heterocyclic fused naphthalimides as antitumor agents: synthesis and biological evaluation.

Abstract：

:Three series of novel oxo-heterocyclic fused naphthalimide derivatives (8a-8f, 13a-13d, 17a-17d) were prepared. The newly-synthesized compounds, and their thio-heterocyclic fused analogs (1a-1c, 2a-2d, 3a-3c) exhibited potent antiproliferative activity correlated well with their structure. Further research demonstrated that all the representative compounds 13a, 2a and 17a, 3a showed strong inhibition activity to topo II similarly with amonafide, and also potent topo I inhibition activity, which was seldom reported before for naphthalimide derivatives. Preliminary exploration proved their DNA sequence preference. In all, dual topo I/topo II inhibition and DNA sequence preference might contribute to enhancing tumor selectivity and overcoming drug resistance.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Tan S,Yin H,Chen Z,Qian X,Xu Y

doi

10.1016/j.ejmech.2012.12.039

subject

Has Abstract

pub_date

2013-04-01 00:00:00

pages

130-8

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(12)00761-1

journal_volume

62

pub_type

杂志文章

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