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 Chemjournal_title
European journal of medicinal chemistryauthors
Tan S,Yin H,Chen Z,Qian X,Xu Ydoi
10.1016/j.ejmech.2012.12.039subject
Has Abstractpub_date
2013-04-01 00:00:00pages
130-8eissn
0223-5234issn
1768-3254pii
S0223-5234(12)00761-1journal_volume
62pub_type
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journal_title:European journal of medicinal chemistry
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pub_type: 杂志文章
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journal_title:European journal of medicinal chemistry
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