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Novel heterocyclic family of phenyl naphthothiazole carboxamides derived from naphthalimides: synthesis, antitumor evaluation, and DNA photocleavage.

Abstract：

:A new heterocyclic family of (2-(dimethylamino)ethyl)-2-substituted phenylnaphtho[2,1-d]thiazole-5-carboxamides modified from naphthalimides was designed, synthesized, and quantitatively evaluated as antitumor agents and photonucleases. All these compounds were found to be more cytotoxic against P388 than against A549. B(3) (m-NO(2)) was found to be the strongest inhibitor for P388 with IC(50) of 1.49 microM, while B(2) was the most cytotoxic compound against A549 with IC(50) of 12 microM. B(4) (p-CH(3)), the most efficient DNA photocleaver, showed detectable DNA cleavage at 0.5 microM and total cleavage from form I to 100% form II at 50 microM. The photocleaving mechanism was changed with the modification to be via superoxide anion and radical.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Li Z,Yang Q,Qian X

doi

10.1016/j.bmc.2005.02.045

subject

Has Abstract

pub_date

2005-05-02 00:00:00

pages

3149-55

issue

9

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(05)00160-4

journal_volume

13

pub_type

杂志文章

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