当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis, photochemical synthesis, DNA binding and antitumor evaluation of novel cyano- and amidino-substituted derivatives of naphtho-furans, naphtho-thiophenes, thieno-benzofurans, benzo-dithiophenes and their acyclic precursors.

Synthesis, photochemical synthesis, DNA binding and antitumor evaluation of novel cyano- and amidino-substituted derivatives of naphtho-furans, naphtho-thiophenes, thieno-benzofurans, benzo-dithiophenes and their acyclic precursors.

Abstract：

:As a part of the research on the improvement of an alternative to conventional photodynamic therapy by light-induced formation of intercalators, we synthesized a series of novel heterocyclic compounds and their acyclic precursors. We now report details about their synthesis/characterization in respect to their potential of photoinduced cyclization, interactions with DNA and inhibition of the tumor cell growth in vitro. Among studied compounds only amidino-furyl-substituted phenyl acrylates were efficiently converted to the corresponding naphthofuranes, while their thiophene analogues, all non-charged derivatives and amidino-phenyl-substituted analogues didn't show acceptable photoconversion. The significantly stronger antiproliferative activity of cyclic analogues could be correlated to the property of these molecules to intercalate into DNA. The acyclic molecules did not show any interaction with DNA, correlating with the inferior biological activity, except for one cyano-bearing molecule.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Starcević K,Kralj M,Piantanida I,Suman L,Pavelić K,Karminski-Zamola G

doi

10.1016/j.ejmech.2006.03.012

subject

Has Abstract

pub_date

2006-08-01 00:00:00

pages

925-39

issue

8

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(06)00133-4

journal_volume

41

pub_type

杂志文章

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