engleski

Novel Cyano- and Amidino-Substituted Derivatives of Thieno[2, 3-b]- and Thieno[3, 2-b]thiophene-2-carboxanilides and Thieno[3’ , 2’ : 4, 5]thieno- and Thieno[2’ , 3’ : 4, 5]thieno [2, 3-c]quinolones: Synthesis, Photochemical Synthesis, DNA binding and Antitumor Evaluation.

A series of cyano- and amidino-substituted derivatives of thieno[2, 3-b]- and thieno[3, 2-b]thiophene-2-carboxanilides and their " cyclic" derivatives (quinolones) were synthesized. "Cyclic" compounds displayed a rather strong and differential antiproliferative effect on various cell lines, while the "acyclic" amidino-substituted compounds were much more active, but showing mostly non-differential cytotoxicity, whereas cyano-substituted compounds (2a, b) produced a strikingly strong effect selectively on HeLa and Hep-2 cell lines. Antiproliferative activity of "cyclic" derivatives is very likely caused by intercalation into DNA, while their "acyclic" analogues use other target(s) and/or mechanisms of action.

thieno[3; 2-b]thiophene-2-carboxanilides; quinolones; amidines; DNA binding; antitumor activity

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