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 |
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Authors: | Jarak Ivana Kralj Marijeta Piantanida Ivo Suman Lidija Zinić Mladen Pavelić Kresimir Karminski-Zamola Grace |
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Institution: | 1. Nanobiotix, France;2. UMR-S 1193 Inserm/University Paris Sud, Centre Hépato-Biliaire, Hôpital Paul Brousse, Villejuif, France |
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Abstract: | A series of cyano- and amidino-substituted derivatives of thieno2,3-b]- and thieno3,2-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. |
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