Trans- and cis-2-phenylindole platinum(II) complexes as cytotoxic agents against human breast adenocarcinoma cell lines

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• 作者：Maria Tom¨¦ ; Concepci¨®n L¨®pez ; Asensio Gonz¨¢lez ; Bahadir Ozay ; Josefina Quirante ; Merc¨¨ Font-Bard¨ªa ; Teresa Calvet ; Carme Calvis ; Ramon Messeguer ; Laura Baldom¨¢ ; Josefa Bad¨ªa
• 关键词：Platinum(II) complexes ; 2-Phenylindole ; Cis- and trans-complexes ; Cytotoxicity ; Cancer
• 刊名：Journal of Molecular Structure
• 出版年：2013
• 出版时间：24 September, 2013
• 年：2013
• 卷：1048
• 期：Complete
• 页码：88-97
• 全文大小：1533 K

文摘

The synthesis and characterization of the new 2-phenylindole derivative: C₈H₃N-2-C₆H₅-3NOMe-5OMe (3c) and the trans- and cis-isomers of [Pt(3c)Cl₂(DMSO)] complexes (4c and 5c, respectively) are described. The crystal structures of 4c¡¤CH₂Cl₂ and 5c confirm: (a) the existence of a Pt-N_indole bond, (b) the relative arrangement of the Cl^? ligands [trans- (in 4c) or cis- (in 5c)] and (c) the anti-(E) configuration of the oxime. The cytotoxic assessment of C₈H₃N-2-(C₆H₄-4¡äR¹)-3NOMe-5R² [with R¹ = R² = H (3a); R¹ = Cl, R² = H (3b) and R¹ = H, R² = OMe (3c)] and the geometrical isomers of [Pt(L)Cl₂(DMSO)] with L = 3a-3c [trans- (4a-4c) and cis- (5a-5c), respectively] against human breast adenocarcinoma cell lines (MDA-MB231 and MCF-7) is also reported and reveals that all the platinum(II) complexes (except 4a) are more cytotoxic than cisplatin in front of the MCF7 cell line. Electrophoretic DNA migration studies of the synthesized compounds in the absence and in the presence of topoisomerase-I have been performed, in order to get further insights into their mechanism of action.