On the synthesis, cytostatic and antitumor properties of new Pt(II) and Pt(IV) complexes with chloroanilines.
The paper reports the synthesis, the chemical characterization and the IR data of new Pt(II) and Pt(IV) complexes, as well as their cytostatic activities on KB cells and antitumour properties against three tumour systems (P388 and L1210 leukemias and advanced B16 melanoma). The following ligands were used: 2,5-dichloroaniline, 3,4-dichloroaniline, 2,4,6-trichloroaniline, 3,4,5-trichloroaniline, 2,3,4,5-tetrachloroaniline and 2,3,5,6-tetrachloroaniline. The tri- and tetrachloroaniline-Pt(II) complexes displayed a fairly good antileukemic activity but lower than cisplatin. The effect of these compounds against advanced B16 melanoma appears more interesting. They show an activity comparable or in some cases higher than cisplatin and other 1,2-diaminocyclohexane-Pt(II) complexes. The M.O. Huckel's calculations were performed on the ligand molecules in order to help us to draw a structure-activity relationship for new compounds.
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D002455:Cell Division / Q000187:drug effects*; D055598:Chemical Phenomena; D002621:Chemistry; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007624:KB Cells; D007939:Leukemia L1210 / Q000188:drug therapy; D007941:Leukemia P388 / Q000188:drug therapy; D008545:Melanoma / Q000188:drug therapy; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy*; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use
D000970:Antineoplastic Agents; D009944:Organoplatinum Compounds