title: Structure-activity relationship and apoptosis induction in A549 cells by the potential anticancer compound cis-bis(3-aminoflavone)dichloroplatinum(II).
abstract: cis-DDP (cis-diamminedichloroplatinum(II), CAS 15663-27-1) is widely used in chemotherapy of many types of cancer. However, besides effectiveness, it gives many side effects which limit its clinical application. Therefore, nowadays studies are focused on searching for novel analogs of cis-DDP, at least equally effective in chemotherapy but less toxic. One of them might be cis-BAFDP (cis-bis(3-aminoflavone)dichloroplatinum(II)) with one of the hydrogen atoms of the amino group of cis-DDP replaced by a flavone ring. 3-Aminoflavone (AF) which posseses the desired NH2 group has been used as non-leaving ligand. The complex has been obtained in the reaction of AF and K2PtCl4. There are no data concerning evaluation of structural studies of cis-BAFDP, the beneficial anticancer properties of which were proved in vitro and in vivo. Therefore it was worthwhile to undertake a confirmation of the chemical structure of this compound by applying various spectroscopic techniques especially because of its potential pharmacological application. With this aim in mind this compound was characterized by: IR, 1H NMR, 195Pt NMR, UV absorption and fluorescence spectroscopy. Moreover, stronger apoptosis induction by cis-BAFDP than cis-DDP in the human nonsmall cancer cell line A549 was observed using Hoechst 33258/propidium iodide double staining.
authors.affiliation: Department of Cytogenetics and Plant Molecular Biology, University of Lodz, Lodz, Poland. beatakosmider@interia.pl
authors.forename: Beata
authors.initials: B
authors.lastname: Kosmider
authors.forename: Sunny A
authors.initials: SA
authors.lastname: Anuels
authors.forename: Dolf
authors.initials: D
authors.lastname: Evenberg
authors.forename: Elzbieta
authors.initials: E
authors.lastname: Zyner
authors.forename: Karim
authors.initials: K
authors.lastname: Bahmed
authors.forename: Regina
authors.initials: R
authors.lastname: Osiecka
authors.forename: Justyn
authors.initials: J
authors.lastname: Ochocki
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D006690:Bisbenzimidazole; D045744:Cell Line, Tumor; D004396:Coloring Agents; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D009336:Necrosis; D009944:Organoplatinum Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D013050:Spectrometry, Fluorescence; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D004396:Coloring Agents; D009944:Organoplatinum Compounds; C488623:cis-bis(3-aminoflavone)dichloroplatinum(II); D006690:Bisbenzimidazole