title: In vitro biological evaluation of platinum(II) complexes with 1-(methoxy substituted benzyl) azetidine-3,3-dicarboxylato ligands.
abstract: A number of platinum(II) complexes with ammine or 1R,2R-diaminocyclohexane as carrier ligands and 1-(methoxy-substituted benzyl) azetidine-3,3-dicarboxylate as leaving groups were synthesized and spectrally characterized. Biological evaluation in vitro showed that some of compounds showed positive antitumor activity. In particular, complex 3a, (1R,2R-diaminocyclohexane)[1-(3-methoxylbenzyl) azetidine-3,3-dicarboxylato)-O,O'] platinum(II), possessed a potent antitumor effect comparable to cisplatin and/or oxaliplatin, and very low toxicity in vivo. Preliminary antitumor mechanism of 3a has been investigated by cell apoptosis assays compared with cisplatin and oxaliplatin.
authors.affiliation: Pharmaceutical Research Center, School of Chemistry & Chemical Engineering, Southeast University, Nanjing 211189, China.
authors.forename: Runting
authors.initials: R
authors.lastname: Yin
authors.forename: Shaohua
authors.initials: S
authors.lastname: Gou
authors.forename: Yanyan
authors.initials: Y
authors.lastname: Sun
authors.forename: Xia
authors.initials: X
authors.lastname: Liu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001384:Azetidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002945:Cisplatin / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008024:Ligands; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D009944:Organoplatinum Compounds / Q000737:chemistry / Q000494:pharmacology; D000077150:Oxaliplatin; D010984:Platinum / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001384:Azetidines; D002264:Carboxylic Acids; D008024:Ligands; D009942:Organometallic Compounds; D009944:Organoplatinum Compounds; D000077150:Oxaliplatin; D010984:Platinum; D002945:Cisplatin