title: Antitumor platinum(II) complexes of N-monoalkyl-1R, 2R-diaminocyclohexane derivatives with alkyl groups as hindrance.
abstract: A number of platinum (II) complexes, characteristic of (1R,2R)-N(1)-alkyl-1,2-diaminocyclohexane derivatives as carrier ligands, were designed, synthesized and characterized, where the alkyl group serving as hindrance is a 1-butyl, 2-methylpropyl or 2-butyl moiety, respectively. In vitro biological evaluation of these platinum complexes revealed that their antitumor activity had a close relationship with the shape of alkyl groups. In vivo antitumor study indicated that complex 1c, [(1R,2R)-N(1)-(2-butyl)-1,2-cyclohexanediamine-N,N'] (oxalato-O,O')platinum (II), possessed rather high antitumor effect and low toxicity compared with cisplatin and oxaliplatin. Antitumor mechanism of 1c has been tentatively studied, which might be different from that of cisplatin and oxaliplatin.
authors.affiliation: Pharmaceutical Research Center, School of Chemistry & Chemical Engineering, Southeast University, Nanjing 211189, PR China.
authors.forename: Yanyan
authors.initials: Y
authors.lastname: Sun
authors.forename: Runting
authors.initials: R
authors.lastname: Yin
authors.forename: Shaohua
authors.initials: S
authors.lastname: Gou
authors.lastname: Zhaojian
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy; D049109:Cell Proliferation / Q000187:drug effects; D015179:Colorectal Neoplasms / Q000188:drug therapy; D003514:Cyclohexylamines / Q000737:chemistry*; D004249:DNA Damage / Q000187:drug effects; D005260:Female; D045325:HCT116 Cells; D056945:Hep G2 Cells; D006801:Humans; D008113:Liver Neoplasms / Q000188:drug therapy; D061986:MCF-7 Cells; D051379:Mice; D008807:Mice, Inbred BALB C; D009944:Organoplatinum Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D003514:Cyclohexylamines; D009944:Organoplatinum Compounds; C030435:1,2-cyclohexanediamine