Pharmaceutical Research Center, School of Chemistry & Chemical Engineering, Southeast University, Nanjing 211189, PR China.
J Inorg Biochem. 2012 Jul;112:68-76. doi: 10.1016/j.jinorgbio.2012.03.003. Epub 2012 Mar 17.
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.
设计、合成并表征了一系列以（1R,2R）-N（1）-烷基-1,2-二氨基环己烷衍生物为载体配体的铂（II）配合物，其中作为位阻基团的烷基分别为 1-丁基、2-甲基丙基或 2-丁基。这些铂配合物的体外生物评价表明，它们的抗肿瘤活性与烷基的形状密切相关。体内抗肿瘤研究表明，与顺铂和奥沙利铂相比，配合物 1c，(1R,2R)-N(1)-(2-丁基)-1,2-环己二胺-N,N'铂（II）具有较高的抗肿瘤活性和较低的毒性。初步研究了 1c 的抗肿瘤机制，其可能与顺铂和奥沙利铂不同。
