新型铂配合物的合成及其抗肿瘤活性

Synthesis and Antitumor Activities of Novel Platinum(Ⅱ) Complexes

以顺-二碘-二环戊胺合铂(Ⅱ)为起始原料,经聚合反应和胺化反应制得顺式-二碘-异丙胺-环戊胺合铂(Ⅱ)(2);2分别与氯化钾,1,1-环丁基二羧酸钾和一水合草酸钾反应,合成了3个新型的铂配合物:顺式-二氯-异丙胺-环戊胺合铂(Ⅱ)(1a,收率36.6%),顺式-1,1-环丁基二羧酸-异丙胺-环戊胺合铂(Ⅱ)(1b,收率43.6%)和顺式-草酸-异丙胺-环戊胺合铂(Ⅱ)(1c,收率28.1%),其结构经1H NMR,IR,ESI-MS和元素分析表征。采用MTT法测定了1a^1c对肝癌(SMMC-7721),肺癌(A-549),乳腺癌(MCF-7)和结肠癌(SW480)的体外抑制活性。结果表明,1a^1c对部分癌细胞的IC50值小于40μm,具有一定的体外肿瘤生长抑制活性。

Three novel platinum （Ⅱ） complexes,cis-dichloro-2-aminopropane （cyclopentylamine） platinum（Ⅱ） （1a,yield of 36.6%）,cis-cyclobutane-1,1-dicarboxylic-2-arninopropanedichloro（cyclopentylamine） platinum （Ⅱ） （1b,yield of 43.6%） and cis-oxalate-2-aminopropane （cyclopentylamine） platinum（Ⅱ） （1c,yield of 28.1%）,were synthesized by the reaction of cis-diiodide-2-aminopropane（cyclopentylamine） platinum（Ⅱ）（2） with potassium chloride,potassium cyclobutane-1,1-dicarboxylic and potassium oxalate monohydrate,respectively.2 was obtained by the polymerization reaction and aminization reaction from cis-diiodide （cyclopentylamine） platinum （Ⅱ）.The structures were characterized by 1 H NMR,IR,ESI-MS and elemental analysis.The in vitro anticancer activities of 1a ～ 1c against SMMC-7721,A-549,MCF-7 and SW480 were measured by MTT method.The resuits showed that 1a ～ 1c exhibited certain antitumor activities,IC50 〈 40 μm.