无机化学学报
無機化學學報
무궤화학학보
JOURNAL OF INORGANIC CHEMISTRY
2008年
6期
856-860
,共5页
佟太锋%刘霞%诸海滨%苟少华%张奕华
佟太鋒%劉霞%諸海濱%茍少華%張奕華
동태봉%류하%제해빈%구소화%장혁화
铂(Ⅱ)配合物%抗肿瘤活性%烷氧基酸根
鉑(Ⅱ)配閤物%抗腫瘤活性%烷氧基痠根
박(Ⅱ)배합물%항종류활성%완양기산근
Pt(Ⅱ) complexes%anti-tumor activity%alkoxycarboxylates
合成了5个以直链和带支链烷氧基乙酸为载体配基的顺铂类配合物,通过红外光谱、核磁共振氢谱和质谱对配合物进行了表征,并测试了化合物对肺腺癌SPC-A1和胃腺癌BGC823的体外抗肿瘤活性.生物活性测试结果表明,配合物的活性与离去基团有很大关系.配合物4(顺-二(异丙氧基乙酸根)·[(1R,2R)-1,2-反式环己二胺]合铂(Ⅱ))在2个细胞系中均显示最高的体外抗肿瘤活性,甚至超过顺铂.
閤成瞭5箇以直鏈和帶支鏈烷氧基乙痠為載體配基的順鉑類配閤物,通過紅外光譜、覈磁共振氫譜和質譜對配閤物進行瞭錶徵,併測試瞭化閤物對肺腺癌SPC-A1和胃腺癌BGC823的體外抗腫瘤活性.生物活性測試結果錶明,配閤物的活性與離去基糰有很大關繫.配閤物4(順-二(異丙氧基乙痠根)·[(1R,2R)-1,2-反式環己二胺]閤鉑(Ⅱ))在2箇細胞繫中均顯示最高的體外抗腫瘤活性,甚至超過順鉑.
합성료5개이직련화대지련완양기을산위재체배기적순박류배합물,통과홍외광보、핵자공진경보화질보대배합물진행료표정,병측시료화합물대폐선암SPC-A1화위선암BGC823적체외항종류활성.생물활성측시결과표명,배합물적활성여리거기단유흔대관계.배합물4(순-이(이병양기을산근)·[(1R,2R)-1,2-반식배기이알]합박(Ⅱ))재2개세포계중균현시최고적체외항종류활성,심지초과순박.
Five cisplatin-typed platinum complexes, characteristic of linear and branched alkoxycarboxylates as leaving groups, were synthesized and characterized by infrared, electro-spray ionization MS and 1H NMR spectroscopy. In vitro cytotoxicities of these complexes against SPC-A1 human lung adenocarcinoma and BGC823 human gastric adenocarcinoma cell lines were evaluated. Biological tests reveal that the cytotoxieities of these compounds are highly related to the nature of leaving groups. Complex 4, cis-(trans-1R, 2R-diaminocyclohexane) bis (2-isopropoxyacetate) platinum (Ⅱ), shows the highest cytotoxicity against both cell lines, and its cytotoxicity is higher than that of cisplatin.