(Pt(am)_n(Ac-Cl)_2)和(Pt(am)_n(CBDCA))配合物的合成、表征及抗肿瘤活性的研究

SYNTHESIS CHARACTERIZATION OF 〔Pt(am)_n(Ac-Cl)_2〕 AND 〔Pt(am)_n(CBDCA)〕 AND THEIR ANTITUMOR ACTIVITY

本文合成及表征了十种铂配合物〔Pt(am)n(Ac-Cl)_2〕和〔Pt(am)_n(CBDCA)〕(n=1,2;am=NH_3、乙二胺、异丙胺、1,2—环已二胺、1,3—环已二胺、1,2,2＇—三甲基—1,3—环戊二胺:CBDCA=1,1＇—环丁二酸根;Ac—Cl=氯乙酸根),其中八种为新配合物。研究了它们的电子结构,并测定了它们对小鼠S—180肉瘤的抑制作用。结果表明,配合物的电子结构和动物实验结果与以前得到的铂配合物的构效关系相一致。

Ten platinum compounds of〔Pt(am)_n(Ac-Cl)_2〕and〔Pt(am)_n(CBDCA)〕(n=1, 2; am=NH_3, en, isopropylamine, 1, 2-diaminocyclohexane, 1, 3-diaminocyclohexane, 1, 2, 2＇-trimethyl- l, 3-diaminocyclopentane; CBDCA=1,1＇-cyclobutanedicarboxylic acid; Ac-Cl=chloroacetic acid)were synthesized and characterized except fer two, all of thecompounds are new. The electronic structure of the compounds was studied by CNDO/2method, and the activity of the complexes against the S-180 Sarcoma was determined. The results are in the agreement with the quantitative relationship between the activity and structure of previous Pt complexes.