Kidani Y, Suzuki K, Noji M, Tashiro T
Faculty of Pharmaceutical Sciences, Nagoya City University, Japan.
Biomed Pharmacother. 1989;43(4):261-4. doi: 10.1016/0753-3322(89)90005-x.
Various steroid-containing platinum (Pt) complexes of 1R,2R-cyclohexanediamine (= 1R,2R-dach) and cis-dl- and trans-dl-2-(aminomethyl)cyclohexylamine (= amcha) were synthesized and their antitumor activity was screened against leukemia L1210 according to the Pt Analog Study Protocol. Among the Pt complexes prepared, Pt 1R,2R-dach complexes of cortisone, hydrocortisone, methylprednisolone, testosterone, estriol and progesterone showed very high antitumor activity. Pt complexes of cis-dl- and trans-dl-amcha prednisolone, Pt(17-OH-progesterone) (trans-dl-amcha), Pt complexes of cis-dl- and trans-dl-amcha progesterone were found to be very effective.
合成了1R,2R-环己二胺（=1R,2R-dach）以及顺式-dl-和反式-dl-2-(氨甲基)环己胺（=amcha）的各种含甾体铂（Pt）配合物，并根据铂类似物研究方案针对白血病L1210筛选了它们的抗肿瘤活性。在所制备的铂配合物中，可的松、氢化可的松、甲泼尼龙、睾酮、雌三醇和孕酮的1R,2R-dach铂配合物表现出非常高的抗肿瘤活性。发现顺式-dl-和反式-dl-amcha泼尼松龙的铂配合物、Pt(17-羟基孕酮)(反式-dl-amcha)、顺式-dl-和反式-dl-amcha孕酮的铂配合物非常有效。
