Hong W S, Kim H T, Kim K H, Kim D K
Department of Internal Medicine, Korea Cancer Center Hospital, Seoul.
Anticancer Res. 1995 Jan-Feb;15(1):51-4.
The in vitro antitumor activity of a new platinum complex, cis-malonato[(4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolan e] platinum(II) (SKI 2053R, NSC D644591), cisplatin (CDDP) and carboplatin (CBDCA) was determined against two human lung cancer (PC-9 and PC-14) and two human stomach cancer (MKN-45 and KATO III) cell lines by human tumor clonogenic assay. The activity of SKI 2053R was compared with those of CDDP and CBDCA in terms of relative antitumor activity (RAA, peak plasma concentration/IC50). Mean IC50 values (microgram/ml) of SKI 2053R, CDDP and CBDCA were 6.4 +/- 0.8, 1.8 +/- 0.7 and 20.6 +/- 12.2, respectively. The RAAs of SKI 2053R, CDDP and CBDCA were 1.6 +/- 0.4, 2.0 +/- 0.8 and 1.2 +/- 0.6, respectively. The differences in these values were not statistically significant. The results, demonstrating that antitumor activity of SKI 2053R is similar to those of CDDP and CBDCA, suggest that SKI 2053R is an interesting candidate for further development as a new anticancer drug.
通过人肿瘤克隆形成试验，测定了一种新型铂配合物顺式丙二酸根[（4R，5R）-4,5-双（氨甲基）-2-异丙基-1,3-二氧戊环]铂（II）（SKI 2053R，NSC D644591）、顺铂（CDDP）和卡铂（CBDCA）对两种人肺癌（PC-9和PC-14）细胞系以及两种人胃癌（MKN-45和KATO III）细胞系的体外抗肿瘤活性。根据相对抗肿瘤活性（RAA，血浆峰值浓度/IC50），将SKI 2053R的活性与CDDP和CBDCA的活性进行了比较。SKI 2053R、CDDP和CBDCA的平均IC50值（微克/毫升）分别为6.4±0.8、1.8±0.7和20.6±12.2。SKI 2053R、CDDP和CBDCA的RAA分别为1.6±0.4、2.0±0.8和1.2±0.6。这些值的差异无统计学意义。结果表明SKI 2053R的抗肿瘤活性与CDDP和CBDCA相似，提示SKI 2053R作为一种新型抗癌药物具有进一步开发的潜力。
