Pérez J M, Fuertes M A, Alonso C, Navarro-Ranninger C
Departamento de Química Inorgánica, Facultad de Ciencias, Universidad Autónoma de Madrid, Spain.
Crit Rev Oncol Hematol. 2000 Aug;35(2):109-20. doi: 10.1016/s1040-8428(00)00053-6.
The discovery in the 1990s of several trans-Pt complexes with in vitro and in vivo activity against tumor cells sensitive and/or resistant to cisplatin has forced the re-evaluation of the structure-activity relationships for platinum antitumor drugs. Because the determinant factors of cytotoxic activity of trans-platinum complexes do not follow the same patterns as those found for cisplatin and its analogues, the differences in cellular and biochemical pharmacology between trans-platinum antitumor complexes and cisplatin might be systematically exploited to design novel trans-platinum complexes with a clinical profile complementary to that of cisplatin and related analogues. Therefore, there may exist a novel molecular rationale for new platinum antitumor drugs development in the twenty-first century.
20世纪90年代发现了几种反式铂配合物，它们在体外和体内对顺铂敏感和/或耐药的肿瘤细胞均具有活性，这迫使人们重新评估铂类抗肿瘤药物的构效关系。由于反式铂配合物细胞毒性活性的决定因素与顺铂及其类似物的情况不同，反式铂类抗肿瘤配合物与顺铂在细胞和生化药理学方面的差异可能会被系统地利用，以设计出临床特征与顺铂及相关类似物互补的新型反式铂配合物。因此，在21世纪开发新型铂类抗肿瘤药物可能存在一种新的分子理论依据。
