Morihira K, Nishimori T, Kusama H, Horiguchi Y, Kuwajima I, Tsuruo T
Department of Chemistry, Tokyo Institute of Technology, Japan.
Bioorg Med Chem Lett. 1998 Nov 3;8(21):2973-6. doi: 10.1016/S0960-894X(98)00539-3.
The C-aromatic taxoids were synthesized to develop effective inhibitors against drug efflux mediated by p-glycoproteins. Among those tested using multi-drug resistant tumor cells (2780AD), the benzoate 11 exhibited significant activity as potent as verapamil, a well-established MDR reversing agent.
合成C-芳族紫杉烷类化合物以开发针对P-糖蛋白介导的药物外排的有效抑制剂。在使用多药耐药肿瘤细胞(2780AD)进行测试的那些化合物中,苯甲酸酯11表现出与维拉帕米相当的显著活性,维拉帕米是一种成熟的多药耐药逆转剂。