新一代紫杉烷类化合物IDN5109和IDN5390的甲氧基化类似物的合成及生物学评价
Synthesis and biological evaluation of methoxylated analogs of the newer generation taxoids IDN5109 and IDN5390.
作者信息
Barboni Luciano, Ballini Roberto, Giarlo Guido, Appendino Giovanni, Fontana Gabriele, Bombardelli Ezio
机构信息
Dipartimento di Scienze Chimiche, Università di Camerino, Via S. Agostino 1, 62032 Camerino (MC), Italy.
出版信息
Bioorg Med Chem Lett. 2005 Dec 1;15(23):5182-6. doi: 10.1016/j.bmcl.2005.08.066. Epub 2005 Sep 23.
Starting from 10-deacetylbaccatin III (7), the 2-debenzoyl-2-m-methoxybenzoyl analogs of the newer generation taxoids IDN5109 (3) and IDN5390 (4) were synthesized. The biological evaluation of these compounds (5 and 6, respectively) showed a general increase of cytotoxicity, as observed in first-generation anticancer taxanes.
从10-脱乙酰浆果赤霉素III（7）开始，合成了新一代紫杉烷类化合物IDN5109（3）和IDN5390（4）的2-脱苯甲酰基-2-间甲氧基苯甲酰基类似物。对这些化合物（分别为5和6）的生物学评价表明，与第一代抗癌紫杉烷类药物一样，其细胞毒性普遍增加。
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