León Leticia G, Donadel Osvaldo J, Tonn Carlos E, Padrón José M
Instituto Universitario de Bio-Orgánica Antonio González, Universidad de La Laguna, C/Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain.
Bioorg Med Chem. 2009 Sep 1;17(17):6251-6. doi: 10.1016/j.bmc.2009.07.053. Epub 2009 Jul 25.
A series of analogs were synthesized in a straightforward manner from naturally available sesquiterpenes ilicic acid and tessaric acid. The in vitro antiproliferative activities were examined in the human solid tumor cell lines A2780, HBL-100, HeLa, SW1573, T-47D and WiDr. The most potent analog induced considerably growth inhibition in the range 1.9-4.5 microM. Cell cycle studies for tessaric acid derivatives indicated a prominent arrest of the cell cycle at the G(2)/M phase. Damage to the cells was permanent as determine by the so called 24+24 drug schedule.
以天然可得的倍半萜类化合物ilicic酸和tessaric酸为原料,通过简单的方法合成了一系列类似物。在人实体瘤细胞系A2780、HBL - 100、HeLa、SW1573、T - 47D和WiDr中检测了它们的体外抗增殖活性。最有效的类似物在1.9 - 4.5微摩尔范围内诱导了显著的生长抑制。对tessaric酸衍生物的细胞周期研究表明,细胞周期在G(2)/M期有明显阻滞。通过所谓的24 + 24药物方案确定,对细胞的损伤是永久性的。