α-硫辛酸衍生物的合成及抗癌活性评价。
Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
机构信息
College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310032, PR China.
出版信息
Bioorg Med Chem Lett. 2010 May 15;20(10):3078-83. doi: 10.1016/j.bmcl.2010.03.112. Epub 2010 Apr 3.
alpha-Lipoic acid derivatives were synthesized and evaluated for their in vitro anticancer activities against NCI-460, HO-8910, KB, BEL-7402, and PC-3 cell lines. The results, for most compounds exhibited dose-dependent inhibitory property and several compounds had good inhibitions at the dose of 100 microg/mL. Compound 17 m was further selected for in vivo evaluation against S180 xenograft in ICR mice, which had 24.7% tumor-weight inhibition through intragastric administration of 200mg/kg of body weight. Moreover, the LD(50) in mice for 17 m through ig exceeded 1000 mg/kg of body weight.
α-硫辛酸衍生物被合成并评估其对 NCI-460、HO-8910、KB、BEL-7402 和 PC-3 细胞系的体外抗癌活性。结果表明，大多数化合物表现出剂量依赖性抑制特性，一些化合物在 100μg/mL 的剂量下具有良好的抑制作用。化合物 17m 进一步被选择用于 S180 荷瘤 ICR 小鼠的体内评价，通过灌胃给予 200mg/kg 体重，其肿瘤重量抑制率为 24.7%。此外，17m 在小鼠中的 LD(50)通过 ig 给药超过 1000mg/kg 体重。
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