抗肿瘤药物 269. 非芳环-A 丹参新酮类似物 TNO，作为一类新型强效抗肿瘤药物。
Antitumor agents 269. Non-aromatic ring-A neotanshinlactone analog, TNO, as a new class of potent antitumor agents.
机构信息
Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA.
出版信息
Bioorg Med Chem Lett. 2009 Nov 15;19(22):6289-92. doi: 10.1016/j.bmcl.2009.09.092. Epub 2009 Sep 29.
Abstract
Tetrahydroneotanshinlactone (TNT) and tetrahydronaphthalene-1-ol (TNO) derivatives were designed, synthesized, and evaluated for cytotoxic activity. The TNO derivatives were found to be a promising novel class of in vitro antitumor agents. The cyclohexene ring-A could dramatically affect the antitumor activity and selectivity. Compound 20 showed the highest potency with ED(50) values of 0.7 and 1.7 microM against SK-BR-3 and ZR-75-1 breast cancer cell lines, respectively.
摘要
四氢丹参酮（TNT）和四氢萘-1-醇（TNO）衍生物被设计、合成并评估了其细胞毒性活性。TNO 衍生物被发现是一类很有前途的新型体外抗肿瘤剂。环己烯环-A 可以显著影响抗肿瘤活性和选择性。化合物 20 对 SK-BR-3 和 ZR-75-1 乳腺癌细胞系的 ED（50）值分别为 0.7 和 1.7μM，显示出最高的效力。
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