抗肿瘤药物 270. 新型取代的 6-苯基-4H-呋喃并[3,2-c]吡喃-4-酮衍生物，作为有效且高选择性的抗乳腺癌药物。
Antitumor agents 270. Novel substituted 6-phenyl-4H-furo[3,2-c]pyran-4-one derivatives as potent and highly selective anti-breast cancer agents.
机构信息
Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599-7568, United States.
出版信息
Bioorg Med Chem. 2010 Jan 15;18(2):803-8. doi: 10.1016/j.bmc.2009.11.049. Epub 2009 Dec 2.
Abstract
6-Phenyl-4H-furo[3,2-c]pyran-4-one derivatives based on neo-tashinlactone (1) were synthesized and evaluated as novel anti-breast cancer agents. Compounds 10-13, 23, 25, and 27 showed potent inhibition against the SK-BR-3 breast cancer cell line. Importantly, 25 and 27 showed the highest cancer cell line selectivity, being approximately 100-250-fold more potent against SK-BR-3 (ED(50) 0.28 and 0.44microM, respectively) compared with other cancer cell lines tested. In addition, 25 displayed low cytotoxicity against normal breast cell lines 184A1 and MCF10A. Compounds 25 and 27 merit further investigation in our continuing program to generate and develop selective anti-breast cancer agents.
摘要
基于 neo-tashinlactone（1）的 6-苯基-4H-呋喃并[3,2-c]吡喃-4-酮衍生物被合成并评估为新型抗乳腺癌药物。化合物 10-13、23、25 和 27 对 SK-BR-3 乳腺癌细胞系表现出强烈的抑制作用。重要的是，25 和 27 对 SK-BR-3 的细胞系选择性最高，与测试的其他癌细胞系相比，其效力分别约高出 100-250 倍（ED（50）分别为 0.28 和 0.44μM）。此外，25 对正常乳腺细胞系 184A1 和 MCF10A 的细胞毒性较低。化合物 25 和 27 在我们继续开发和生成选择性抗乳腺癌药物的项目中值得进一步研究。
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