作为抗癌剂的13-氨基木香烃内酯衍生物的合成。
Synthesis of 13-amino costunolide derivatives as anticancer agents.
作者信息
Srivastava Sanjay K, Abraham Aji, Bhat Beena, Jaggi Manu, Singh Anu T, Sanna Vinod K, Singh Gurvinder, Agarwal Shiv K, Mukherjee Rama, Burman Anand C
机构信息
Divisions of Medicinal Chemistry, Dabur Research Foundation, 22, Site IV, Sahibabad, Ghaziabad, India.
出版信息
Bioorg Med Chem Lett. 2006 Aug 15;16(16):4195-9. doi: 10.1016/j.bmcl.2006.05.083. Epub 2006 Jun 12.
A number of costunolide derivatives (4a-p) have been synthesized and evaluated for their in vitro cytotoxicity against eight tumor and a non-tumor cell lines. Compound 4d showed around 2-fold better cytotoxicity against SW-620 (colon) cell line with improved safety index than costunolide (1). While compounds 4e, 4g, and 4p have shown around 2- to 3-fold better cytotoxicity against MIAPaCa2 (pancreas), K-562 (leukemia) and PA-1 (ovary) cell lines as well as better safety index in comparison to costunolide (1). Compound 4p also exhibited cytotoxicity against HBL100 (breast) cell line with 2-fold better safety index. Structure-activity relationship has been described.
已合成了多种木香内酯衍生物（4a - p），并评估了它们对八种肿瘤细胞系和一种非肿瘤细胞系的体外细胞毒性。化合物4d对SW - 620（结肠）细胞系的细胞毒性比木香内酯（1）高约2倍，且安全指数有所提高。而化合物4e、4g和4p对MIAPaCa2（胰腺）、K - 562（白血病）和PA - 1（卵巢）细胞系的细胞毒性比木香内酯（1）高约2至3倍，且安全指数更高。化合物4p对HBL100（乳腺）细胞系也表现出细胞毒性，安全指数高2倍。已描述了构效关系。
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