Indian Institute of Chemical Biology (CSIR), Kolkata, India.
Bioorg Med Chem Lett. 2010 Dec 1;20(23):6947-50. doi: 10.1016/j.bmcl.2010.09.126. Epub 2010 Oct 23.
A series of analogues of andrographolide, prepared through chemo-selective functionalization at C14 hydroxy, have been evaluated for in vitro cytotoxicities against human leukemic cell lines. Two of the analogues (6a, 9b) exhibited significant potency. Preliminary studies on structure-activity relationship (SAR) revealed that the α-alkylidene-γ-butyrolactone moiety of andrographolide played a major role in the activity profile. The structures of the analogues were established through spectroscopic and analytical data.
通过 C14 位羟基地化反应合成了一系列穿心莲内酯类似物，并对其进行了体外抗人白血病细胞系细胞毒性评价。其中两个类似物（6a、9b）表现出显著的活性。对构效关系（SAR）的初步研究表明，穿心莲内酯的α-亚甲基-γ-丁内酯部分在活性谱中起主要作用。通过光谱和分析数据确定了类似物的结构。
