Mukherjee Rama, Jaggi Manu, Siddiqui Mohammad J A, Srivastava Sanjay K, Rajendran Praveen, Vardhan Anand, Burman Anand C
Division of Experimental Oncology, Dabur Research Foundation, 22, Site IV, Sahibabad, Ghaziabad 201 010, UP, India.
Bioorg Med Chem Lett. 2004 Aug 2;14(15):4087-91. doi: 10.1016/j.bmcl.2004.05.034.
A series of 3-O-acyl, 3-hydrazine, 2-bromo, and 20,29-dibromo betulinic acid derivatives (1-27) have been synthesized and screened for in vitro cytotoxic activity on human cancer cell lines MOLT-4, JurkatE6.1, CEM.CM3, BRISTOL8, U937, DU145, PA-1, A549, and L132. A number of compounds have shown ED(50)<1 microg/mL against the cancer cell lines tested and have shown better cytotoxicity than betulinic acid. Compounds 13, 19, 20, 23, and 27 were the best derivatives and were selected as lead molecules for further development. The structure-activity relationship has been described.
合成了一系列3 - O - 酰基、3 - 肼基、2 - 溴以及20,29 - 二溴桦木酸衍生物（1 - 27），并对其在人癌细胞系MOLT - 4、JurkatE6.1、CEM.CM3、BRISTOL8、U937、DU145、PA - 1、A549和L132上的体外细胞毒性活性进行了筛选。许多化合物对所测试的癌细胞系显示出ED(50)<1μg/mL，并且表现出比桦木酸更好的细胞毒性。化合物13、19、20、23和27是最佳衍生物，被选为进一步开发的先导分子。已描述了构效关系。
