Saxena Hari Om, Faridi Uzma, Kumar J K, Luqman Suaib, Darokar M P, Shanker Karuna, Chanotiya Chandan S, Gupta M M, Negi Arvind S
Central Institute of Medicinal and Aromatic Plants (CIMAP), P.O. CIMAP, Kukrail Picnic Spot Road, Lucknow, U.P., India.
Steroids. 2007 Nov;72(13):892-900. doi: 10.1016/j.steroids.2007.07.012. Epub 2007 Aug 6.
Chalcone derivatives on estradiol framework have been synthesized. Some of the derivatives showed potent anticancer activity against some human cancer cell lines. Compounds 9 and 19 showed potent activity against MCF-7, a hormone dependent breast cancer cell line. Chalcone 7 was further modified to the corresponding indanone derivative (19) using the Nazarov reaction, which showed better activity than the parent compound against the MCF-7 breast cancer cell line. Active anticancer derivatives were also evaluated for osmotic hemolysis using the erythrocyte as a model system. It was observed that chalcone derivatives showing cytotoxicity against cancer cell lines did not affect the fragility of erythrocytes and hence may be considered as non-toxic to normal cells.
已合成了基于雌二醇骨架的查尔酮衍生物。其中一些衍生物对某些人类癌细胞系显示出强大的抗癌活性。化合物9和19对MCF-7（一种激素依赖性乳腺癌细胞系）显示出强大活性。使用纳扎罗夫反应将查尔酮7进一步修饰为相应的茚满酮衍生物（19），该衍生物对MCF-7乳腺癌细胞系显示出比母体化合物更好的活性。还以红细胞为模型系统评估了活性抗癌衍生物的渗透性溶血情况。观察到对癌细胞系显示出细胞毒性的查尔酮衍生物不会影响红细胞的脆性，因此可被认为对正常细胞无毒。
