Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa.
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2234-7. doi: 10.1016/j.bmcl.2010.02.017. Epub 2010 Feb 10.
The synthesis and biological evaluation of two novel series of natural-product-like hybrids based on the chalcone, thiolactone and isatin scaffolds is herein described. Results for a 36-member beta-amino alcohol triazole library showed that the thiolactone-chalcones, with IC(50)s ranging from 0.68 to 6.08 microM, were more active against W2 strain Plasmodium falciparum than the isatin-chalcones with IC(50)s of 14.9 microM or less. Also of interest is falcipain-2 inhibitory activity displayed by the latter, whereas the thiolactone-chalcones lacked enzyme inhibitory activity.
本文描述了基于查尔酮、硫内酯和靛基质骨架的两个新型天然产物样杂合化合物系列的合成和生物评价。对 36 个β-氨基醇三唑文库的研究结果表明，硫内酯-查尔酮的 IC50 值为 0.68 至 6.08 μM，比 IC50 值小于或等于 14.9 μM 的靛基质-查尔酮对 W2 株疟原虫更有效。同样值得关注的是，后者表现出对疟原虫蛋白酶 2 的抑制活性，而硫内酯-查尔酮则缺乏酶抑制活性。
