Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Istanbul University, Istanbul, Turkey.
J Enzyme Inhib Med Chem. 2009 Aug;24(4):1015-23. doi: 10.1080/14756360802608021.
A series of new 2-aryl-4-thiazolidinones (3 and 4) was synthesized from 2-hydroxy-2,2-diphenyl-N'-[(substituted phenyl)methylene]acetohydrazides (2) and mercaptoacetic acid or 2-mercaptopropionic acid. The antimycobacterial activity of these compounds was determined and several leads with 95-99% inhibition at 6.25 microg/mL test concentration were identified. In addition, antitumor activities were measured against several tumor cell lines, and significant growth inhibition was observed for compound 4p. Taken together, 2-aryl-4-thiazolidinones were shown to be promising scaffolds for both antimycobacterial and tumor-targeting compounds.
一系列新的 2-芳基-4-噻唑烷酮（3 和 4）是由 2-羟基-2,2-二苯基-N'-[(取代苯基)亚甲基]乙二酰肼（2）和巯基乙酸或 2-巯基丙酸合成的。这些化合物的抗分枝杆菌活性被测定，发现了几个在 6.25μg/mL 测试浓度下具有 95-99%抑制率的先导化合物。此外，还针对几种肿瘤细胞系测定了抗肿瘤活性，化合物 4p 表现出显著的生长抑制作用。总之，2-芳基-4-噻唑烷酮被证明是具有抗分枝杆菌和肿瘤靶向作用的有前途的支架。
