Sharath Kumar Kothanahally S, Hanumappa Ananda, Vetrivel Maruthai, Hegde Mahesh, Girish Yarabhally R, Byregowda Thinnali R, Rao Suguna, Raghavan Sathees C, Rangappa Kanchugarakoppal S
Department of Studies in Chemistry, Manasagangotri, University of Mysore, Mysuru 570006, India.
Department of Veterinary Pathology, Veterinary College, Hebbal, Bengaluru 560024, India.
Bioorg Med Chem Lett. 2015 Sep 1;25(17):3616-20. doi: 10.1016/j.bmcl.2015.06.069. Epub 2015 Jun 27.
4-Thiazolidinone derivatives were synthesized using T3P®-DMSO media as a cyclodehydrating agent. All the molecules were tested for their cytotoxicity against leukemic cell lines. The compound 3-(4-bromophenyl)-2-(4-(dimethylamino)phenyl)thiazolidin-4-one (4e) with electron donating substituent at para position of phenyl ring displayed considerable cytotoxicity against Reh and Nalm6 cells with an IC50 value of 11.9 and 13.5 μM, respectively. Furthermore, the compound 4e tested for tumor regression studies induced by EAC in Swiss albino mouse. Both in vitro and in vivo results suggested significant antiproliferative activity of compound 4e in Reh cells and mouse tumor tissue treated with compound 4e showed multifocal areas of necrosis and numerous number of apoptotic cells.
使用T3P®-二甲基亚砜介质作为环脱水剂合成了4-噻唑烷酮衍生物。对所有分子进行了针对白血病细胞系的细胞毒性测试。在苯环对位带有供电子取代基的化合物3-(4-溴苯基)-2-(4-(二甲基氨基)苯基)噻唑烷-4-酮(4e)对Reh和Nalm6细胞显示出相当大的细胞毒性,IC50值分别为11.9和13.5μM。此外,对化合物4e进行了瑞士白化小鼠中由艾氏腹水癌(EAC)诱导的肿瘤消退研究测试。体外和体内结果均表明化合物4e在Reh细胞中具有显著的抗增殖活性,用化合物4e处理的小鼠肿瘤组织显示出多灶性坏死区域和大量凋亡细胞。