Department of Chemistry and Biochemistry, University of Texas-Arlington, Arlington, TX 76019-0065, USA.
Department of Chemistry and Biochemistry, University of Texas-Arlington, Arlington, TX 76019-0065, USA; Department of Pesticide Chemistry, National Research Centre, Dokki, Giza 12622, Egypt.
Bioorg Med Chem. 2019 Oct 15;27(20):115047. doi: 10.1016/j.bmc.2019.115047. Epub 2019 Aug 14.
A series of N-substituted (Z)-2-imino-(5Z)-ylidene thiazolidines/thiazolidin-4-ones were synthesized and their antiproliferative activities against colon (HCT-116) and breast (MCF7) cancer cell lines were evaluated utilizing an MTT growth assay. A 2D-QSAR investigation was conducted to probe and validate the obtained antiproliferative properties for the thiazolidine derivatives. The majority of the thiazolidines exhibit higher potency against a colon cancer cell line relative to the standard reference. The p-halophenylimino p-anisylidene derivatives exhibited the highest anti-proliferative activity against HCT116 relative to control (IC = 8.9-10.0 μM compared to 20.4 μM observed for 5-fluorouracil as positive control). An X-ray study confirmed the Z, Z'-configurations for two examples of the synthesized compounds.
合成了一系列 N-取代的（Z）-2-亚氨基-（5Z）-亚乙烯基噻唑烷/噻唑烷-4-酮，并通过 MTT 生长测定法评估了它们对结肠（HCT-116）和乳腺（MCF7）癌细胞系的抗增殖活性。进行了二维 QSAR 研究，以探究和验证噻唑烷衍生物的获得的增殖抑制特性。大多数噻唑烷类化合物对结肠癌细胞系的活性均高于标准参考物。对卤代苯基亚氨基对甲氧基苯亚甲基衍生物对 HCT116 的抗增殖活性最高，与阳性对照物 5-氟尿嘧啶（IC=8.9-10.0μM）相比，其抑制率为 20.4μM。X 射线研究证实了两种合成化合物的 Z，Z'-构型。
