Batran Rasha Z, Ahmed Eman Y, Awad Hanem M, Ali Korany A, Abdel Latif Nehad A
Chemistry of Natural Compounds Department, Pharmaceutical and Drug Industries Research Institute, National Research Centre Dokki Cairo 12622 Egypt
Tanning Materials and Leather Technology Department, National Research Centre Dokki Cairo 12622 Egypt.
RSC Adv. 2023 Oct 4;13(42):29070-29085. doi: 10.1039/d3ra03483f.
A series of thiazoline and thiazolidinone-based 4-hydroxycoumarin derivatives were synthesized using both conventional synthesis procedures and microwave-assisted techniques. The new compounds were evaluated for their cytotoxic effect against three human cancer cell lines; MCF-7, HCT-116 and HepG2 and one normal human cell line (BJ-1). The promising anti-proliferative compounds 2a, 2b, 6a and 6b were assessed for inhibiting EGFR and PI3K/mTOR. Compound 6a showed the highest inhibition activity towards the signaling pathway. The apoptotic effect and cell cycle arrest potential of derivative 6a were examined. Moreover, the molecular docking, physicochemical properties and pharmacokinetic parameters of the promising compound were investigated, as well.
使用传统合成方法和微波辅助技术合成了一系列基于噻唑啉和噻唑烷酮的4-羟基香豆素衍生物。评估了这些新化合物对三种人类癌细胞系（MCF-7、HCT-116和HepG2）和一种正常人类细胞系（BJ-1）的细胞毒性作用。对有前景的抗增殖化合物2a、2b、6a和6b进行了抑制表皮生长因子受体（EGFR）和磷脂酰肌醇-3-激酶/哺乳动物雷帕霉素靶蛋白（PI3K/mTOR）的评估。化合物6a对信号通路显示出最高的抑制活性。检测了衍生物6a的凋亡作用和细胞周期阻滞潜力。此外，还研究了该有前景化合物的分子对接、理化性质和药代动力学参数。
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