Abstract

Objective: Synthesis, characterization of novel thiazole hydrazine derivatives and inhibitory action against the VEGFR-2. Methods: The novel synthesized derivatives were appraised for their ability to inhibit the growth of cancer cells in vitro utilizing 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay method. Results and Discussion: The synthesized derivatives divulge moderate to noteworthy in vitro anticancer activity towards the chosen cancer cell lines. Compounds (Va), (Vb), and (Ve) exhibited prominent anticancer activities with IC₅₀ values 10.24–15.44 µM. Conclusions: Amongst these, compound (Va), (Vb), and (Ve) showed the most potent inhibition when compared with other tested compounds. Thus, the reports obtained of the current studies divulge that the thiazole hydrazine derivatives can be developed as auspicious anticancer entities in future.

中文翻译：

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新型噻唑肼衍生物的合成、表征及其对 VEGFR-2 的抑制作用

摘要

目的：新型噻唑肼衍生物的合成、表征及其对 VEGFR-2 的抑制作用。方法：采用3-(4,5-二甲基噻唑-2-基)-2,5-二苯基溴化四唑(MTT)测定法评价新型合成衍生物体外抑制癌细胞生长的能力。结果和讨论：合成的衍生物对所选癌细胞系具有中等至显着的体外抗癌活性。化合物 ( Va )、( Vb ) 和 ( Ve ) 表现出显着的抗癌活性，IC ₅₀值为 10.24–15.44 µM。结论：其中，与其他测试化合物相比，化合物 ( Va )、( Vb ) 和 ( Ve ) 显示出最有效的抑制作用。因此，目前的研究报告表明，噻唑肼衍生物将来可以开发为有利的抗癌实体。