El-Sayed Amira A, Elsayed Elsayed A, Amr Abd El-Galil E
Laboratory of Synthetic Organic Chemistry, Chemistry Department, Faculty of Science, Ain Shams University, Abbassia, Cairo 11566, Egypt.
Bioproducts Research Department, Zoology Department, Faculty of Science, King Saud University, Riyadh 11451, Saudi Arabia.
ACS Omega. 2021 Mar 2;6(10):7147-7156. doi: 10.1021/acsomega.1c00202. eCollection 2021 Mar 16.
Herein, we used nicotinonitrile derivatives , as scaffolds to build novel and active antineoplastic agents. The reaction of nicotinonitrile derivatives , with POCl/PCl and/or hydrazine hydrate afforded 2-chloropyridones , and 2-hydrazinyl nicotinonitrile derivatives ,, respectively, as building blocks for various heterocyclic compounds. The structures of all of the synthesized heterocycles were elucidated from their spectral and elemental analyses. The cytotoxic activities of the prepared derivatives were evaluated against different cancer cell lines. Results revealed potential cytotoxic effects of the synthesized compounds against evaluated cell lines, where NCIH 460 and RKOP 27 cell lines were the most affected by the prepared compounds. Derivative was the most effective against all tested cell lines in terms of the obtained IC values (25 ± 2.6, 16 ± 2, 127 ± 25, 422 ± 26, and 255 ± 2 nM against NCIH 460, RKOP 27, HeLa, U937, and SKMEL 28 cells, respectively).
在此,我们使用烟腈衍生物作为构建新型活性抗肿瘤药物的骨架。烟腈衍生物与POCl₃/PCl₅和/或水合肼反应,分别得到2 - 氯吡啶酮和2 - 肼基烟腈衍生物,作为各种杂环化合物的构建单元。所有合成杂环的结构均通过光谱和元素分析得以阐明。对所制备衍生物的细胞毒性活性针对不同癌细胞系进行了评估。结果显示合成化合物对所评估的细胞系具有潜在的细胞毒性作用,其中NCIH 460和RKOP 27细胞系受所制备化合物的影响最大。就所获得的IC值而言,衍生物对所有测试细胞系最为有效(分别对NCIH 460、RKOP 27、HeLa、U937和SKMEL 28细胞的IC值为25 ± 2.6、16 ± 2、127 ± 25、422 ± 26和255 ± 2 nM)。