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Synthesis and Biological Evaluation of Chalcone Derivatives of 1,2,4-Thiadiazol-Benzo[d]imidazol-2-yl)quinolin-2(1H)-one as Anticancer Agents
Chemical Data Collections Pub Date : 2020-12-01 , DOI: 10.1016/j.cdc.2020.100556
Yazala Jyothsna Pragathi , Deekala Veronica , Kowthalam Anitha , Mandava Venkata Basaveswara Rao , Rudraraju Ramesh Raju

Abstract A new series of chalcone incorporated 2-quinoline-benzimidazole-1,2,4-thiadiazoles (9a-j) were designed, synthesized and examined for their anticancer activities against four different human cancer cell lines like MCF-7 (breast cancer), A549 (Lung cancer), Colo-205 (Colon cancer) and A2780 (Ovarian cancer) and compared with clinical drug candidate as etoposide. Among them, compound 9d showed potent anticancer activities against MCF-7, A549, Colo-205 and A2780 cell lines with IC50 values of 0.012±0.007 µM, 0.074±0.004 µM, 1.46±0.73 µM and 0.083±0.002 µM, respectively.

中文翻译:

1,2,4-噻二唑-苯并[d]咪唑-2-基)喹啉-2(1H)-酮查耳酮衍生物作为抗癌剂的合成与生物学评价

摘要 设计、合成了一系列新的查尔酮结合 2-喹啉-苯并咪唑-1,2,4-噻二唑 (9a-j) 并检测了它们对四种不同的人类癌细胞系如 MCF-7(乳腺癌)的抗癌活性、A549(肺癌)、Colo-205(结肠癌)和A2780(卵巢癌)并与作为依托泊苷的临床候选药物进行比较。其中,化合物9d对MCF-7、A549、Colo-205和A2780细胞系显示出有效的抗癌活性,IC50值分别为0.012±0.007 µM、0.074±0.004 µM、1.46±0.73 µM和0.082±0。
更新日期:2020-12-01
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