彗星试验
分子生物学
细胞毒性T细胞
MTT法
化学
DNA损伤
DNA断裂
细胞培养
生物
癌症研究
DNA
细胞凋亡
生物化学
体外
遗传学
程序性细胞死亡
作者
Nada S. Ibrahim,Farid M. Sroor,Karima F. Mahrous,Jassmin A. Abd Elaleem,Ismail A. Abdelhamid
标识
DOI:10.1002/slct.202301754
摘要
Abstract A novel series of 2‐cyano‐ N ‐(tetrahydrobenzo[ b ]thiophen‐2‐yl)acrylamide derivatives were synthesized and their structures were confirmed using several spectral tools. All compounds were subjected to MTT assay to elucidate their cytotoxic effect against human hepatocellular carcinoma (HEPG2), human Caucasian breast adenocarcinoma (MCF7), human pancreatic cancer cell line (PACA2), human prostate cancer cell line (PC3), and normal skin fibroblast (BJ1). Among them, the acrylamide derivatives 5 , 10 and 14 exerted potent activities against MCF7 with IC 50 values of 61.2, 66.4, and 55.3 μg/ml respectively. A molecular docking was performed to study the possibility of the molecular binding of these three compounds with the active site of signal transducer and activator of transcription 1 protein (STAT1). Gene expression analysis demonstrated the significant down‐regulation of RBL2 (RB transcriptional corepressor like 2) and STAT2 (Signal transducer and activator of transcription 2) in treated MCF7 cells and also showed the significant effect in down‐regulating KRAS (Ki‐ras2 Kirsten rat sarcoma viral oncogene homolog) and SMAD (Sma and Mad proteins) genes in PC3 cells. Comet assay revealed the best effect of Ethyl 2‐(2‐cyano‐3‐(3,4‐dimethoxyphenyl)acrylamido)‐4,5,6,7‐tetrahydrobenzo[ b ]thiophene‐3‐carboxylate in damaging the DNA of MCF7 cells (18.75±1.50 %). Also, DNA fragmentation was studied electrophoretically, which confirmed the results of the comet assay.
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