Department of Chemistry, Saurashtra University, Rajkot, Gujarat, 360005, India.
Department of Chemistry, RK University, Rajkot, Gujarat, 360020, India.
Mol Divers. 2023 Jun;27(3):1345-1357. doi: 10.1007/s11030-022-10493-7. Epub 2022 Jul 19.
A novel series of benzofuran bearing thiazole hybrids were synthesized by the multistep reaction approach. All synthesized molecules were selected by the National Cancer Institute, USA for one-dose anticancer activity against 60 various human cancer cell lines indicating nine types of cancer. Among thirteen compounds, two compounds showed higher lethality, so, it was selected for five-dose anticancer screening against all cancer cell lines. Compound 8g and 8h were displayed remarkable antiproliferative activity with GI values ranging from 0.295 to 4.15 μM and LC values ranging from 4.43 to > 100 μM. All data are compared with standard drugs fluorouracil and doxorubicin. Compound 8g showed higher potency as a cytotoxic molecule then fluorouracil. Furthermore, all new hybrids were studied for molecular docking into the active binding sites of 1HOV protein.
通过多步反应方法合成了一系列新型苯并呋喃噻唑杂合体。所有合成的分子均由美国国立癌症研究所选择，用于针对 60 种不同的人类癌细胞系进行单次剂量抗癌活性测试，涵盖九种癌症类型。在这 13 种化合物中，有两种化合物表现出更高的致死性，因此被选择用于对所有癌细胞系进行五剂量抗癌筛选。化合物 8g 和 8h 表现出显著的抗增殖活性，GI 值范围为 0.295 至 4.15 μM，LC 值范围为 4.43 至 >100 μM。所有数据均与标准药物氟尿嘧啶和阿霉素进行了比较。化合物 8g 作为细胞毒性分子的效力高于氟尿嘧啶。此外，所有新的杂合体都被研究了其与 1HOV 蛋白的活性结合位点的分子对接。
