新型基于咪唑并[2,1-]噻唑的芳基腙：揭示其合成方法以及抗增殖和诱导凋亡的潜力。
New imidazo[2,1-]thiazole-based aryl hydrazones: unravelling their synthesis and antiproliferative and apoptosis-inducing potential.
作者信息
Shareef Mohd Adil, Devi Ganthala Parimala, Rani Routhu Sunitha, Kumar C Ganesh, Kamal Ahmed, Babu Bathini Nagendra
机构信息
Department of Fluoro-Agrochemicals , CSIR-Indian Institute of Chemical Technology , Tarnaka , Hyderabad , India . Email:
Academy of Scientific and Innovative Research , Ghaziabad 201 002 , India.
出版信息
RSC Med Chem. 2020 Jul 22;11(10):1178-1184. doi: 10.1039/d0md00188k. eCollection 2020 Oct 1.
Abstract
Herein, we have designed and synthesized new imidazo[2,1-]thiazole-based aryl hydrazones () and evaluated their anti-proliferative potential against a panel of human cancer cell lines. Among the synthesized compounds, and elicited promising cytotoxicity against the breast cancer cell line MDA-MB-231 with IC values of 1.65 and 1.12 μM, respectively. Cell cycle analysis revealed that and significantly arrest MDA-MB-231 cells in the G0/G1 phase. In addition, detailed biological studies such as annexin V-FITC/propidium iodide, DCFH-DA, JC-1 and DAPI staining assays revealed that and triggered apoptosis in MDA-MB-213 cells. Overall, the current work demonstrated the cytotoxicity and apoptosis-inducing potential of and in breast cancer cells and suggested that they could be explored as promising antiproliferative leads in the future.
摘要
在此，我们设计并合成了新型咪唑并[2,1 - ]噻唑基芳基腙（），并评估了它们对一组人类癌细胞系的抗增殖潜力。在合成的化合物中，和对乳腺癌细胞系MDA - MB - 231表现出有前景的细胞毒性，IC值分别为1.65和1.12 μM。细胞周期分析表明，和显著使MDA - MB - 231细胞停滞在G0/G1期。此外，诸如膜联蛋白V - FITC/碘化丙啶、DCFH - DA、JC - 1和DAPI染色分析等详细的生物学研究表明，和在MDA - MB - 213细胞中引发了凋亡。总体而言，当前工作证明了和在乳腺癌细胞中的细胞毒性和诱导凋亡的潜力，并表明它们未来有望作为有前景的抗增殖先导物进行探索。
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