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New imidazo[2,1-b]thiazole-based aryl hydrazones: unravelling their synthesis and antiproliferative and apoptosis-inducing potential
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-07-22 , DOI: 10.1039/d0md00188k
Mohd Adil Shareef 1, 2 , Ganthala Parimala Devi 1, 2 , Sunitha Rani Routhu 3 , C Ganesh Kumar 3 , Ahmed Kamal 2, 4 , Bathini Nagendra Babu 1, 2
Affiliation  

Herein, we have designed and synthesized new imidazo[2,1-b]thiazole-based aryl hydrazones (9a–w) and evaluated their anti-proliferative potential against a panel of human cancer cell lines. Among the synthesized compounds, 9i and 9m elicited promising cytotoxicity against the breast cancer cell line MDA-MB-231 with IC50 values of 1.65 and 1.12 μM, respectively. Cell cycle analysis revealed that 9i and 9m 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 9i and 9m triggered apoptosis in MDA-MB-213 cells. Overall, the current work demonstrated the cytotoxicity and apoptosis-inducing potential of 9i and 9m in breast cancer cells and suggested that they could be explored as promising antiproliferative leads in the future.

中文翻译:

新的咪唑并[2,1-b]噻唑基芳基:揭示它们的合成及其抗增殖和诱导凋亡的潜力

在这里,我们设计并合成了新的基于咪唑并[2,1 - b ]噻唑的芳基(9a–w),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,9i9m引发了针对乳腺癌细胞系MDA-MB-231的有希望的细胞毒性,IC 50值分别为1.65和1.12μM。细胞周期分析显示9i9m将MDA-MB-231细胞显着阻滞在G0 / G1期。此外,详细的生物学研究(例如膜联蛋白V-FITC /碘化丙啶,DCFH-DA,JC-1和DAPI染色试验)显示9i9m触发了MDA-MB-213细胞的凋亡。总的来说,目前的研究证明了9i9m在乳腺癌细胞中具有细胞毒性和诱导细胞凋亡的潜力,并建议将来可以将它们作为有希望的抗增殖药加以研究。
更新日期:2020-07-22
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