New imidazo[2,1- b]thiazole-based aryl hydrazones: unravelling their synthesis and antiproliferative and apoptosis-inducing potential

  • RSC Med Chem. 2020 Jul 22;11(10):1178-1184. 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
Affiliations
  • 1. Department of Fluoro-Agrochemicals , CSIR-Indian Institute of Chemical Technology , Tarnaka , Hyderabad , India . Email: [email protected].
  • 2. Academy of Scientific and Innovative Research , Ghaziabad 201 002 , India.
  • 3. Organic Synthesis and Process Chemistry Division , CSIR-Indian Institute of Chemical Technology , Tarnaka , Hyderabad 500007 , India.
  • 4. School of Pharmaceutical Education and Research (SPER) , Jamia Hamdard , New Delhi 110062 , India.
PMID: 33479622 DOI: 10.1039/d0md00188k
Abstract

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.