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Novel Thiadiazoline Spiro Quinoline Analogues Induced Cell death in MCF-7 cells via G2/M Phase Cell Cycle Arrest

Authors :
Selvaraj Shyamsivappan
Raju Vivek
Thangaraj Suresh
Adhigaman Kaviyarasu
Sundarasamy Amsaveni
Shunmuganarayanan Athimoolam
Palathurai Subramaniam Mohan
Publication Year :
2021
Publisher :
Research Square Platform LLC, 2021.

Abstract

A progression of novel thiadiazoline spiro quinoline derivatives were synthesized from potent thiadiazoline spiro quinoline derivatives . The synthesized compounds portrayed by different spectroscopic studies and single X-ray crystallographic studies. The compounds were assessed for in vitro anticancer properties towards MCF-7 and HeLa cells. The compounds showed superior inhibition action MCF-7 malignant growth cells. Amongst, the compound 4a showed significant inhibition activity, the cell death mechanism was evaluated by fluorescent staining, and flow cytometry, RT-PCR, and western blot analyses. The in vitro anticancer results revealed that the compound 4a induced apoptosis by inhibition of estrogen receptor alpha (ERα) and G2/M phase cell cycle arrest. The binding affinity of the compounds with ERα and pharmacokinetic properties were confirmed by molecular docking studies.

Details

Database :
OpenAIRE
Accession number :
edsair.doi...........c3f30f2fd580be56c551f17f8f07c34e
Full Text :
https://doi.org/10.21203/rs.3.rs-289802/v1