Literature DB >> 33607574

Furan-2-carboxamide derivative, a novel microtubule stabilizing agent induces mitotic arrest and potentiates apoptosis in cancer cells.

B Shwetha1, M Srinivasa Sudhanva2, G S Jagadeesha3, N R Thimmegowda3, Vivek K Hamse4, B T Sridhar5, K N Thimmaiah6, C S Ananda Kumar7, Rangappa Shobith8, K S Rangappa9.   

Abstract

The vital role played by microtubules in the cell division process, marks them as a potential druggable target to decimate cancer. A novel furan-2-carboxamide based small molecule, is a selective microtubule stabilizing agent (MSA) with IC50 ranging from 4 µM to 8 µM in different cancer cell lines. Inhibition of tubulin polymerization or stabilization of tubulin polymers abrogates chromosomal segregation during cell division, results in cell cycle arrest and leads to cell death due to the delayed repair mechanism. A novel furan-2-carboxamide based small molecule exhibited potent anti-proliferative and anti-metastatic property In-Vitro against the panel of cancer cells. Annexin V-FITC/PI, double staining reveals potent cytotoxic effect of SH09 against HeLa cells. FACS analysis displays induction of G2/M arrest and accumulation of subG1 population of cells upon treatment with SH09. Molecular docking study unveils SH09 binding affinity to the Taxol binding pocket of tubulin proteins and MM-GBSA also confirms strong binding energies of SH09 with tubulin proteins.
Copyright © 2020. Published by Elsevier Inc.

Entities:  

Keywords:  Anticancer agents; Apoptosis; Furan-2-carboxamide; Microtubule stabilizing agents

Year:  2021        PMID: 33607574     DOI: 10.1016/j.bioorg.2020.104586

Source DB:  PubMed          Journal:  Bioorg Chem        ISSN: 0045-2068            Impact factor:   5.275


  2 in total

1.  Synthesis and In Vitro Characterization of Selective Cannabinoid CB2 Receptor Agonists: Biological Evaluation against Neuroblastoma Cancer Cells.

Authors:  Francesca Gado; Rebecca Ferrisi; Sarah Di Somma; Fabiana Napolitano; Kawthar A Mohamed; Lesley A Stevenson; Simona Rapposelli; Giuseppe Saccomanni; Giuseppe Portella; Roger G Pertwee; Robert B Laprairie; Anna Maria Malfitano; Clementina Manera
Journal:  Molecules       Date:  2022-05-07       Impact factor: 4.927

2.  Design and Synthesis of Some New Furan-Based Derivatives and Evaluation of In Vitro Cytotoxic Activity.

Authors:  Syed Nasir Abbas Bukhari; Hasan Ejaz; Mervat A Elsherif; Kashaf Junaid; Islam Zaki; Reham E Masoud
Journal:  Molecules       Date:  2022-04-18       Impact factor: 4.927

  2 in total

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