Premium
A Small Molecule with Bridged Carbonyl and Tri‐fluoro‐aceto‐phenone Groups Impedes Microtubule Dynamics and Subsequently Triggers Cancer Cell Apoptosis
Author(s) -
Mohapatra Saswat,
Gupta Varsha,
Mondal Prasenjit,
Chatterjee Shreyam,
Bhunia Debmalya,
Ghosh Surajit
Publication year - 2021
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202100192
Subject(s) - microtubule , chemistry , moiety , apoptosis , tubulin , cancer cell , cancer , benzothiazole , stereochemistry , microbiology and biotechnology , cancer research , biophysics , biochemistry , biology , genetics
We identified a new microtubule targeted small molecule, which showed significant anticancer activity and induced apoptotic death of cancer cells. Precisely the central bridged carbonyl group and trifluoro‐acetophenone group of a bis‐benzothiazole molecule (BBT) interacts with tubulin close to the curcumin site and perturbs microtubule dynamics as well as causes microtubule depolymerization. We observed a significant enhancement of fluorescence while BBT interacts with the tubulin through bridged carbonyl moiety, a similar phenomenon to colchicine. Further, BBT activates tumor‐suppressing bim and p53‐puma axes to inhibit cancer survival. It also shows promising results against a tumor spheroid model. BBT is also capable of tumor regression, which shows that this molecule can serve as a potential template for the design of next‐generation microtubule targeted anticancer drugs.