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Issue 4, 2016
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Identification of gallic acid based glycoconjugates as a novel tubulin polymerization inhibitors

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Abstract

A novel class of gallic acid based glycoconjugates were designed and synthesized as potential anticancer agents. Among all the compounds screened, compound 2a showed potent anticancer activity against breast cancer cells. The latter resulted in tubulin polymerization inhibition and induced G2/M cell cycle arrest, generation of reactive oxygen species, mitochondrial depolarization and subsequent apoptosis in breast cancer cells. In addition, ultraviolet-visible spectroscopy and fluorescence quenching studies of the compound with tubulin confirmed direct interaction of compounds with tubulin. Molecular modeling studies revealed that it binds at the colchicine binding site in tubulin. Further, 2a also exhibited potent in vivo anticancer activity in LA-7 syngeneic rat mammary tumor model. Current data projects its strong candidature to be developed as anticancer agent.

Graphical abstract: Identification of gallic acid based glycoconjugates as a novel tubulin polymerization inhibitors

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Supplementary files

Article information


Submitted
12 Oct 2015
Accepted
01 Dec 2015
First published
01 Dec 2015

Org. Biomol. Chem., 2016,14, 1338-1358
Article type
Paper
Author version available

Identification of gallic acid based glycoconjugates as a novel tubulin polymerization inhibitors

K. Upadhyaya, Hamidullah, K. Singh, A. Arun, M. Shukla, N. Srivastava, R. Ashraf, A. Sharma, R. Mahar, S. K. Shukla, J. Sarkar, R. Ramachandran, J. Lal, R. Konwar and R. P. Tripathi, Org. Biomol. Chem., 2016, 14, 1338
DOI: 10.1039/C5OB02113H

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