Jump to main content
Jump to site search

Issue 9, 2016
Previous Article Next Article

Synthesis and biological evaluation of novel indole derivatives containing sulfonamide scaffold as potential tubulin inhibitor

Author affiliations

Abstract

Microtubule-targeted drugs play a critical role in various types of cancer therapy worldwide. In our study, a series of novel indole derivatives containing a sulfonamide scaffold were designed, synthesized and biologically evaluated as potential tubulin polymerization inhibitors. Among them, compound 18 displayed the most potent inhibitory effect on antiproliferative activity against four types of human cancer cell lines (IC50 values of 0.24–0.59 μM) and tubulin assembly (IC50 = 1.82 μM). Further investigation demonstrated that compound 18 is a potent inducer of apoptosis in HeLa cells and could cause cell arrest in the G2/M phase of the cell cycle. Molecular docking and confocal microscopy assay results indicate that compound 18 could bind tightly to the colchicine binding site of tubulin and act as a tubulin polymerization inhibitor. A 3D-QSAR model was also built to provide more information which could be applied to the design of new molecules with more potent tubulin inhibitory activity.

Graphical abstract: Synthesis and biological evaluation of novel indole derivatives containing sulfonamide scaffold as potential tubulin inhibitor

Back to tab navigation

Supplementary files

Article information


Submitted
09 May 2016
Accepted
21 Jun 2016
First published
22 Jun 2016

Med. Chem. Commun., 2016,7, 1759-1767
Article type
Research Article

Synthesis and biological evaluation of novel indole derivatives containing sulfonamide scaffold as potential tubulin inhibitor

R. Man, D. Tang, X. Lu, Y. Duan, X. Tao, M. Yang, L. Wang, B. Wang, C. Xu and H. Zhu, Med. Chem. Commun., 2016, 7, 1759
DOI: 10.1039/C6MD00255B

Search articles by author

Spotlight

Advertisements