Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2021 Nov 5:223:113656.
doi: 10.1016/j.ejmech.2021.113656. Epub 2021 Jun 18.

Anticancer properties of indole derivatives as IsoCombretastatin A-4 analogues

Shannon Pecnard  1 , Abdallah Hamze  2 , Jérome Bignon  3 , Bastien Prost  4 , Alain Deroussent  5 , Laura Gallego-Yerga  6 , Rafael Peláez  6 , Ji Yeon Paik  7 , Marc Diederich  7 , Mouad Alami  8 , Olivier Provot  9
Affiliations

Anticancer properties of indole derivatives as IsoCombretastatin A-4 analogues

Shannon Pecnard et al. Eur J Med Chem. .

Abstract

In this study, a variety of original ligands related to Combretastatin A-4 and isoCombretastatin A-4, able to inhibit the tubulin polymerization into microtubules, was designed, synthesized, and evaluated. Our lead compound 15d having a quinazoline as A-ring and a 2-substituted indole as B-ring separated by a N-methyl linker displayed a remarkable sub-nanomolar level of cytotoxicity (IC50 < 1 nM) against 9 human cancer cell lines.

Keywords: Cancer; Cytotoxicity; Indole; Oxazinoindole; Pyridoindole; Quinazoline; Tubulin; isoCA-4.

PubMed Disclaimer

Conflict of interest statement

Declaration of competing interest The authors declare no conflict of interest.

MeSH terms

LinkOut - more resources