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Anti-cancer Activity of M-Carborane-Containing Trimethoxyphenyl Derivatives Through Tubulin Polymerization Inhibition

Anti-cancer Activity of M-Carborane-Containing Trimethoxyphenyl Derivatives Through Tubulin Polymerization Inhibition

Asako Kaise, Yasuyuki Endo, Kiminori Ohta

Bioorg Med Chem. 2019 Mar 15;27(6):1139-1144.

PMID: 30773422

Abstract:

m-Carborane-containing compound 1a was identified as a cell growth inhibitor from a random screening of a boron compound library. As 1a is a mixture of diastereomers due to the presence of two chiral carbons, we designed achiral derivatives 2-4 and studied the structure-activity relationships of the methoxy groups on the benzene ring. 3,4,5-Trimethoxybenzyl derivative 2a and 3,4,5-trimethoxybenzoyl derivative 3a showed more potent anti-cancer activity against the human breast cancer cell line MDA-MB-453 than lead compound 1a. Compound 3a inhibited tubulin polymerization in a dose-dependent manner.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP16986246	m-Carborane		16986-24-6	Price

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