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n-[3-(2,5-dimethoxybenzyloxy)-4-(methanesulfonyl-methylamino)phenyl]-1,3-benzodioxole-5-carboxamide

Development stage
Preclinical
Lead developer
King AbdulAziz University
Modality
Small Molecules
01

Overview

n-[3-(2,5-dimethoxybenzyloxy)-4-(methanesulfonyl-methylamino)phenyl]-1,3-benzodioxole-5-carboxamide, also referred to as Compound 10, is a novel nimesulide-derived small molecule designed as a tubulin-targeting anticancer agent. Developed by modifying the scaffold of the non-steroidal anti-inflammatory drug (NSAID) nimesulide, this compound incorporates a dimethoxy benzamide moiety and a benzodioxole group to enhance its affinity for the colchicine binding site on tubulin. By inhibiting tubulin polymerization, the drug disrupts microtubule dynamics, leading to mitotic arrest and apoptosis in cancer cells. Preclinical evaluations have demonstrated potent antiproliferative activity against breast cancer (MDA-MB-468) and prostate cancer (DU145) cell lines with nanomolar IC50 values, while showing significantly lower toxicity toward benign cells.

Other names
Nimesulide derivative 10
02

Targets

TUBB (Tubulin (alpha and beta subunits))

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