Design, synthesis, <i>in silico</i> studies, and apoptotic antiproliferative activity of novel thiazole-2-acetamide derivatives as tubulin polymerization inhibitors.

ABSTRACT:

Introduction

Tubulin polymerization inhibitors have emerged as interesting anticancer therapies. We present the design, synthesis, and structural elucidation of novel thiazole-based derivatives to identify novel tubulin inhibitors with potent antiproliferative efficacy and strong inhibition of tubulin polymerization.

Methods

The novel compounds consist of two scaffolds. Scaffold A compounds 10a-e and scaffold B compounds 13a-e. the structures of the newly synthesized compounds 10a-e and 13a-e were validated using ¹H NMR, ¹³C NMR, and elemental analysis.

Results and discussion

The most effective antitubulin derivative was 10a, exhibiting an IC₅₀ value of 2.69 μM. Subsequently, 10o and 13d

SUBMITTER: Al-Wahaibi LH 

PROVIDER: S-EPMC12040969 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature