5-arylalkynyl-2-benzoyl thiophene: a novel microtubule inhibitor exhibits antitumor activity without neurological toxicity.

ABSTRACT: The composition of microtubules involving several steps, including the polymerization and depolymerization of α-tubulin and β-tubulin heterodimers. Microtubule-targeting agents can increase or inhibit microtubule polymerization, thereby disrupting the dynamic process and stalling cells in G2/M phase. Microtubule-targeting agents are generally cytotoxic, which neurological toxicity being one of the significant adverse events associated. We recently reported a novel 5-arylalkynyl-2-benzoyl thiophene (PST-3) that exhibited broad-spectrum cellular cytotoxicity and in vivo potency with high safety. PST-3 was a substrate of p-gp, which could not cross the blood-brain barrier and lead to less neurotoxicity. The antitumor activities in vitro demonstrated that PST-3 combined with the

SUBMITTER: Zhuang Y 

PROVIDER: S-EPMC8822276 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature