A new class of cytotoxic agents targets tubulin and disrupts microtubule dynamics.

ABSTRACT: Despite the advances in treatment strategies, cancer is still the second leading cause of death in the USA. A majority of the currently used cancer drugs have limitations in their clinical use due to poor selectivity, toxic side effects and multiple drug resistance, warranting the development of new anticancer drugs of different mechanisms of action. Here we describe the design, synthesis and initial biological evaluation of a new class of antimitotic agents that modulate tubulin polymerization. Structurally, these compounds are chalcone mimics containing a 1-(1H-imidazol-2-yl)ethan-1-one moiety, which was initially introduced to act as a metal-binding group and inhibit histone deacetylase enzymes. Although several analogues selectively inhibited purified HDAC8 with IC₅₀ values

SUBMITTER: Al-Hamashi AA 

PROVIDER: S-EPMC8530978 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature