PVHD121 is potent antimitotic agent that binds to the colchicine site of tubulin. PVHD121 selectively inhibits microtubule formation at centrosomes during mitosis. It delays entry into mitosis causing long lasting mitotic arrest by activation of spindle checkpoint.
potent antimitotic agent that inhibits microtubule formation at centrosomes during mitosis
A quinazoline derivative PVHD121 (1a) was shown to have strong antiproliferative activity against various tumor-derived cell lines, including A549 (lung), NCI-H460 (lung), HCT116 (colon), MCF7 (breast), PC3 (prostate), and HeLa (cervical) cells with IC50 values from 0.1 to 0.3 μM.
In the research field of tubulin-binding agents for the development of anticancer agents, hidden targets are emerging as a problem in understanding the exact mechanisms of actions. The quinazoline derivative 1-(4-methoxyphenyl)-1-(quinazolin-4-yl)ethan-1-ol (PVHD121) has anti-cell proliferative activity and inhibits tubulin polymerization
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