2. Academic Validation
  3. Discovery of novel 2-aryl-4-benzoyl-imidazole (ABI-III) analogues targeting tubulin polymerization as antiproliferative agents

Discovery of novel 2-aryl-4-benzoyl-imidazole (ABI-III) analogues targeting tubulin polymerization as antiproliferative agents

  • J Med Chem. 2012 Aug 23;55(16):7285-9. doi: 10.1021/jm300564b.
Jianjun Chen 1,  Sunjoo Ahn,  Jin Wang,  Yan Lu,  James T Dalton,  Duane D Miller,  Wei Li
Affiliations

Affiliation

  • 1 Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
PMID: 22783954 DOI: 10.1021/jm300564b
Abstract

Novel ABI-III compounds were designed and synthesized based on our previously reported ABI-I and ABI-II analogues. ABI-III compounds are highly potent against a panel of melanoma and prostate Cancer cell lines, with the best compound having an average IC(50) value of 3.8 nM. They are not substrate of Pgp and thus may effectively overcome Pgp-mediated multidrug resistance. ABI-III analogues maintain their mechanisms of action by inhibition of tubulin polymerization.

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