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  • Title: Discovery of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers. 2. Identification of more aqueous soluble analogs as potential anticancer agents.
    Author: Kemnitzer W, Kuemmerle J, Zhang HZ, Kasibhatla S, Tseng B, Drewe J, Cai SX.
    Journal: Bioorg Med Chem Lett; 2009 Aug 01; 19(15):4410-5. PubMed ID: 19500976.
    Abstract:
    As a continuation of our efforts to discover and develop the 3-aryl-5-aryl-1,2,4-oxadiazole series of apoptosis inducers as potential anticancer agents, we explored substitutions at the 2- and 3-positions of the 3-aryl group to improve the aqueous solubility properties and identify development candidates. A small substitution such as methyl or hydroxymethyl at the 2-position was well tolerated. This modification, in combination with a 3-substituted furan ring as the 5-aryl group, resulted in 4g and 4h, which have improved solubility properties. Compound 4g was found to have good in vivo efficacy in animal studies via intravenous administration.
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