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  • Title: Synthesis and anti-tumor activity of novel combretastatins: combretocyclopentenones and related analogues.
    Author: Nam NH, Kim Y, You YJ, Hong DH, Kim HM, Ahn BZ.
    Journal: Bioorg Med Chem Lett; 2002 Aug 05; 12(15):1955-8. PubMed ID: 12113817.
    Abstract:
    A series of 2-(3,4,5-trimethoxyphenyl)-3-arylcyclopent-2-ene-1-ones (8a-8e) and their related analogues, including pentenone 9a, pentenol 10a, pentene 12a, and furane 15, were synthesized and evaluated for cytotoxicity against murine and human tumor cell lines. Compounds 8a-c, 8e and 9a showed strong cytotoxicity with IC(50) values in the range of 8-34ng/mL. Compound 8e exhibited significant anti-tumor activity in BDF1 mice bearing Lewis lung carcinoma cells with an inhibition ratio of 59%.
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