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  • Title: Design, synthesis and biological evaluation of some novel substituted quinazolines as antitumor agents.
    Author: Alanazi AM, Abdel-Aziz AA, Al-Suwaidan IA, Abdel-Hamide SG, Shawer TZ, El-Azab AS.
    Journal: Eur J Med Chem; 2014 May 22; 79():446-54. PubMed ID: 24763265.
    Abstract:
    A novel series of 6-chloro-2-p-tolylquinazolinone and substituted-(4-methylbenzamido)benzamide (1-20) were designed, synthesized and evaluated for their in-vitro antitumor activity. Compounds 3, 14 and 16 possessed remarkable broad-spectrum antitumor activity. Compound 16 was found to be a particularly active growth inhibitor of the renal cancer (GI50 = 4.07 μM), CNS cancer (GI50 = 7.41 μM), ovarian cancer (GI50 = 7.41 μM) and non-small cell lung cancer (GI50 = 7.94 μM). Compound 16 ranks as nearly 1.5-fold more potent (mean GI50 = 15.8 μM) compared to 5-FU (mean GI50 = 22.6 μM).
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