Alanazi Amer M, Abdel-Aziz Alaa A-M, Al-Suwaidan Ibrahim A, Abdel-Hamide Sami G, Shawer Taghreed Z, El-Azab Adel S
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia; Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt.
Eur J Med Chem. 2014 May 22;79:446-54. doi: 10.1016/j.ejmech.2014.04.029. Epub 2014 Apr 12.
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).
设计、合成了一系列新型的6-氯-2-对甲苯基喹唑啉酮和取代的-(4-甲基苯甲酰胺基)苯甲酰胺(1-20)，并对其体外抗肿瘤活性进行了评估。化合物3、14和16具有显著的广谱抗肿瘤活性。发现化合物16是一种特别有效的肾癌生长抑制剂(GI50 = 4.07 μM)、中枢神经系统癌(GI50 = 7.41 μM)、卵巢癌(GI50 = 7.41 μM)和非小细胞肺癌(GI50 = 7.94 μM)。与5-氟尿嘧啶(平均GI50 = 22.6 μM)相比，化合物16的效力几乎高1.5倍(平均GI50 = 15.8 μM)。
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