Taher Azza Taher, Helwa Amira Atef
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
Chem Pharm Bull (Tokyo). 2012;60(10):1305-13. doi: 10.1248/cpb.c12-00557. Epub 2012 Aug 3.
The synthesis of some new 4-chloro-pyrimidine-5-carbonitriles (3b-d), 4-substituted-amino-pyrimidine-5-carbonitriles (4a-g), trioxo and dioxo-thiazolo[3,2-a]pyrimidine-6-carbonitriles (5a-c and 6a-h) have been described. The obtained compounds were evaluated for their in-vitro antitumor activity. A single dose (10 µM) of the test compounds was used in the National Cancer Institute (NCI) 60 cell lines panel assay. Compounds 3c and 4f showed high inhibitory activity against leukemia, whereas, compounds 3b and 4d, g displayed moderate activity. On the other hand, all compounds were screened for their in-vitro antibacterial and antifungal activities. Compounds 3d and 4b exhibited significant antibacterial activity against Staphylococcus aureus. Compound 4e showed two folds inhibitory activity against Entrobacter aerogener compared with the reference drug Tobramycin.
已描述了一些新型4-氯嘧啶-5-腈（3b - d）、4-取代氨基嘧啶-5-腈（4a - g）、三氧代和二氧代噻唑并[3,2 - a]嘧啶-6-腈（5a - c和6a - h）的合成。对所获得的化合物进行了体外抗肿瘤活性评估。在国立癌症研究所（NCI）60细胞系实验中使用单剂量（10 µM）的测试化合物。化合物3c和4f对白血病显示出高抑制活性，而化合物3b和4d、g表现出中等活性。另一方面，对所有化合物进行了体外抗菌和抗真菌活性筛选。化合物3d和4b对金黄色葡萄球菌表现出显著的抗菌活性。与参考药物妥布霉素相比，化合物4e对产气肠杆菌显示出两倍的抑制活性。
