Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
Arch Pharm (Weinheim). 2011 Mar;344(3):184-96. doi: 10.1002/ardp.201000188. Epub 2010 Dec 22.
Synthesis and evaluation of anticancer and antimicrobial activity of some novel pyrazolopyrimidines and fused pyrazolopyrimidines are reported. Twelve analogs were selected to be evaluated for their in vitro anticancer potential against a panel of three human tumor cell lines: hepatocellular carcinoma HepG2, cervical carcinoma HelaS3 and colon carcinoma CaCo. The obtained data revealed that eight compounds namely; 6b, 6d, 7c, 8c, 10b, 12b, 13a and 13b were able to exhibit variable degrees of anticancer activities against the three used cell lines, of which compound 6d proved to be the most active. On the other hand, all the newly synthesized compounds were subjected to in vitro antibacterial and antifungal screening. Almost all the tested compounds were found to possess variable degrees of antimicrobial activities. Collectively, compounds 7c, 8c, 12b, 13a and 13b could be considered as possible agents with dual anticancer and antimicrobial activities.
报告了一些新型吡唑并嘧啶和稠合吡唑并嘧啶的合成及抗癌和抗菌活性评价。选择了 12 种类似物来评估它们对三种人肿瘤细胞系（肝癌 HepG2、宫颈癌 HelaS3 和结肠癌 CaCo）的体外抗癌潜力。获得的数据表明，有 8 种化合物，即 6b、6d、7c、8c、10b、12b、13a 和 13b，能够对三种使用的细胞系表现出不同程度的抗癌活性，其中化合物 6d 表现出最强的活性。另一方面，所有新合成的化合物都进行了体外抗菌和抗真菌筛选。几乎所有测试的化合物都被发现具有不同程度的抗菌活性。总的来说，化合物 7c、8c、12b、13a 和 13b 可以被认为是具有抗癌和抗菌双重活性的潜在药物。
