Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
Arch Pharm Res. 2012 Nov;35(11):1909-17. doi: 10.1007/s12272-012-1107-6. Epub 2012 Dec 4.
New series of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines (7a,b) and thieno[2,3-b:4,5-b'] dipyridine (11a-c) were synthesized from 4-aryl-6-(4-chlorophenyl)-2-thioxo-1,2-dihydro pyridine-3-carbonitriles 4a,b via application of Thorpe-Zielger reaction. The novel target compounds were evaluated in vitro for their anticancer activity against human breast adenocarcinoma MCF-7 and colon carcinoma cell line (HCT 116). Most of the tested compounds exploited potent to moderate growth inhibitory activity, in particular compound 11d, which exhibited superior potency to the reference drug Doxorubicin (IC(50) = 5.95, 6.09 and 8.48, 8.15 μM, respectively). The structures of the compounds obtained were determined by spectroscopic data.
新型吡啶并[3',2':4,5]噻吩并[3,2-d]嘧啶（7a，b）和噻吩并[2,3-b:4,5-b']二吡啶（11a-c）系列化合物是由 4-芳基-6-(4-氯苯基)-2-硫代-1,2-二氢吡啶-3-甲腈 4a，b 通过 Thorpe-Zielger 反应合成得到的。对这些新的目标化合物进行了体外抗癌活性测试，针对人乳腺癌 MCF-7 和结肠癌细胞系（HCT 116）进行了测试。大多数测试的化合物都表现出了很强到中等的生长抑制活性，特别是化合物 11d，其对参考药物阿霉素（IC（50）= 5.95、6.09 和 8.48、8.15 μM）的活性更强。通过光谱数据确定了获得的化合物的结构。
