新型 6-芳基-5-氰基硫脲的合成及生物活性评价，作为潜在的抗菌和抗癌药物。

Synthesis and bioactivity evaluation of new 6-aryl-5-cyano thiouracils as potential antimicrobial and anticancer agents.

机构信息

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, P.O. Box, 11562, Egypt.

出版信息

Molecules. 2012 Aug 17;17(8):9868-86. doi: 10.3390/molecules17089868.

Several novel 6-aryl-5-cyano thiouracil derivatives were synthesized and explored for their activities as antibacterial, antifungal and anticancer agents. The antimicrobial evaluation revealed that compounds 7b and 7c possessed superior antibacterial activity against the Gram positive bacteria S. aureus and B. subtilis compared to the reference drug amoxicillin. Moreover, compound 4i was found to be a broad spectrum antimicrobial agent and it also exhibited the highest antifungal activity against C. albicans, even higher than the reference drug amphotericin B (MIC = 2.34, 3.00 μg/mL respectively). Selected compounds were tested for in vitro cytotoxicity at a single 10(-5) M concentration in accordance to the NCI (USA) protocol. The preliminary screening results showed that most of the compounds had limited cytotoxic activity against renal cancer UO-31 and/or A498 cell lines. Nevertheless, compounds 6d and 6i displayed potent growth inhibitory effect toward non-small cell lung cancer HOP-92 and leukemia MOLT-4 cell lines, respectively.

合成了几种新型 6-芳基-5-氰基硫脲衍生物，并研究了它们作为抗菌、抗真菌和抗癌剂的活性。抗菌评价表明，化合物 7b 和 7c 对革兰氏阳性菌金黄色葡萄球菌和枯草芽孢杆菌具有比参考药物阿莫西林更强的抗菌活性。此外，化合物 4i 是一种广谱抗菌剂，它对白色念珠菌的抗真菌活性也最高，甚至高于参考药物两性霉素 B（MIC = 2.34、3.00μg/mL）。根据 NCI（美国）方案，以单一 10(-5) M 浓度测试了选定的化合物的体外细胞毒性。初步筛选结果表明，大多数化合物对肾癌细胞 UO-31 和/或 A498 细胞系的细胞毒性有限。然而，化合物 6d 和 6i 对非小细胞肺癌 HOP-92 和白血病 MOLT-4 细胞系的生长抑制作用分别表现出很强的抑制效果。