Synthesis and Preliminary Biological Evaluation of New Heterocyclic Carboxamide Models
作者:Kamal Sweidan、Jorn Engelmann、Walid Rayyan、Dima Sabbah、Musa Zarga、Tariq Al-Qirim、Yusuf Al-Hiari、Ghassan Sheikha、Ghassan Shattat
DOI:10.2174/1570180812666141201222527
日期:2015.3.24
The heterocyclic system is a promising core nucleus in many bioactive compounds. This work describes our effort
to synthesize and characterize a set of new biphenyl, benzofuran and benzothiophene carboxamide derivatives. Our
biological studies showed that compounds 10 and 17 have antifungal activity against C. galabrate more potent than fluconazole
compounds 9, 10, and 17 exerted cytotoxic activities in immortalized embryonic mouse fibroblast cells (3T3)
and a human cervical cancer cell line (HeLa); in particular, the cyclic amidine derivative 17 showed selective toxicity
against HeLa. This study showed that the tested compounds have the potential to be useful as antitumor drugs after further
optimization.
杂环系统是许多生物活性化合物中一个有潜力的核心核。本工作描述了我们合成和表征一组新的联苯、苯并呋喃和苯并噻吩羧酰胺衍生物的努力。我们的生物学研究表明,化合物10和17对C. galabrate的抗真菌活性比氟康唑更强;化合物9、10和17在永生化胚胎小鼠成纤维细胞(3T3)和人类宫颈癌细胞系(HeLa)中表现出细胞毒活性;特别是环状脒衍生物17对HeLa表现出选择性毒性。这项研究表明,经过进一步优化,被测试的化合物有可能作为有用的抗癌药物。