摘要：A series of 2-[(arylidene)amino]-cycloalkyl[b]thiophene-3- -carbonitriles (2a-x) was synthesized by incorporation of substituted aromatic aldehydes in Gewald adducts (1a-c).The title compounds were screened for their antifungal activity against Candida krusei and Criptococcus neoformans and for their antiproliferative activity against a panel of 3 human cancer cell lines (HT29,NCI H-292 and HEP).For antiproliferative activity,the partial least squares (PLS) methodology was applied.Some of the prepared compounds exhibited promising antifungal and proliferative properties.The most active compounds for antifungal activity were cyclohexyl[b]thiophene derivatives,and for antiproliferative activity cycloheptyl[b]thiophene derivatives,especially 2-[(1H-indol-2-yl-methylidene)amino]- -5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carbonitrile (2r),which inhibited more than 97 % growth of the three cell lines.The PLS discriminant analysis (PLS-DA) applied generated good exploratory and predictive results and showed that the descriptors having shape characteristics were strongly correlated with the biological data.
关键词：cycloalkyl[b]thiophene derivatives;antifungal activity;antiproliferative activity;PLS-DA;Pentacle program
