New series of cyclopenta(hepta)[b]thiophene and fused cyclohepta[b]thiophene analogs were synthesized. The new analogs were assessed for antibacterial efficacy toward Escherichia coli ATCC 12435, Bacillus cereus UW 85 and Staphylococcus aureus. Compounds 5a, 6b and 12 showed eminent activity toward all selected bacterial strains compared to ampicillin. The antifungal efficacy of the same analogs was also examined toward Candida albicans and Aspergillus fumigatus 293, whereas 5a,b and 12 showed excellent efficacy toward both of the tested fungi. Moreover, 4b, 6a, 14a and 17 demonstrated interesting antifungal efficacy toward A. fumigatus. The same analogs were assessed for antiquorum-sensing efficacy toward Chromobacterium violacium ATCC 12472, whereas 5a, 12 and 15a demonstrated moderate activity. The new analogs were also esteemed for in vitro antitumor activity over HepG2, MCF-7 and HT-29 cancer cell lines. Results indicated that 6b and 10 are the most potent analogs against the three tested cell lines. In addition, 5a, 6a, 7 and 15a displayed interesting activity toward all tested cell lines. The active in vitro antitumor analogs were screened for in vivo antitumor activity over EAC in mice as well as in vitro cytotoxicity toward W138 human normal cell line. Results demonstrated that 6a,b and 10 have the highest in vivo activity, and that all tested compounds were found to be less cytotoxic than 5-FU toward W138 normal cell line. The DNA-binding affinity of the active antimicrobial and/or antitumor analogs was also assessed, whereas 4a, 5b, 10 and 15a exhibited the highest affinity. In silico studies affirmed that the inspected compounds are compatible with Lipinski's rule of five with expected good oral absorption.

合成了新系列的环戊（庚）[ b ]噻吩和稠合的环庚[ b ]噻吩类似物。评估了新的类似物对大肠杆菌ATCC 12435，蜡状芽孢杆菌UW 85和金黄色葡萄球菌的抗菌效果。与氨苄青霉素相比，化合物5a，6b和12对所有选定的细菌菌株均具有显着活性。还检查了相同类似物对白色念珠菌和烟曲霉293的抗真菌功效，而5a，b和12对两种被测真菌均显示出优异的功效。而且，图4b，6a，14a和17证明了对A的有趣的抗真菌功效。曲霉。评估了相同的类似物对紫细菌ATCC 12472的抗群体感应功效，而5a，12和15a表现出中等活性。新的类似物还因其对HepG2，MCF-7和HT-29癌细胞系的体外抗肿瘤活性而备受推崇。结果表明6b和10是针对三种测试细胞系的最有效的类似物。此外，5a，6a，7和15a对所有测试的细胞系显示出有趣的活动。针对在小鼠中对EAC的体内抗肿瘤活性以及对W138人正常细胞系的体外细胞毒性，筛选了活性的体外抗肿瘤类似物。结果表明6a，b和10具有最高的体内活性，并且发现所有测试的化合物对W138正常细胞系的细胞毒性均低于5-FU。还评估了活性抗微生物和/或抗肿瘤类似物的DNA结合亲和力，而4a，5b，10和15a表现出最高的亲和力。在计算机上 研究证实，所检查的化合物符合Lipinski的五种定律，并具有良好的口服吸收性。