An efficient synthesis and biological evaluation of novel analogues of natural product Cephalandole A: A new class of antimicrobial and antiplatelet agents

摘要

Cephalandole A2, a small indole alkaloid isolated from the Taiwanese orchid Cephalanceropsis gracilis (Orchidaceae),exhibits anticancer activity. Surprisingly, this natural product has not been evaluated for any other biological activity so far. To discover other novel potential of Cephalandole A2, an efficient and economic synthetic protocol for novel Cephalandole A analogues21a-ohas been developed, in only 3 steps from using indole, and applied for their biological activity. Biological testing showed that Cephalandole A2and its novel analogues21a-oexhibited potential antimicrobial and antiplatelet activity in preliminary assay. To the best of our knowledge, this is the first report of Cephalandole A2and its novel synthetic analogues21a-oas a new class of antimicrobial and antiplatelet agents. In this study,2and other analogues i.e.,21b,21d,21iand21oshowed promising antimicrobial activity against the phytopathogenic bacteria and fungi. Cephalandole A2,21c,21fand21i, also showed potent antiplatelet activity.