The total synthesis of majusculamide D(1)was achieved from commercially available materials.In addition,we synthesized eight analogues including three stereoisomers of majusculamide D that differ in the fatty acid cha...The total synthesis of majusculamide D(1)was achieved from commercially available materials.In addition,we synthesized eight analogues including three stereoisomers of majusculamide D that differ in the fatty acid chain.Six analogues including a simplified analogue 29 exhibited significant nanomolar-level IC50 values against Panc-1 cells in MTT assays.A preliminary SAR analysis indicated that the hydroxyl group at C10 and C2−C3 unsaturated double bond of majusculamide D were essential in maintaining the high activity against Panc-1 cells and the orientation of C40-Me and C42-Me groups was tolerable.展开更多
基金supported by the National Natural Science Foundation of China(82073695 to L.W.and U1801288 to Y.C.)the Fundamental Research Funds for the Central Universities and Hundred Young Academic Leaders Program of Nankai University to L.W.(Nankai University),the Frontiers Science Center for New Organic Matter(63181206).
文摘The total synthesis of majusculamide D(1)was achieved from commercially available materials.In addition,we synthesized eight analogues including three stereoisomers of majusculamide D that differ in the fatty acid chain.Six analogues including a simplified analogue 29 exhibited significant nanomolar-level IC50 values against Panc-1 cells in MTT assays.A preliminary SAR analysis indicated that the hydroxyl group at C10 and C2−C3 unsaturated double bond of majusculamide D were essential in maintaining the high activity against Panc-1 cells and the orientation of C40-Me and C42-Me groups was tolerable.
