Design and synthesis of new lupeol derivatives and their α-glucosidase inhibitory and cytotoxic activities

A series of lupeol derivatives 2, 2a-2f, 2a-2h, 3a-3e, and 4a-4b were designed, synthesised and evaluated for their alpha-glucosidase inhibitory and cytotoxic activities. Among synthetic derivatives, lupeol analogues 2b and 2e containing a benzylidene chain exhibited the best activity against alpha-glucosidase and superior to the positive agent with the IC50 values of 29.4 +/- 1.33 and 20.1 +/- 0.91 mu M, respectively. Lupeol analogues 2d and 3a showed weak cytotoxicity against K562 cell line with the IC50 values of 76.6 +/- 2.40 and 94.4 +/- 1.51 mu M, respectively. [GRAPHICS] .

Automated summary

A series of lupeol derivatives were designed and synthesized for their inhibitory activity against alpha-glucosidase and cytotoxic activities. Lupeol analogues 2b and 2e showed the best activity against alpha-glucosidase, while 2d and 3a exhibited weak cytotoxicity against K562 cell line.