Design, modification of phyllanthone derivatives as anti-diabetic and cytotoxic agents.

Twelve benzylidene derivatives, one Baeyer-Villiger oxidative, six imine derivatives were successfully designed and synthesised from phyllanthone. In the search for potential new anti-diabetic agents, phyllanthone along with its benzylidene and oxidation analogues were evaluated for enzyme inhibition against -glucosidase. In the benzylidene series, most analogues displayed stronger activity than the mother compound. Compound revealed the strongest activity, outperforming the acarbose positive control with an IC value of 19.59 µM. Phyllanthone and its derivatives were then tested for cytotoxic activity against the K562 cell line. The imine analogues displayed the most powerful cytotoxic activity with and having IC values of 57.55 and 68.02 µM, respectively.