Design, modification of phyllanthone derivatives as anti-diabetic and cytotoxic agents.
Nat Prod Res
; 36(1): 371-378, 2022 Jan.
Article
in En
| MEDLINE
| ID: mdl-32608266
ABSTRACT
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 α-glucosidase. In the benzylidene series, most analogues displayed stronger activity than the mother compound. Compound 1c revealed the strongest activity, outperforming the acarbose positive control with an IC50 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 3cand 3d having IC50 values of 57.55 and 68.02 µM, respectively.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Cytotoxins
/
Glycoside Hydrolase Inhibitors
Language:
En
Journal:
Nat Prod Res
Year:
2022
Document type:
Article
Affiliation country: