Design, modification of phyllanthone derivatives as anti-diabetic and cytotoxic agents
| Autor: | Thanh-The Ngo, Thi-Phuong Nguyen, Jirapast Sichaem, Thuc-Huy Duong, Hoang-Vinh-Truong Phan, Van-Giau Vo, Tien-Cong Nguyen, Van-Kieu Nguyen, Duc-Dung Pham, Ngoc-Hong Nguyen, Huu-Hung Nguyen |
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| Rok vydání: | 2020 |
| Předmět: |
Design modification
010405 organic chemistry Cytotoxins Organic Chemistry Imine alpha-Glucosidases Plant Science 01 natural sciences Biochemistry Combinatorial chemistry 0104 chemical sciences Analytical Chemistry Molecular Docking Simulation 010404 medicinal & biomolecular chemistry chemistry.chemical_compound Structure-Activity Relationship chemistry Hypoglycemic Agents Glycoside Hydrolase Inhibitors Acarbose Cytotoxicity |
| DOI: | 10.6084/m9.figshare.12600942.v1 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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