1. Synthesis of aminomethyl linked (+)-usnic acid derivatives via the Mannich reaction and evaluation of their biological activities.
- Author
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Guddeti, Dileep Kumar, Kolukula, Ashwini, Siva, Bandi, Jadav, Surender Singh, Tiwari, Ashok K., Komati, Anusha, Andugulapati, Sai Balaji, Ramalingam, Vaikundamoorthy, and Katragadda, Suresh Babu
- Subjects
MANNICH reaction ,ACID derivatives ,SECONDARY amines ,ANTIOXIDANTS ,MOLECULAR docking - Abstract
(+)-Usnic acid (UA), a natural dibenzofuran derivative, abundantly produced by lichens and possess wide number of biomedical applications including antibacterial, anti-inflammatory, anti-oxidant and anticancer activities. In the present study, as series of usnic acid derivatives (3a-3i) were synthesised using Mannich reaction assessed for their antioxidant, α-glucosidase, and anticancer activities. The in vitro antioxidant activity showed that compound 3d displayed potent antioxidant activity by scavenging the activities of DPPH and ABTS
+ . The compounds 3d and 3e showed potent cytotoxic activity against HepG2 cancer cells by arresting the cell cycle at S phase and regulating the Bax/BcL2 expression and subsequently induce the apoptosis. Overall, the results clearly indicated that (+)-usnic acid derivatives bearing secondary amines are useful scaffolds for the development of drug candidates for treatment of oxidative stress mediated cancer and metabolic disorders. [ABSTRACT FROM AUTHOR]- Published
- 2025
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