Synthesis and Biological Evaluation of Sclareolide-Indole Conjugates and Their Derivatives.

ABSTRACT: Sclareolide is a sesquiterpene lactone isolated from various plant sources in tons every year and is commercially used as a flavor ingredient in the cosmetic and food industries. Antitumor and antiviral activities of sclareolide have been previously reported. However, biological studies of sclareolide synthetic analogous are few. In view of these, we developed a robust synthetic method that allows the assembly of 36 novel sclareolide-indole conjugates and their derivatives. The synthetic method was based on TiCl₄-promoted nucleophilic substitution of sclareolide-derived hemiacetal 4, while electron-rich aryles including indoles, polyphenol ethers, and pyrazolo [1,5-a]pyridine were good substrates. The stereochemistry of the final products was confirmed by single-crystal X

SUBMITTER: Cheng Y 

PROVIDER: S-EPMC9961340 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature