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DOI: 10.1055/s-0032-1320265
Briarane Diterpenoids: Potential tumor cell growth inhibitor
The structural complexity of briarane diterpenoids challenges the chemical synthesis and SAR studies of the intriguing metabolites. Our systematic study on briarane deterpenoids concerning their chemistry and bioactivities led the isolation and structural elucidation of a series of briaranes, gemmacolides G-Y. The absolute configuration was determined by a TDDFT/CD approach. In in vitro bioassays, gemmacolide J, V, and Y (1, 2, 3), showed potent growth inhibition towards tumor cell lines of A549 and MG63, being stronger than the positive control of adriamycin. The identification of possible new targets of compound 1 was conducted using the Inverse Virtual Screening approach, which showed significant interactions in the binding sites gamma, ftase, tank1, and jmjd3. The tumor cell growth inhibitory mechanism of compound 1 is currently under investigation.