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Design, synthesis, and evaluation of cystargolide-based β-lactones as potent proteasome inhibitors.
TLDR
The novel drug lead 5k is a more potent proteasome inhibitor than carfilzomib with mid-to-low nanomolar IC50 measurements and it is cytotoxic against multiple cancer cell lines at levels approaching those of carfilZomib.
Total synthesis and absolute stereochemistry of the proteasome inhibitors cystargolides A and B.
TLDR
Evaluation of synthetic cystargolides and derivatives showed that the natural (2S,3R) stereochemistry is essential for activity, and benzyl esters (-)-10 and (-)-15 were found to be about 100 times more potent, and to selectively kill MCF-7 cancerous cells.
A total synthesis of (-)-Hortonone C.
TLDR
Comparison of optical rotation data confirmed that the absolute configuration of natural hortonone C is (6S,7S,10S), and its absolute stereochemistry confirmed.
Design, synthesis, and evaluation of cystargolide-based beta-lactones as potent proteasome inhibitors.
The peptidic β-lactone proteasome inhibitors (PIs) cystargolides A and B were used to conduct structure-activity relationship (SAR) studies in order to assess their anticancer potential. A total of