Arizona State University

Arizona Board of Regents, a Body Corporate

Robin K Pettit

George R Pettit

Rui Tan

Pablo Arce

The present disclosure relates to Silstatin compounds, pharmaceutical compositions comprising such compounds, kits, and methods for using such compounds or pharmaceutical compositions.

Silstatin compounds

The present invention is directed to cyclodepsipeptide compounds having antineoplastic and/or antimicrobial activity, preferably Kitastatin 1. The present invention is further directed to methods of inhibiting cancer cell growth and/or microbial growth in a host inflicted therewith by administering cyclodepsipeptide compounds to the inflicted host.

Cyclodepsipeptides with antineoplastic activity and methods of using to inhibit cancer and microbial growth

Antifungals based on dolasatin 10 and four structural modifications thereof (herein &ldquo;peptides&rdquo;) and methods of treating a host afflicted with a fungi-induced infection are herein described. In broth macrodilution assays, these peptides were fungicidal for ATCC stains and clinical isolates of . Specificity for was also demonstrated in the solid-phase disk diffusion assay, and fungicidal activity confirmed in killing kinetics experiments. Broth macrodilution minimum inhibitory and minimum fungicidal concentrations for the most potent modification ranged from 0.0975-1.56 &mgr;g/ml and 0.0975-6.24 &mgr;g/ml respectively. The minimum inhibitory concentrations were nearly identical in the presence of human serum, but increased with lowered pH. Suitable dosage forms for use of the novel antifungals are also described.

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Fort McDowell, AZ, United States of America

Robin K Pettit