Cyclic Peptides and Cyclic Depsipeptides with Antitumor Activity (24095/23053/22081)

A novel family of peptide compounds with enhanced anti-proliferative activity has been synthesized at Northwestern University. These peptide inhibitors have anticancer activity exceeding that of two known growth inhibitors. This newly identified family of compounds has been tested in human prostate, human breast cancer, melanoma and human colon cancer cell lines.

ADVANTAGE: A novel class of peptide molecules that inhibit cell growth across a variety of human cancer cell lines has been created.

SUMMARY: Several isolated marine natural products exhibit cytotoxicity against a variety of cancer cell lines. Sansalvamide A and Scytalidamide A are two such natural products that show cytotoxic activity. Synthesis of cyclic peptide analogs of these natural materials afforded new compounds having anticancer activity greater than that of these two known growth inhibitors. Reduced cell proliferation versus Sansalvamide A and Scytalidamide A was observed in PC-3 human prostate cancer, MDA‑MB231 breast cancer, and WM115 melanoma cell lines when treated with these new proliferation inhibitors (Table). Furthermore, an 80-fold reduction in effective dosage was also observed in HCT-116 human colon carcinoma bioassay versus Sansalvamide A. Recent data has shown analogs with greater efficacy (references). An efficient solid phase synthesis of the cyclic peptides has been developed providing a wide range of potential cancer inhibiting compounds

A series of compounds has been prepared and tested in vitro across several human cancer cell lines. The compounds are attractive candidates for further analysis and development. A patent application has been filed and Northwestern University seeks to develop the discovery.

Journal of Medicinal Chemistry, 2005, Vol. 48, No. 10, 3630-38 Biochemical & Biophysical Research Communications 340 (2006) 1224-1228

Type of Offer: Licensing

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