Presentation Title

Reinvestigation of Mycothiazole and Analogs Reveals Picomolar Potency Against Tumor Cell Lines

Location

Guzman 202, Dominican University of California

Start Date

4-17-2019 4:00 PM

End Date

4-17-2019 5:00 PM

Department

Natural Sciences and Mathematics

Student Type

Undergraduate

Faculty Mentor(s)

Tyler Johnson, PhD

Presentation Format

Poster Presentation

Abstract/Description

REINVESTIGATION OF MYCOTHIAZOLE AND ANALOGS REVEALS PICOMOLAR POTENCY AGAINST TUMOR CELL LINES

Joseph D. Morris,1 Colon V. Cook,1 Nicole L. McIntosh,1 Marcos A. Ogarrio,1 Taylor Garcia,1 Lauren Persi,1 Phillip Crews,3 Frederick A. Valeriote,2 and Tyler A. Johnson.1

1Department of Natural Sciences and Mathematics, Dominican University of California, San Rafael, CA 94901 USA, 2Department of Internal Medicine, Division of Hematology and Oncology, Henry Ford Hospital, Detroit, MI 48202, 3Department of Chemistry and Biochemistry,University ofCalifornia,Santa Cruz,CA95064

Pancreatic cancer is one of the most difficult cancers to treat as there are no effective frontline therapeutics. Mycothiazole (1) has shown low nanomolar potency (IC50 ~3-5 nM) and selectivity against a variety of tumor cell lines. Recently, we investigated 1 in an effort to explore its structural activity relationship (SAR) against pancreatic (PANC-1) cancer cell lines and made a remarkable discovery. Upon purification of 1, unless it is: a) stored in an aprotic solvent, b) dried under nitrogen, and c) stored under argon, it decomposes. After retesting a sample of 1 that was prepared using a-c, we discovered a 20-30 fold increase in the potency of 1 against PANC-1 cancer cell lines (IC50 ~140 pM). We have prepared two other analogs of 1, which include: 8-O-acetylmycothiazole (2) and 8-Oxomycothiazole (3) and the SAR data results of these compounds 1-3 against PANC-1 cancer cell lines are reported here in.

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Apr 17th, 4:00 PM Apr 17th, 5:00 PM

Reinvestigation of Mycothiazole and Analogs Reveals Picomolar Potency Against Tumor Cell Lines

Guzman 202, Dominican University of California

REINVESTIGATION OF MYCOTHIAZOLE AND ANALOGS REVEALS PICOMOLAR POTENCY AGAINST TUMOR CELL LINES

Joseph D. Morris,1 Colon V. Cook,1 Nicole L. McIntosh,1 Marcos A. Ogarrio,1 Taylor Garcia,1 Lauren Persi,1 Phillip Crews,3 Frederick A. Valeriote,2 and Tyler A. Johnson.1

1Department of Natural Sciences and Mathematics, Dominican University of California, San Rafael, CA 94901 USA, 2Department of Internal Medicine, Division of Hematology and Oncology, Henry Ford Hospital, Detroit, MI 48202, 3Department of Chemistry and Biochemistry,University ofCalifornia,Santa Cruz,CA95064

Pancreatic cancer is one of the most difficult cancers to treat as there are no effective frontline therapeutics. Mycothiazole (1) has shown low nanomolar potency (IC50 ~3-5 nM) and selectivity against a variety of tumor cell lines. Recently, we investigated 1 in an effort to explore its structural activity relationship (SAR) against pancreatic (PANC-1) cancer cell lines and made a remarkable discovery. Upon purification of 1, unless it is: a) stored in an aprotic solvent, b) dried under nitrogen, and c) stored under argon, it decomposes. After retesting a sample of 1 that was prepared using a-c, we discovered a 20-30 fold increase in the potency of 1 against PANC-1 cancer cell lines (IC50 ~140 pM). We have prepared two other analogs of 1, which include: 8-O-acetylmycothiazole (2) and 8-Oxomycothiazole (3) and the SAR data results of these compounds 1-3 against PANC-1 cancer cell lines are reported here in.