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Chemical synthesis and antitumor activity of FR901464 and its analogs

*Abstract: Pitt Researchers Create Anticancer Molecule 10- to 100-times More Powerful Than Leading Treatment Investigators have discovered a unique total chemical synthesis of FR901464 and its analog. While the IC50 of FR901464 was known to be 1 nM against breast cancer cells (MCF-7 cells), it was discovered that this novel synthetic analog was far more potent than FR901464 against these cells. The inventors believe that these compounds inhibit RNA splicing and can also be used in diseases in which this is evident.Applications1. Cancer chemotherapeutics2. Potential new therapeutic targests for cancerAdvantages1. High antitumor activity, more potent than paclitaxol2. More concise total synthesis of FR901464 than those reported in the literature3. Exhibits antitumor activity at low concentrations (0.056-0.18 mg/kg)Non Provisional Patent Application Filednew Provisional Patent Applications filed

*Principal Investigation: Name: Brian Albert, Mr.
Department: Chemistry

Name: Kazunori Koide, Assistant Professor
Department: Chemistry

Name: Ananthapadmanabhan Sivaramakrishnan
Department:

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