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Article Abstract
CYT997 was discovered as a potent tubulin polymerization inhibitor possessing potent cytotoxic activity against a range of cancer cells. Details of SAR studies, pharmacokinetic investigations and synthesis of compounds leading to the discovery of CYT997 are reported.
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Identification and validation of microtubule depolymerizing agent, CYT997, as a potential drug candidate for hepatocellular carcinoma.
Liver Int
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Asian Liver Center, Department of Surgery, School of Medicine, Stanford, California, USA.
Background And Aims: Hepatocellular carcinoma (HCC) is a typically fatal malignancy with limited treatment options and poor survival rates, despite recent FDA approvals of newer treatment options. We aim to address this unmet need by using a proprietary computational drug discovery platform that identifies drug candidates with the potential to advance rapidly and successfully through preclinical studies.
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HBV Core Promoter Inhibition by Tubulin Polymerization Inhibitor (SRI-32007).
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Drug Discovery, Southern Research, Birmingham, AL, USA.
Approximately 257 million people chronically infected with hepatitis B virus (HBV) worldwide are at risk of developing hepatocellular carcinoma (HCC). However, despite the availability of potent nucleoside/tide inhibitors, currently there are no curative therapies for chronic HBV infections. To identify potential new antiviral molecules, a select group of compounds previously evaluated in clinical studies were tested against 12 different viruses.
View Article and Find Full Text PDFGateways to clinical trials.
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Thomson Reuters, Barcelona, Spain.
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View Article and Find Full Text PDFDiscovery of CYT997: a structurally novel orally active microtubule targeting agent.
Bioorg Med Chem Lett
August 2009
Cytopia Research Pty Ltd, Richmond, VIC 3121, Australia.
CYT997 was discovered as a potent tubulin polymerization inhibitor possessing potent cytotoxic activity against a range of cancer cells. Details of SAR studies, pharmacokinetic investigations and synthesis of compounds leading to the discovery of CYT997 are reported.
View Article and Find Full Text PDF