Fluorescent CDK Inhibitors for Treatment of Cancer
Compounds of the invention demonstrate higher % inhibition of CDK2/A and CDK2/E than known CDK2 inhibitor, seliciclibA fluorescent label allow these compounds to be used as both a therapeutic to treat cancer and a diagnostic to detect cancerous cells and monitor treatmentCell growth inhibition potency (IC50) in certain cancer cell lines is superior to known CDK inhibitors purvanalol and seliciclib
The invention describes promising new fluorescent small molecule pharmaceutical leads for the treatment of cancer by inhibition of cyclin dependant kinase (CDK). The novel compounds are more potent than known CDK inhibitors, purvalanols A and B as well as phase II clinical drug candidate, roscovitine (seliciclib). These compounds are especially potent inhibitors of CDK2 isoforms and effectively arrest tumor cells in the G2/M phase. These new compounds may be an effective new tool for not only for treating, but also diagnosing cancer and monitoring cancer therapy.
美國
