Boronic-Chalcone Analogs as MDM2 Inhibitor

A series of boronic-chalcone derivatives were synthesized and tested for antitumor activity against human breast cancer cell lines. The results show the boronic-chalcones are more toxic to breast cancer cells compared to normal breast cells than other known chalcones. Description (Set) Proposed Use (Set) A class of anticancer agents such as chalcones has shown promising therapeutic efficacy for the management of human cancers. Recent studies have shown that anticancer agents such as chalcones induce apoptosis in variety of cell types, including breast cancers. Biochemical experiments showed that these compounds can disrupt the MDM2/p53 protein complex, releasing p53 from both the p53/MDM2 and DNA-bound p53/MDM2 complexes. However, these carboxylic acid analogs of chalcone are equally toxic to normal cells. In this proposal, a boronic-chalcone strategy is outlined that will overcome this limitation Patent (Set) WO 03/106384

Inventor(s): Khan, Saeed R.

Type of Offer: Licensing

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