Potent and Non-toxic Molecules for Castration-resistant Prostate Cancer

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Researchers at Purdue University have developed potent synthetic small molecules with high potential as drugs against castration-resistant prostate cancer (CRPC) that are non-toxic in normal human cell lines. To address the heterogeneity of cellular pathways in cancer, the source of a cancer's ability to become resistant to therapy, the investigators designed these molecules using a machine learning approach that targets the protein network implicated in the disease state to guide compound selection and synthesis. The series of compounds developed inhibits proliferation of C4-2 androgen-insensitive human prostate adenocarcinoma cells with IC50 as low as 0.72 nM, and the compounds are much more potent than a control, the current steroidal CRPC drug, abiraterone (ABI). The most potent compound and other active leads were also more metabolically stable than ABI in a mouse liver microsome assay. Further, these compounds promise to combat metastasis; they slow migration of cells relative to untreated cells in both LNCaP and C4-2 cell lines.

-Addresses drug resistance

Potential Applications:
-Disease Research
-Cancer Therapy
Feb 28, 2020

Feb 28, 2019
United States
Purdue Office of Technology Commercialization
The Convergence Center
101 Foundry Drive, Suite 2500
West Lafayette, IN 47906

Phone: (765) 588-3475
Fax: (765) 463-3486
Email: otcip@prf.org