Mitochondrial-targeted Hsp90 C-terminal inhibitors manifest anti-proliferative activity |
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| Institution: | 1. Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, West Lafayette, IN 47907, USA;2. Department of Comparative Pathobiology, College of Veterinary Medicine, Purdue University, West Lafayette, IN 47907, USA;3. Purdue University Libraries Purdue University, West Lafayette, IN 47907, USA;4. Purdue University Center for Cancer Research, Purdue University, West Lafayette, IN 47907, USA |
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| Abstract: | The development of C-terminal heat shock protein 90 kDa (Hsp90) inhibitors has emerged as a potential treatment for cancer. Similarly, small molecules that target the mitochondria have proven to be efficacious towards cancer, as the reprogramming of mitochondrial function is often associated with oncogenic transformation. Herein, we report the development of triphenylphosphonium (TPP)-conjugated Hsp90 C-terminal inhibitors, their anti-proliferative activity, and accumulation in the mitochondria. In general, TPP-conjugated Hsp90 C-terminal inhibitors were found to manifest increased activity against various cancer cell lines when compared to the parent compounds. |
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| Keywords: | Hsp90 C-terminal inhibitor Novobiocin Triphenylphosphonium Anticancer |
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