Design, Synthesis, And Evaluation Of Heat Shock Protein 90 Inhibitors In Human Breast Cancer And Its Metastasis.

Design, Synthesis, And Evaluation Of Heat Shock Protein 90 Inhibitors In Human Breast Cancer And Its Metastasis.
Curr Pharm Biotechnol. 2016 Oct 31;
Authors: Gumus M, Özgür A, Tutar L, Disli A, Koca İ, Tutar Y
Abstract
In the present study, a series of benzodiazepine derivatives were designed and synthesized as novel heat shock protein 90 (Hsp90) inhibitor for target specific cancer treatment. Their anticancer activities were determined by XTT cell proliferation assay against human breast cancer cell line (MCF-7). Also, we investigated the antiangiogenic effects of the compounds on human vascular endothelium (HUVEC) cell line. In order to determine the anti-proliferative mechanism of the compounds, in silico molecular docking studies were performed between Hsp90 ATPase domain and benzodiazepine derivatives. Further, these compounds interfere with ATPase function of Hsp90. Expression analysis of known cancer drug target genes suggest that the benzodiazepine derivatives have remarkable anticancer activity and can serve as Hsp90 inhibitors.
PMID: 27804852 [PubMed - as supplied by publisher]

Source: Current Pharmaceutical Biotechnology - October 30, 2016 Category: Biotechnology Authors: Gumus M, Özgür A, Tutar L, Disli A, Koca İ, Tutar Y Tags: Curr Pharm Biotechnol Source Type: research