15864-27-4Relevant academic research and scientific papers
From Bacteria to Cancer: A Benzothiazole-Based DNA Gyrase B Inhibitor Redesigned for Hsp90 C-Terminal Inhibition
Pugh, Kyler W.,Zhang, Zheng,Wang, Jian,Xu, Xiuzhi,Munthali, Vitumbiko,Zuo, Ang,Blagg, Brian S. J.
, p. 1535 - 1538 (2020)
Heat shock protein 90 (Hsp90) is a molecular chaperone that is responsible for the folding and maturation of client proteins that are associated with all ten hallmarks of cancer. Hsp90 N-terminal pan inhibitors have experienced unfavorable results in clinical trials due to induction of the heat shock response (HSR), among other concerns. Novobiocin, a well characterized DNA gyrase B inhibitor, was identified as the first Hsp90 C-terminal inhibitor that manifested anticancer effects without induction of the HSR. In this letter, a library of Hsp90 C-terminal inhibitors derived from a benzothiazole-based scaffold, known to inhibit DNA gyrase B, was designed, synthesized, and evaluated. Several compounds were found to manifest low micromolar activity against both MCF-7 and SKBr3 breast cancer cell lines via Hsp90 C-terminal inhibition.
Novel hydrazone derivatives comprising aryl or heteroaryl group substituted at terminal amine and use thereof
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Paragraph 1193; 1195-1197, (2020/08/28)
The present invention relates to novel hydrazone derivatives with an aryl or heteroaryl group substituted at a terminal amine group thereof and a use thereof.
