Synthesis and Evaluation of Simplified Cruentaren A Analogues

Autor: Xiaozheng Dou, Bhargav A. Patel, Terin D’Amico, Chitra Subramanian, Eric Cousineau, Yi Yi, Mark Cohen, Brian S. J. Blagg
Rok vydání: 2022
Předmět:
Zdroj: The Journal of Organic Chemistry. 87:9940-9956
ISSN: 1520-6904
0022-3263
DOI: 10.1021/acs.joc.2c00948
Popis: The 90 kDa heat shock protein (Hsp90) belongs to a group of molecular chaperones that regulate homeostasis via the folding of nascent polypeptides into their biologically active proteins, many of which are involved in cancer development and progression. As a result, inhibition of Hsp90 is an exciting area of research for the treatment of cancer. However, most of the 18 Hsp90 N-terminal inhibitors evaluated in clinical trials exhibited deleterious side effects and toxicities. Cruentaren A is a natural product that manifests potent anticancer activity against various human cancer cell lines via disruption of interactions between Hsp90α and F
Databáze: OpenAIRE