{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Yang M"],"funding":["Fundamental Research Funds for the Central Universities","Natural Science Foundation of Liaoning Province of China"],"pagination":["2551-2565"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9518286"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["37(1)"],"pubmed_abstract":["The molecular chaperone HSP90 plays an essential role in cancer occurrence and development. Therefore, it is an important target for the development of anticancer drugs. 1,3-Dibenzyl-2-aryl imidazolidine (<b>8)</b> is a previously reported inhibitor of HSP90; however, its anticancer activity is poor. In this work, chemical modification of <b>8</b> led to the discovery of 2,4-diarylimidazoles and 2,4-bis(benzyloxy)-5-arylpyrimidines as two types of novel HSP90 N-terminal inhibitors. <b>16l</b> and <b>22k</b> exhibited antiproliferative activity against multiple breast cancer cell lines with IC<sub>50</sub> values at the low micromolar level. <b>16l</b> and <b>22k</b> induced significant degradation of the client proteins AKT and ERK and a lower level of the heat shock response in comparison"],"journal":["Journal of enzyme inhibition and medicinal chemistry"],"pubmed_title":["Design, synthesis, biological evaluation and molecular docking study of 2,4-diarylimidazoles and 2,4-bis(benzyloxy)-5-arylpyrimidines as novel HSP90 N-terminal inhibitors."],"pmcid":["PMC9518286"],"funding_grant_id":["2020-MS-105","DUT20LK20; DUT22YG111"],"pubmed_authors":["Cheng C","Liu Y","Li Y","Shi M","Li C","Yang M","Yin L","Xue H"],"additional_accession":[]},"is_claimable":false,"name":"Design, synthesis, biological evaluation and molecular docking study of 2,4-diarylimidazoles and 2,4-bis(benzyloxy)-5-arylpyrimidines as novel HSP90 N-terminal inhibitors.","description":"The molecular chaperone HSP90 plays an essential role in cancer occurrence and development. Therefore, it is an important target for the development of anticancer drugs. 1,3-Dibenzyl-2-aryl imidazolidine (<b>8)</b> is a previously reported inhibitor of HSP90; however, its anticancer activity is poor. In this work, chemical modification of <b>8</b> led to the discovery of 2,4-diarylimidazoles and 2,4-bis(benzyloxy)-5-arylpyrimidines as two types of novel HSP90 N-terminal inhibitors. <b>16l</b> and <b>22k</b> exhibited antiproliferative activity against multiple breast cancer cell lines with IC<sub>50</sub> values at the low micromolar level. <b>16l</b> and <b>22k</b> induced significant degradation of the client proteins AKT and ERK and a lower level of the heat shock response in comparison","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Dec","modification":"2026-05-28T00:35:48.639Z","creation":"2025-04-19T05:15:14.09Z"},"accession":"S-EPMC9518286","cross_references":{"pubmed":["36120957"],"doi":["10.1080/14756366.2022.2124407"]}}