dc.contributor | Universidade Federal do Espírito Santo (UFES) | |
dc.contributor | Universidade Estadual Paulista (UNESP) | |
dc.contributor | Federal University of ABC | |
dc.contributor | Universidade de São Paulo (USP) | |
dc.date.accessioned | 2022-04-28T19:48:50Z | |
dc.date.accessioned | 2022-12-20T01:33:16Z | |
dc.date.available | 2022-04-28T19:48:50Z | |
dc.date.available | 2022-12-20T01:33:16Z | |
dc.date.created | 2022-04-28T19:48:50Z | |
dc.date.issued | 2021-09-01 | |
dc.identifier | Current Topics in Medicinal Chemistry, v. 21, n. 22, p. 1999-2017, 2021. | |
dc.identifier | 1873-4294 | |
dc.identifier | 1568-0266 | |
dc.identifier | http://hdl.handle.net/11449/223132 | |
dc.identifier | 10.2174/1568026621666210705170047 | |
dc.identifier | 2-s2.0-85122028445 | |
dc.identifier.uri | https://repositorioslatinoamericanos.uchile.cl/handle/2250/5403261 | |
dc.description.abstract | Background: Natural products have been universally approached in the research of novel trends useful to detail the essential paths of the life sciences and as a strategy for pharmacothera-peutics. Objective: This work focuses on further modification to the 6-hydroxy-flavanone building block aiming to obtain improved BCR-ABL kinase inhibitors. Methods: Ether derivatives were obtained from Williamson synthesis and triazole from Mi-crowave-assisted click reaction. Chemical structures were finely characterized through IR,1H and13 C NMR and HRMS. They were tested for their inhibitory activity against BCR-ABL kinase. Results: Two inhibitors bearing a triazole ring as a pharmacophoric bridge demonstrated the strongest kinase inhibition at IC50 value of 364 nM (compound 3j) and 275 nM (compound 3k). Conclusion: 6-hydroxy-flavanone skeleton can be considered as a promising core for BCR-ABL kinase inhibitors. | |
dc.language | eng | |
dc.relation | Current Topics in Medicinal Chemistry | |
dc.source | Scopus | |
dc.subject | 6-hydroxy-flavanone skeleton | |
dc.subject | BCR-ABL kinase inhibitors | |
dc.subject | Chronic myeloid leukemia | |
dc.subject | Semisynthesis | |
dc.subject | Triazole | |
dc.subject | Williamson synthesis | |
dc.title | Flavonoid Derivatives Targeting BCR-ABL Kinase: Semisynthesis, Molecular Dynamic Simulations and Enzymatic Inhibition | |
dc.type | Artículos de revistas | |