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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

lavonoid Derivatives Targeting BCR-ABL Kinase: Semisynthesis, Molecular Dynamic Simulations and Enzymatic Inhibitio

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Author(s):
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Ribeiro, Rayssa [1] ; Eloy, Mariana A. [1] ; Francisco, Carla S. [2] ; Javarini, Clara L. [2] ; Ayusso, Gabriela M. [3] ; Fonseca, Victor Da Rocha [2] ; Romao, Wanderson [2] ; Regasini, Luis O. [3] ; Araujo, Sheila C. [4] ; Almeida, Michell O. [5] ; Honorio, Kathia M. [6, 4] ; de Paula, Heberth [7] ; Lacerda Jr, Valdemar ; Morais, Pedro A. B. [1]
Total Authors: 14
Affiliation:
[1] Univ Fed Espirito Santo, Programa Posgrad Agroquim, BR-29500000 Alegre, ES - Brazil
[2] Univ Fed Espirito Santo, Programa Posgrad Quim, BR-29075910 Vitoria, ES - Brazil
[3] Univ Estadual Paulista, Programa Posgrad Microbiol, BR-15054000 Sao Jose Do Rio Preto, SP - Brazil
[4] Fed Univ ABC, CCNH, BR-09210580 Santo Andre, SP - Brazil
[5] Inst Quim Sao Carlos USP, BR-13563120 Sao Carlos, SP - Brazil
[6] Univ Sao Paulo, Escola Artes Ciencias & Humanidades, BR-03828000 Sao Paulo, SP - Brazil
[7] Univ Fed Espirito Santo, Ctr Ciencias Exatas Nat & Saude, BR-29500000 Alegre, ES - Brazil
Total Affiliations: 7
Document type: Journal article
Source: CURRENT TOPICS IN MEDICINAL CHEMISTRY; v. 21, n. 22, p. 1999-2017, 2021.
Web of Science Citations: 2
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 pharmacotherapeutics. 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 Microwave-assisted click reaction. Chemical structures were finely characterized through IR, H-1 and C-13 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. (AU)

FAPESP's process: 17/10118-0 - Study and application of electrochemical technology for the analysis and degradation of endocrine interferents: materials, sensors, processes and scientific dissemination
Grantee:Marcos Roberto de Vasconcelos Lanza
Support Opportunities: Research Projects - Thematic Grants
FAPESP's process: 16/24524-7 - STRUCTURAL ANALYSIS AND MOLECULAR MODELING STUDIES FOR NATURAL AND SYNTHETIC LIGANTS RELATED TO NEGLECTED DISEASES
Grantee:Kathia Maria Honorio
Support Opportunities: Regular Research Grants