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

Molecular Design, Synthesis and Evaluation of 2,3-Diarylquinoxalines as Estrogen Receptor Ligands

Full text
Sangi, Diego P. [1, 2] ; Cominetti, Marcia R. [3] ; Becceneri, Amanda B. [3] ; Resende, Flavia A. [4] ; Varanda, Eliana A. [4] ; Montanari, Carlos A. [5] ; Paixao, Marcio W. [1] ; Correa, Arlene G. [1]
Total Authors: 8
[1] Univ Fed Sao Carlos, Dept Quim, BR-13565905 Sao Carlos, SP - Brazil
[2] Univ Fed Fluminense, Inst Ciencias Exatas, BR-27213145 Volta Redonda, RJ - Brazil
[3] Univ Fed Sao Carlos, Dept Gerontol, BR-13565905 Sao Carlos, SP - Brazil
[4] Univ Estadual Paulista, Fac Ciencias Farmaceut Araraquara, Dept Ciencias Biol, BR-14801902 Araraquara, SP - Brazil
[5] Univ Sao Paulo, Inst Quim Sao Carlos, BR-13566590 Sao - Brazil
Total Affiliations: 5
Document type: Journal article
Source: Medicinal Chemistry; v. 11, n. 8, p. 736-746, 2015.
Web of Science Citations: 0

Selective Estrogen Receptor Modulators (SERMs) are characteristically capable of being antagonist and agonist of estrogen receptors and, therefore, they can inhibit or stimulate estrogen production in different tissues. Aiming to contribute to the identification of new synthetic SERMs candidates, the basic skeletons of raloxifene and tamoxifene were used as model. Here of, a set of 2,3-diaryl-quinoxalines having 2-(piperidin-1-yl) ethanol in the side chain have been synthesized and evaluated against human mammary carcinoma cells estrogen dependent (MCF-7), as well as in recombinant yeast assays (RYA) expressing estrogen receptor. Compound LSPN332 showed 40% inhibition of MCF-7 and EC50= 290.6 mu M in RYA. The efficient synthesis of 2,3-diarylquinoxalines represents an excellent opportunity to identify new SERMs, and should therefore be of interest to the medicinal chemistry community. (AU)

FAPESP's process: 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery
Grantee:Glaucius Oliva
Support type: Research Grants - Research, Innovation and Dissemination Centers - RIDC
FAPESP's process: 11/01893-3 - Optimizing trypanosomatid agents by integration of in silico, calorimetry and cell-based assays
Grantee:Carlos Alberto Montanari
Support type: Regular Research Grants
FAPESP's process: 13/50680-8 - Quinoxaline derivatives as antiparasitic drugs: proof of concept
Grantee:Arlene Gonçalves Corrêa
Support type: Research Grants - Research Partnership for Technological Innovation - PITE