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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.)

Antiproliferative and pro-apoptotic activities of 2 `- and 4 `-aminochalcones against tumor canine cells

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Author(s):
Santos, Mariana B. ; Pinhanelli, Vitor C. ; Garcia, Mayara A. R. ; Silva, Gabriel ; Baek, Seung J. ; Franca, Suzelei C. ; Fachin, Ana L. ; Marins, Mozart ; Regasini, Luis O.
Total Authors: 9
Document type: Journal article
Source: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY; v. 138, p. 884-889, SEP 29 2017.
Web of Science Citations: 9
Abstract

In the present study, a series of 2'- and 4'-aminochalcones were synthesized and their antiproliferative activity against a canine malignant histiocytic cell line (DH82) was evaluated. Particularly aminochalcones with a hydrophobic substituent on ring B proved to be potent antiproliferative agents. Among these compounds, aminochalcones 3, 4 and 11 inhibited the growth of DH82 cells, with IC50 values of 34.4, 31.4 and 38.2 mu M, respectively, and were three times more potent than etoposide (IC50 = 95.5 mu M). The selected chalcones induced death through apoptosis rather than necrosis in DH82 and non-tumorigenic Madin-Darby canine kidney cells (MDCK). Further experiments suggested that the aminochalcones interfere with the regulation of oncogenesitumor suppressor genes. Aminochalcone 11 inhibited transcription of the TOP011 alpha and TP53 genes and aminochalcone 4 down-regulated Sp1 protein expression in a concentration-dependent manner. (C) 2017 Elsevier Masson SAS. All rights reserved. (AU)

FAPESP's process: 14/18330-0 - Synthesis and biological evaluation of curcumin-cinnamaldehyde hybrids as bacterial cell division inhibitors
Grantee:Luis Octávio Regasini
Support type: Regular Research Grants
FAPESP's process: 14/15307-7 - Molecular analysis of the response of human and canine tumor strain lines to the flavonoid trans-chalcone
Grantee:Mozart de Azevedo Marins
Support type: Regular Research Grants