| Full text | |
| 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. 6-pg., 2017-09-29. |
| 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: | 14/15307-7 - Molecular analysis of the response of human and canine tumor strain lines to the flavonoid trans-chalcone |
| Grantee: | Mozart de Azevedo Marins |
| Support Opportunities: | Regular Research Grants |
| FAPESP's process: | 14/18330-0 - Synthesis and biological evaluation of curcumin-cinnamaldehyde hybrids as bacterial cell division inhibitors |
| Grantee: | Luis Octávio Regasini |
| Support Opportunities: | Regular Research Grants |