| Full text | |
| Author(s): |
da Silva, Rafaela Binda
;
Borlot, Jessica Rodrigues Pereira Oliveira
;
Santos, Carolina Rosa
;
Rodrigues e Oliveira, Ligia
;
de Almeida, Larissa Costa
;
Costa-Lotufo, Leticia Veras
;
Regasini, Luis Octavio
;
Kitagawa, Rodrigo Rezende
;
de Medeiros, Edna Faria
;
Borges, Warley de Souza
Total Authors: 10
|
| Document type: | Journal article |
| Source: | CHEMISTRY & BIODIVERSITY; v. 21, n. 11, p. 7-pg., 2024-10-03. |
| Abstract | |
Chalcones are a group of molecules with recognized biological potential against many diseases, including cancer. Thus, studies on this structure and derivatives have become an attractive chemical strategy to optimize their observed biological activities. One of the synthetic routes used to obtain chalcone derivatives is esterification using either commercial acid chlorides or carboxylic acids. This work focuses on preparing chalcone derivatives and investigating their biological potential against cancer cells. Compound 3'-hydroxychalcone (1) was synthetized by Claisen-Schmidt condensation followed by esterification of the 3'-OH, resulting in eight compounds named 1a-b and 2a-f. All structures were confirmed by 1H and 13C NMR and FT-IR, and cytotoxicity was evaluated in the HCT 116 (colon adenocarcinoma), MCF-7 (breast adenocarcinoma), and CCD-18Co (nontumoral colon fibroblasts) cell lines. Chalcone derivatives were generally more active toward the colon cancer cell line, and 1a and 2b were selected for IC50 determination, presenting IC50 values of approximately 10 mu M in HCT 116 cells and above 20 mu M in both MCF7 and CDC-18-Co cells, suggesting moderate selectivity. Additionally, we tested compounds 1a and 2b in combination with doxorubicin, but they did not act synergistically with this anthracycline. In conclusion, considering these compounds obtained by the esterification reaction, 1a and 2d showed better results against cytotoxic cells. image (AU) | |
| FAPESP's process: | 15/17177-6 - Integrative approach on the sustainable prospection of marine natural products: from diversity to anticancer compounds |
| Grantee: | Leticia Veras Costa Lotufo |
| Support Opportunities: | BIOTA-FAPESP Program - Thematic Grants |
| FAPESP's process: | 14/50926-0 - INCT 2014: biodiversity and natural products |
| Grantee: | Vanderlan da Silva Bolzani |
| Support Opportunities: | BIOTA-FAPESP Program - Thematic Grants |