| Full text | |
| Author(s): |
Tezuka, Daiane Yukie
[1, 2]
;
de Albuquerque, Sergio
[3]
;
Montanari, Carlos Alberto
[1]
;
Leitao, Andrei
[1, 2]
Total Authors: 4
|
| Affiliation: | [1] Univ Sao Paulo, Med Chem Grp NEQUIMED, Sao Carlos Inst Chem IQSC, Sao Paulo - Brazil
[2] Programa Posgrad Bioengn EESC USP, Sao Paulo - Brazil
[3] Univ Sao Paulo FCFRP USP, Lab Parasitol, Fac Ciencias Farmaceut Ribeirao Preto, Sao Paulo - Brazil
Total Affiliations: 3
|
| Document type: | Journal article |
| Source: | LETTERS IN DRUG DESIGN & DISCOVERY; v. 17, n. 7, p. 867-872, 2020. |
| Web of Science Citations: | 0 |
| Abstract | |
Background: Compounds previously studied as anticancer were screened against trypomastigotes to access the bioactivity. The epimastigote form of Trypanosoma cruzi Y strain and the promastigote form of Leishmania amazonensis and Leishmania infantum were used in this work. Methods: Cell-based assays were performed to access the bioactivity of the compounds using MTT and the flow cytometry methods. Results: Neq0438, Neq0474 and Neq0440 had the highest potency, with EC50 of 39 mu M (L. amazonensis), 52 mu M (T. cruzi) and 81 mu M (T. cruzi), respectively. These molecules were inactive for Balb/C fibroblast cell line at concentrations above 250 mu M, showing selectivity for the parasites. Conclusion: This is the first report that demonstrates antiparasitic activity for the 2-aminopyridine scaffold, with cross-activity against cancer cells. (AU) | |
| FAPESP's process: | 13/18009-4 - Molecular design, synthesis and trypanocidal activity of cruzain reversible covalent inhibitors |
| Grantee: | Carlos Alberto Montanari |
| Support Opportunities: | Research Projects - Thematic Grants |
| FAPESP's process: | 18/15904-6 - Characterization of cysteine protease inhibitors with antineoplastic activity by in silico and cell-based assays coupled with chemical analyses |
| Grantee: | Andrei Leitão |
| Support Opportunities: | Regular Research Grants |