Affiliation:
1. Departamento de Química Instituto de Ciências Exatas Universidade Federal de Juiz de Fora Rua José Lourenço Kelmer, s/n, São Pedro Juiz de Fora Minas Gerais Brazil 36036-900
2. Instituto de Química Universidade Federal do Rio de Janeiro Rio de Janeiro Brazil
3. Departamento de Fisiologia e Biofísica Instituto de Ciências Biológicas Universidade Federal de Minas Gerais Av. Pres. Antônio Carlos, 6627 – Pampulha Belo Horizonte Brazil 31270-901
Abstract
AbstractBreast cancer is responsible for causing the death of women across various age groups worldwide. Alkylphosphocholines such as miltefosine are attractive for the chemical therapy of this neoplasm, but have disadvantages such as gastrointestinal problems, occasional hepatotoxicity and nephrotoxicity, and potential teratogenicity. In the present study, a series of 1‐alkyl‐1,2,3‐triazoles and organic salts were synthesized, as new non‐classical miltefosine bioisosteres, and biological studies were performed using human cells from the triple‐negative MDA‐MB‐231 breast cancer. The results showed that 1,2,3‐triazolic salts substituted with aliphatic chains of 16 carbons showed antitumor action, with half‐maximum inhibitory concentration values between 3.2 and 6.4 μM. Furthermore, clonogenic assays were conducted to predict the chemosensitivity of the most promising compounds, which supported the findings from the IC50 values, highlighting two main compounds with significant efficacy in reducing clonogenic survival compared to the control group. In conclusion, two 1,2,3‐triazolic salts exhibited promising antitumor effects and warrant further investigation for potential therapeutic use against the disease.
Funder
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
Conselho Nacional de Desenvolvimento Científico e Tecnológico
Fundação de Amparo à Pesquisa do Estado de Minas Gerais