Synthesis and in vitro cytotoxic evaluation of 3-alkylpyridine alkaloids analogs linked to a thiosemicarbazone group.

• Autor(a) principal: Moreira, Paulo Otávio Lourenço
• Data de Publicação: 2015
• Outros Autores: Barbosa, Camila de Souza, da Silva, Karen Cipriano, Marques Neves Gonçalves, Alessandra Mirtes, Silva, Luciana Maria, Viana, Gustavo Henrique Ribeiro, Varotti, Fernando de Pilla
• Tipo de documento: Artigo
• Idioma: por
• Título da fonte: Revista Científica da Faculdade de Medicina de Campos
• Texto Completo: https://www.fmc.br/ojs/index.php/RCFMC/article/view/40

Cancer remains a devastating worldwide disease. One characteristic of cancer is the rapid growth of abnormal cells, invading adjacent regions of the body and spreading to other organs. The increase number of cancer cases has driven the search for new antitumor compounds. The goal of chemotherapy is to eliminate cancer cells, preserving the health ones. However, most chemotherapeutic agents has a non-specific action, killing both normal and malignant cells. In this context, compounds with dual action planned by molecular hybridization has a great therapeutic interest. In this work, five new synthetic compounds designed by molecular hybridization of analogs of 3-Alkylpyridine alkaloids covalently linked to a thiosemicarbazone group were tested in vitro against two human tumor cell lines: colon cancer (RKO-AS-45-1) and cervical malignant (HeLa). Cytotoxicity assays were performed by MTT colorimetric method. Compound 3d was the most active of the serie for HeLa (IC50 = 19,48uM) and RKO-AS-45-1 strain (IC50 = 22,28uM). Moreover, it was possible to deduce a correlation between the cytotoxic activity and the side chain´s size of hybrid compounds. In conclusion, the synthesis of hybrid compounds obtained by classical synthetic methods, generating clean products with good yields, is a promising strategy for the development of new antitumor agents.