Abstract

GUTIERREZ, Joyce E. et al. Synthesis and antiproliferative activity of a mixture (⁺/_) 7-chloro-(4-thioalkylquinoline) derivatives. Inducing apoptosis and DNA/RNA damage. Rev.Colomb.Quim. [online]. 2023, vol.52, n.1, pp.10-18.  Epub Mar 02, 2024. ISSN 0120-2804.  https://doi.org/10.15446/rev.colomb.quim.v52n1.110787.

After cardiovascular diseases, cancer, a non-communicable pathology, has been considered the second cause of death each year globally and as the most important barrier to increasing life expectancy in the 21st century. Advances of great relevance have been made in its prevention and treatment, however, there is still a long way to go to achieve an effective treatment for each type of cancer. This paper describes approaches to reposition and synthesis of hybrid molecules with potential antineoplastic activity. To obtain the key intermediate aldehyde, the Dess-Martin oxidation methodology was used, which was coupled with the corresponding ketones using LDA. The final hybrid compounds were obtained as a racemic mixture. The in vitro antiproli-ferative activity of the final compounds was evaluated against eight cell lines derived from human solid tumors, and four non-cancerous cell lines. The compound 11d turned out to be the most effective and with the highest safety index. The results suggested that these compounds could block the cell cycle and induce apoptosis and death in CCRF-CEM cells in a dose-dependent manner in vitro.

Keywords : cancer; cell cycle; sulfanyl derivatives; racemic mixture.

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