Abstract
To design new compounds suitable as starting points for anticancer drug development, we have synthesized a novel series of benzoxazoles with pharmaceutically advantageous piperazine and fluorine moieties attached to them. The newly synthesized benzoxazoles and their corresponding precursors were evaluated for cytotoxicity on human A-549 lung carcinoma cells and non-cancer HepaRG hepatocyes. Some of these new benzoxazoles show potential anticancer activity, while two of the intermediates show lung cancer selective properties at low concentrations where healthy cells are unaffected, indicating a selectivity window for anticancer compounds.
Highlights
Despite all the progress in biomedical research, cancer remains a leading cause of death worldwide.many efforts have been made to find new therapeutic agents that could potentially improve cancer therapy by using more selective and less toxic drugs.Heterocyclic compounds are considered to be the most interesting drug-based structures in medicinal chemistry due to their widespread presence in lead compounds
As a part of our ongoing research in developing new potentially bioactive heterocyclic compounds, this study describes the synthesis of new 4-fluoro-5-(substituted phenylheterocyclic compounds, this study describes the synthesis of new 4-fluoro-5-(substituted piperazin-1-yl)-2-nitro-phenoles (6) and their corresponding 5-fluoro-6-(substituted phenylphenyl-piperazin-1-yl)-2-nitro-phenoles (6) and their corresponding 5-fluoro-6-(substituted piperazin-1-yl)-benzoxazoles (7) functionalized with both piperazine and fluorine moieties
A novel series of 5-fluoro-2-methyl-6-(4-arylpiperazin-1-yl)benzoxazoles (7a–j) incorporating both fluorine and piperazine were prepared in good yields
Summary
Despite all the progress in biomedical research, cancer remains a leading cause of death worldwide.many efforts have been made to find new therapeutic agents that could potentially improve cancer therapy by using more selective and less toxic drugs.Heterocyclic compounds are considered to be the most interesting drug-based structures in medicinal chemistry due to their widespread presence in lead compounds. Despite all the progress in biomedical research, cancer remains a leading cause of death worldwide. Many efforts have been made to find new therapeutic agents that could potentially improve cancer therapy by using more selective and less toxic drugs. Benzoxazoles have received much attention in recent years because of their broad spectrum of biological activities. Recent studies show that several benzoxazole analogues exhibit a number of biological activities including anticancer [1], antifungal [2], antituberculosis [3], mPGES-1 inhibitor [4], 5-HT receptor antagonist [5], CETP inhibitor [6], and antiplasmodial [7] activities. Broad therapeutic spectrum compounds intrinsically possess a certain amount of cytotoxicity
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