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Synthesis and Preliminary Biological Evaluation of New Heterocyclic Carboxamide Models

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Sweidan,  K
Department High-Field Magnetic Resonance, Max Planck Institute for Biological Cybernetics, Max Planck Society;

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Engelmann,  J
Department High-Field Magnetic Resonance, Max Planck Institute for Biological Cybernetics, Max Planck Society;

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Citation

Sweidan, K., Engelmann, J., Abu Rayyan, W., Sabbah, D., Abu Zarga, M., Sabbah, D., et al. (2015). Synthesis and Preliminary Biological Evaluation of New Heterocyclic Carboxamide Models. Letters in Drug Design Discovery, 12(5), 417-429. doi:10.2174/1570180812666141201222527.


Cite as: http://hdl.handle.net/11858/00-001M-0000-002A-4645-2
Abstract
The heterocyclic system is a promising core nucleus in many bioactive compounds. This work describes our effort to synthesize and characterize a set of new biphenyl, benzofuran and benzothiophene carboxamide derivatives. Our biological studies showed that compounds 10 and 17 have antifungal activity against C. galabrate more potent than fluconazole compounds 9, 10, and 17 exerted cytotoxic activities in immortalized embryonic mouse fibroblast cells (3T3) and a human cervical cancer cell line (HeLa); in particular, the cyclic amidine derivative 17 showed selective toxicity against HeLa. This study showed that the tested compounds have the potential to be useful as antitumor drugs after further optimization.