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  Synthesis and Preliminary Biological Evaluation of New Heterocyclic Carboxamide Models

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.

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Item Permalink: http://hdl.handle.net/11858/00-001M-0000-002A-4645-2 Version Permalink: http://hdl.handle.net/21.11116/0000-0000-B683-E
Genre: Journal Article

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 Creators:
Sweidan, K1, Author              
Engelmann, J1, Author              
Abu Rayyan, W, Author
Sabbah, D, Author
Abu Zarga, M, Author
Sabbah, D, Author
Al-Qirim, T, Author
Al-Hiari, Y, Author
Abu Sheikha, G, Author
Shattat, G, Author
Affiliations:
1Department High-Field Magnetic Resonance, Max Planck Institute for Biological Cybernetics, Max Planck Society, ou_1497796              

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 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.

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 Dates: 2015-06
 Publication Status: Published in print
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 Table of Contents: -
 Rev. Method: -
 Identifiers: DOI: 10.2174/1570180812666141201222527
BibTex Citekey: SweidanEASASAAAS2015
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Title: Letters in Drug Design Discovery
Source Genre: Journal
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Pages: - Volume / Issue: 12 (5) Sequence Number: - Start / End Page: 417 - 429 Identifier: -