Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis and Preliminary Biological Evaluation of New Heterocyclic Carboxamide Models

Author(s): Kamal Sweidan, Jorn Engelmann, Walid Abu Rayyan, Dima Sabbah, Musa Abu Zarga, Dima Sabbah, Tariq Al-Qirim, Yusuf Al-Hiari, Ghassan Abu Sheikha, Ghassan Shattat.

Graphical Abstract:


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.

Keywords: Antifungal activity, cervical cancer cell, cytotoxicity, heterocyclic compounds, NMR, Synthesis.

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Article Details

VOLUME: 12
ISSUE: 5
Year: 2015
Page: [417 - 429]
Pages: 13
DOI: 10.2174/1570180812666141201222527
Price: $58