4.2 Article

Synthesis and Preliminary Biological Evaluation of New Heterocyclic Carboxamide Models

期刊

LETTERS IN DRUG DESIGN & DISCOVERY
卷 12, 期 5, 页码 417-429

出版社

BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1570180812666141201222527

关键词

Antifungal activity; cervical cancer cell; cytotoxicity; heterocyclic compounds; NMR; Synthesis

资金

  1. Deanship of Scientific Research at the University of Jordan
  2. Al-Zaytoonah University of Jordan
  3. Deutsche Forschungsgemeinschaft (DFG)

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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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