Synthesis of novel nicotinohydrazide and (1,3,4-oxadiazol-2-yl)-6-(trifluoromethyl)pyridine derivatives as potential anticancer agents

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4829-4831. doi: 10.1016/j.bmcl.2016.08.020. Epub 2016 Aug 10.

Abstract

A series of novel nicotinohydrazide derivatives 6a-g and 1,3,4-oxadiazole functionalized pyridine derivatives 7a-k and 8a-d were prepared in series of steps. All the compounds were screened for cytotoxicity against HeLa (cervical), DU145 (prostate), HepG2 (liver) and MBA-MB-231 (breast) human cancer cell lines. Compounds 6h, 6i, 7d, 7h, 7i and 8b which showed promising cytotoxicity at <15μM concentration have been identified. Further optimization of the structure is underway to identify a lead compound.

Keywords: 1,3,4-Oxadiazole; Anticancer agents; Cyclization; Human cancer cell lines; Nicotinohydrazide.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis*
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Humans
  • Pyridines / chemical synthesis*
  • Pyridines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Pyridines