Discovery of 2-pyridineformamide thiosemicarbazones as potent antiausterity agents

Bioorg Med Chem Lett. 2014 Jan 15;24(2):458-61. doi: 10.1016/j.bmcl.2013.12.044. Epub 2013 Dec 18.

Abstract

Series of 2-pyridineformamide thiosemicarbazones were synthesized. Their preferential cytotoxicity in nutrient deprived medium (NDM) was evaluated using PANC-1 human pancreatic cancer cells by employing an antiausterity strategy. 2-Pyridineformamide thiosemicarbazones induced apoptosis and exhibited preferential cytotoxic activity toward PANC-1 cells in NDM, with potencies in the submicromolar range. These compounds are potential candidates for the development of therapeutics against pancreatic cancer.

Keywords: 2-Pyridineformamide thiosemicarbazones; Antiausterity agents; Apoptosis; Nutrition starvation; Pancreatic cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / therapeutic use
  • Cell Line, Tumor
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor / methods
  • Formamides / chemistry*
  • Formamides / therapeutic use
  • Humans
  • Pancreatic Neoplasms / drug therapy*
  • Pancreatic Neoplasms / pathology
  • Pyridines / chemistry*
  • Pyridines / therapeutic use
  • Thiosemicarbazones / chemistry*
  • Thiosemicarbazones / therapeutic use

Substances

  • 2-pyridineformamide
  • Antineoplastic Agents
  • Formamides
  • Pyridines
  • Thiosemicarbazones