Synthesis and evaluation of c-Src kinase inhibitory activity of pyridin-2(1H)-one derivatives

Karam Chand, Suchita Prasad, Rakesh K. Tiwari, Amir N. Shirazi, Sumit Kumar, Keykavous Parang, Sunil K. Sharma

Research output: Contribution to journalArticlepeer-review

13 Scopus citations


Src kinase, a prototype member of the Src family of kinases (SFKs), is over-expressed in various human tumors, and has become a target for anticancer drug design. In this perspective, a series of eighteen 2-pyridone derivatives were synthesized and evaluated for their c-Src kinase inhibitory activity. Among them, eight compounds exhibited c-Src kinase inhibitory activity with IC 50 value of less than 25 μM. Compound 1-[2-(dimethylamino)ethyl]- 5-(2-hydroxy-4-methoxybenzoyl)pyridin-2(1H)-one (36) exhibited the highest c-Src kinase inhibition with an IC50 value of 12.5 μM. Furthermore, the kinase inhibitory activity of compound 36 was studied against EGFR, MAPK and PDK, however no significant activity was observed at the highest tested concentration (300 μM). These results provide insights for further optimization of this scaffold for designing the next generation of 2-pyridone derivatives as candidate Src kinase inhibitors.

Original languageEnglish (US)
Pages (from-to)75-82
Number of pages8
JournalBioorganic Chemistry
StatePublished - 2014
Externally publishedYes


  • c-Src kinase inhibition
  • Chromone
  • Pyridin-2(1H)-one
  • Synthesis

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Medicine(all)


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