Synthesis and Anticancer Study of Novel 4H-Chromen Derivatives

Anticancer Agents Med Chem. 2017;17(8):1070-1083. doi: 10.2174/1871520615666160504094945.

Abstract

Objective/method: A series of 4H-chromen-4-one derivatives (A1-A16) have been designed and synthesized, and they were screened for BRAF kinase inhibitory activity. Furthermore, their biological activities were evaluated in vitro.

Result: Compounds A03 and A10 displayed the most potent antiproliferative activity against human osteosarcoma cell line (U2OS) and A16 displayed the most potent antiproliferative activity against human melanoma cancer cell line (A375) in vitro, which was valuable to study further.

Keywords: 4H-Chromen-4-one; BRAF (V600E) kinase; anticancer activity; design; in vitro; synthesis.

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Benzopyrans / chemical synthesis
  • Benzopyrans / chemistry
  • Benzopyrans / pharmacology*
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Antineoplastic Agents
  • Benzopyrans