Synthesis and Anticancer Activity of 3-(Substituted Aroyl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole Derivatives

Chem Biodivers. 2017 Feb;14(2). doi: 10.1002/cbdv.201600219. Epub 2017 Feb 1.

Abstract

A series of 3-(substituted aroyl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole derivatives were synthesized and determined for their anticancer activity against eleven cancer cell lines and two normal tissue cell lines using MTT assay. Among the synthesized compounds, compound 3f was the most potent compound against A375, CT-26, HeLa, MGC80-3, NCI-H460 and SGC-7901 cells (IC50 = 8.2 - 31.7 μm); 3g, 3n and 3a were the most potent compounds against CHO (IC50 = 8.2 μm), HCT-15 (IC50 = 21 μm) and MCF-7 cells (IC50 = 18.7 μm), respectively. Importantly, all the target compounds showed no cytotoxicity towards the normal tissue cell (IC50 > 100 μm). Thus, these compounds with the potent anticancer activity and low toxicity have potential for the development of new anticancer chemotherapy agents.

Keywords: Anticancer activities; Cytotoxic activities; MTT Assay; Pyrrole derivatives; Synthesis.

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Proliferation / drug effects*
  • Cells, Cultured
  • Dose-Response Relationship, Drug
  • Drug Design*
  • Drug Screening Assays, Antitumor
  • Human Umbilical Vein Endothelial Cells
  • Humans
  • Molecular Structure
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Pyrroles / chemical synthesis*
  • Pyrroles / pharmacology*
  • Structure-Activity Relationship

Substances

  • (4-bromophenyl)(4-(3,4,5-trimethoxyphenyl)-1H-pyrrol-3-yl)methanone
  • Antineoplastic Agents
  • Pyrroles