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Synthesis of novel imidazopyridines and their biological evaluation as potent anticancer agents: A promising candidate for glioblastoma

  • Dilek Güçlü
  • , Burak Kuzu
  • , İsrafil Tozlu
  • , Filiz Taşpınar
  • , Hande Canpınar
  • , Mehmet Taşpınar
  • , Nurettin Menges
  • Yuzuncu Yil University

Research output: Contribution to journalArticlepeer-review

26 Citations (Scopus)

Abstract

Novel imidazopyridine derivatives were synthesized according to a very simple protocol and then subjected to cytotoxicity testing against LN-405 cells. Two of the compounds exhibited antiproliferative effects on LN-405 cells at 10 and 75 µM and were selected as lead compounds for further study. Safety experiment for lead compounds on WS1 was carried out and IC50 values were calculated as 480 and 844 µM. LN-405 cell line were incubated with the lead compounds and then tested for DNA damage by comet assay and effects on cell cycle using flow cytometry. The results of these two tests showed that both lead compounds affected the G0/G1 phase and did not allow the cells to reach the synthesis phase. The log BB (blood–brain barrier) and Caco-2 permeability of the synthesized molecules were calculated and it was shown that imidazopyridine derivatives taken orally are likely to pass through gastrointestinal membrane and the blood–brain barrier.

Original languageEnglish
Pages (from-to)2647-2651
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume28
Issue number15
DOIs
Publication statusPublished - 15 Aug 2018

Keywords

  • ADME
  • Allene
  • Antiproliferative effect
  • CBOZXBCCVAKTNK-UHFFFAOYSA-N
  • CLGRBFHSSUCYBQ-UHFFFAOYSA-N
  • Comet assay
  • FBCRTGNQQCEZCY-UHFFFAOYSA-N
  • Flow cytometry
  • Heterocyclic chemistry
  • IKZIOBHJALXEDP-UHFFFAOYSA-N
  • INRFCXWTOWNWDJ-UHFFFAOYSA-N
  • LYJGPJYYRQGSMQ-UHFFFAOYSA-N
  • MCUUOBZJMYTMGY-UHFFFAOYSA-N
  • XMUFPJJKQBYFBC-UHFFFAOYSA-N
  • YJZACXKDSZKXAC-UHFFFAOYSA-N
  • ZMLDNJNPCKLPTJ-UHFFFAOYSA-N

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