TY - JOUR
T1 - Synthesis of novel imidazopyridines and their biological evaluation as potent anticancer agents
T2 - A promising candidate for glioblastoma
AU - Güçlü, Dilek
AU - Kuzu, Burak
AU - Tozlu, İsrafil
AU - Taşpınar, Filiz
AU - Canpınar, Hande
AU - Taşpınar, Mehmet
AU - Menges, Nurettin
N1 - Publisher Copyright:
© 2018 Elsevier Ltd
PY - 2018/8/15
Y1 - 2018/8/15
N2 - 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.
AB - 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.
KW - ADME
KW - Allene
KW - Antiproliferative effect
KW - CBOZXBCCVAKTNK-UHFFFAOYSA-N
KW - CLGRBFHSSUCYBQ-UHFFFAOYSA-N
KW - Comet assay
KW - FBCRTGNQQCEZCY-UHFFFAOYSA-N
KW - Flow cytometry
KW - Heterocyclic chemistry
KW - IKZIOBHJALXEDP-UHFFFAOYSA-N
KW - INRFCXWTOWNWDJ-UHFFFAOYSA-N
KW - LYJGPJYYRQGSMQ-UHFFFAOYSA-N
KW - MCUUOBZJMYTMGY-UHFFFAOYSA-N
KW - XMUFPJJKQBYFBC-UHFFFAOYSA-N
KW - YJZACXKDSZKXAC-UHFFFAOYSA-N
KW - ZMLDNJNPCKLPTJ-UHFFFAOYSA-N
UR - https://www.scopus.com/pages/publications/85049312276
U2 - 10.1016/j.bmcl.2018.06.033
DO - 10.1016/j.bmcl.2018.06.033
M3 - Article
C2 - 30042044
AN - SCOPUS:85049312276
SN - 0960-894X
VL - 28
SP - 2647
EP - 2651
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 15
ER -