Please use this identifier to cite or link to this item: https://hdl.handle.net/11147/8886
Title: Synthesis and biological evaluation of new chloro/acetoxy substituted isoindole analogues as new tyrosine kinase inhibitors
Authors: Köse, Aytekin
Kaya, Meltem
HorasanKishalı, Nurhan
Akdemir, Atilla
Şahin, Ertan
Kara, Yunus
Şanlı Mohamed, Gülşah
Keywords: Norcantharimides
Isoindole
Cytotoxicity
HeLa cells
Publisher: Academic Press
Abstract: We have developed a versatile synthetic approach for the synthesis of new isoindole derivatives via the cleavage of ethers from tricyclic imide skeleton compounds. An exo-cycloadduct prepared from the Diels-Alder reaction of furan and maleic anhydride furnished imide derivatives. The epoxide ring was opened with Ac2O or Ac2O/AcCl in the presence of a catalytic amount of H2SO4 in order to yield new isoindole derivatives 8a-d and 9a-d. The anticancer activity of these compounds was evaluated against the HeLa cell lines. The synthesized compounds showed inhibitory effects on the viability of HeLa cells and the degree of cytotoxicity was increased with the level of bigger branched isoindole derivatives. To better understand the acting mechanism of these molecules, western blot analysis was performed with using mTOR and its downstream substrates. In addition, human mTOR and ribozomal S6 kinase beta 1 (RS6K beta 1) have been investigated with molecular modelling studies as possible targets for compound series 8 and 9.
URI: https://doi.org/10.1016/j.bioorg.2019.103421
https://hdl.handle.net/11147/8886
ISSN: 0045-2068
1090-2120
Appears in Collections:Chemistry / Kimya
PubMed İndeksli Yayınlar Koleksiyonu / PubMed Indexed Publications Collection
Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection
WoS İndeksli Yayınlar Koleksiyonu / WoS Indexed Publications Collection

Files in This Item:
File SizeFormat 
1-s2.0-S0045206819313306-main.pdf3.95 MBAdobe PDFView/Open
Show full item record



CORE Recommender

SCOPUSTM   
Citations

11
checked on Jun 21, 2024

WEB OF SCIENCETM
Citations

10
checked on Mar 16, 2024

Page view(s)

778
checked on Jun 17, 2024

Download(s)

184
checked on Jun 17, 2024

Google ScholarTM

Check




Altmetric


Items in GCRIS Repository are protected by copyright, with all rights reserved, unless otherwise indicated.