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
Kaya, Meltem
Şanlı Mohamed, Gülşah
Izmir Institute of Technology. Chemistry
Keywords: Norcantharimides
Isoindole
Cytotoxicity
HeLa cells
Issue Date: 2020
Publisher: Academic Press Inc.
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.
Description: Sanli-Mohamed, Gulsah/0000-0003-0282-4428; Akdemir, Atilla/0000-0001-8416-0471
WOS: 000505596300076
PubMed: 31759659
URI: https://doi.org/10.1016/j.bioorg.2019.103421
https://hdl.handle.net/11147/8886
ISSN: 0045-2068
1090-2120
Appears in Collections:PubMed İndeksli Yayınlar Koleksiyonu / PubMed Indexed Publications Collection
Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection
WoS İndeksli Yayınlar Koleksiyonu / WoS Indexed Publications Collection

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