420137-05-9Relevant academic research and scientific papers
Synthesis and characterisation of novel tricyclic and tetracyclic furoindoles: Biological evaluation as SAHA enhancer against neuroblastoma and breast cancer cells
Bingul, Murat,Arndt, Greg M.,Marshall, Glenn M.,Black, David Stc.,Cheung, Belamy B.,Kumar, Naresh
, (2021/09/28)
The dihydropyranoindole structures were previously identified as promising scaffolds for improving the anti-cancer activity of histone deacetylase inhibitors. This work describes the synthesis of related furoindoles and their ability to synergize with suberoylanilide hydroxamic acid (SAHA) against neuroblastoma and breast cancer cells. The nucleophilic substitution of hydroxyin-dole methyl esters with α-haloketones yielded the corresponding arylether ketones, which were subsequently cyclized to tricyclic and tetracyclic furoindoles. The furoindoles showed promising individual cytotoxic efficiency against breast cancer cells, as well as decent SAHA enhancement against cancer cells in select cases. Interestingly, the best IC50 value was obtained with the non-cyclized intermediate.
Selective NR1/2B N-methyl-D-aspartate receptor antagonists among indole-2-carboxamides and benzimidazole-2-carboxamides
Borza, István,Bozó, éva,Barta-Szalai, Gizella,Kiss, Csilla,Tárkányi, Gábor,Demeter, ádám,Gáti, Tamás,Háda, Viktor,Kolok, Sándor,Gere, Anikó,Fodor, László,Nagy, József,Galgóczy, Kornél,Magdó, Ildikó,ágai, Béla,Fetter, József,Bertha, Ferenc,Keserü, Gy?rgy M.,Horváth, Csilla,Farkas, Sándor,Greiner, István,Domány, Gy?rgy
, p. 901 - 914 (2008/02/03)
(4-Benzylpiperidine-1-yl)-(6-hydroxy-1H-indole-2-yl)-methanone (6a) derived from (E)-1 -(4-benzylpiperidin-1-yl)-3-(4-hydroxy-phenyl)-propenone (5) was identified as a potent NR2B subunit-selective antagonist of the NMDA receptor. To establish the structu
