9,10-Dibromo-N-aryl-9,10-dihydro-9,10-[3,4]epipyrroloanthracene-12,14-diones: Synthesis and Investigation of Their Effects on Carbonic Anhydrase Isozymes I, II, IX, and XII
Özet
N-substituted maleimides were synthesized from maleic anhydride and primary amines. 1,4-Dibromodibenzo[e,h]bicyclo-[2,2,2]octane-2,3-dicarboximide derivatives (4a-f) were prepared by the [4+2] cycloaddition reaction of dibromoanthracenes with the N-substituted maleimide derivatives. The carbonic anhydrase (CA, EC 4.2.1.1) inhibitory effects of the new derivatives were assayed against the human (h) isozymes hCA I, II, IX, and XII. All tested bicyclo dicarboximide derivatives exhibited excellent inhibitory effects in the nanomolar range, with K-i values in the range of 117.73-232.87 nM against hCA I and of 69.74-111.51 nM against hCA II, whereas they were low micromolar inhibitors against hCA IX and XII.
Anahtar kelimeler
Atıf için künye
Goksu, H., Topal, M., KESKIN, A., Gültekin, M. S., Çelik, M., Gülçin, İ., Tanç, M., & SUPURAN, C. T. (2016). 9,10-Dibromo-N-aryl-9,10-dihydro-9,10-[3,4]epipyrroloanthracene-12,14-diones: Synthesis and Investigation of Their Effects on Carbonic Anhydrase Isozymes I, II, IX, and XII. Archiv der Pharmazie, 349(6), 466–474. https://doi.org/10.1002/ardp.201600047
BibTeX
@article{goksu2016-68066,
author = {Goksu, Haydar and Topal, Meryem and KESKIN, Ali and Gültekin, Mehmet Serdar and Çelik, Murat and Gülçin, İlhami and Tanç, Muhammet and SUPURAN, Claudiu T.},
title = {9,10-Dibromo-N-aryl-9,10-dihydro-9,10-[3,4]epipyrroloanthracene-12,14-diones: Synthesis and Investigation of Their Effects on Carbonic Anhydrase Isozymes I, II, IX, and XII},
journal = {Archiv der Pharmazie},
year = {2016},
volume = {349},
number = {6},
pages = {466--474},
issn = {0365-6233},
doi = {10.1002/ardp.201600047},
url = {https://akademik.atauni.edu.tr/yayinlar/68066-910-dibromo-n-aryl-910-dihydro-910-34epipyrroloanthracene-1214-diones-synthesis}
}