Ιδρυματικό Αποθετήριο
Πολυτεχνείο Κρήτης
Πολυτεχνείο Κρήτης
EN
|
EL
| URI | http://purl.tuc.gr/dl/dias/BB4F4358-458D-48EF-86FE-104612E2E789 | - |
| Αναγνωριστικό | http://www.sciencedirect.com/science/article/pii/S0223523413003838 | - |
| Αναγνωριστικό | https://doi.org/10.1016/j.ejmech.2013.06.015 | - |
| Γλώσσα | en | - |
| Μέγεθος | 12 pages | en |
| Τίτλος | Identification of novel chromone based sulfonamides as highly potent and selective inhibitors of alkaline phosphatases | en |
| Δημιουργός | Mariya al-Rashida | en |
| Δημιουργός | Rabia Raza | en |
| Δημιουργός | Ghulam Abbas | en |
| Δημιουργός | Muhammad Shakil Shah | en |
| Δημιουργός | Kostakis Georgios | en |
| Δημιουργός | Κωστακης Γεωργιος | el |
| Δημιουργός | Joanna Lecka | en |
| Δημιουργός | Jean Sévigny | en |
| Δημιουργός | Muhammad Muddassar | en |
| Δημιουργός | Constantina Papatriantafyllopoulou | en |
| Δημιουργός | Jamshed Iqbal | en |
| Εκδότης | Elsevier | en |
| Περίληψη | A new series of structurally diverse chromone containing sulfonamides has been developed. Crystal structures of three representative compounds (2a, 3a and 4a) in the series are reported. All compounds were screened for their inhibitory potential against alkaline phosphatases (ALPs). Two main classes of ALP isozymes were selected for this study, the tissue non-specific alkaline phosphatase (TNALP) from bovine and porcine source and the tissue-specific intestinal alkaline phosphatases (IALPs) from bovine source. All sulfonamide compounds had a marked preference for IALP (Ki, up to 0.01 ± 0.001 μM) over TNALPs. Kinetics studies of the compounds showed competitive mode of inhibition. Molecular docking studies were carried out in order to characterize the selective inhibition of the compounds. An additional interesting aspect of these chromone sulfonamides is their inhibitory activity against ecto-5′-nucleotidase enzyme. | en |
| Τύπος | Peer-Reviewed Journal Publication | en |
| Τύπος | Δημοσίευση σε Περιοδικό με Κριτές | el |
| Άδεια Χρήσης | http://creativecommons.org/licenses/by/4.0/ | en |
| Ημερομηνία | 2015-12-03 | - |
| Ημερομηνία Δημοσίευσης | 2013 | - |
| Θεματική Κατηγορία | Alkaline phosphatase inhibitors | en |
| Θεματική Κατηγορία | Ecto-5′-nucleotidase inhibitors | en |
| Θεματική Κατηγορία | Chromones | en |
| Θεματική Κατηγορία | Sulfonamides | en |
| Θεματική Κατηγορία | Molecular docking | en |
| Θεματική Κατηγορία | Structure activity relationships (SARs) | en |
| Βιβλιογραφική Αναφορά | M. al-Rashida, R. Raza, G. Abbas, M. S. Shah, G. E. Kostakis, J. Lecka, J. Sévigny, M. Muddassar, C. Papatriantafyllopoulou, and J. Iqbal, "Identification of novel chromone based sulfonamides as highly potent and selective inhibitors of alkaline phosphatases", Europ. J. Medicin. Chem., vol. 66, pp. 438-449, Aug. 2013. doi:10.1016/j.ejmech.2013.06.015 | en |
Copyright © DIAS 2013
