Structure-based design and synthesis of novel pseudosaccharine derivatives as antiproliferative agents and kinase inhibitors
Elsayed, Mohamed S A; El-Araby, Moustafa E; Serya, Rabah; El-Khatib, Ahmed H; Linscheid, Michael W; Khaled A M Abouzid;
Abstract
This study is concerned with the implementation of structure-based techniques for the design of new heterocyclic compounds based on pseudosaccharine scaffold with protein kinase inhibition activity. This nucleus was exploited based on the well-known quinazoline core and its interactions with several protein kinases. Two series of compounds employing this new scaffold were synthesized and evaluated at enzymatic and cellular levels. Compound 9b displayed broad spectrum antiproliferative activity on NCI 60-cell lines panel with mean GI50 of 5.4 μM. Investigation of the molecular mechanism showed probable inhibitory activity against Src kinase.
Other data
Title | Structure-based design and synthesis of novel pseudosaccharine derivatives as antiproliferative agents and kinase inhibitors | Authors | Elsayed, Mohamed S A; El-Araby, Moustafa E; Serya, Rabah ; El-Khatib, Ahmed H; Linscheid, Michael W; Khaled A M Abouzid | Keywords | Benzo[d]isothiazole 1,1-dioxide;Pseudosaccharine;Antiproliferative;Kinase;Docking;CELL LUNG-CANCER;C-MET;SRC;DISCOVERY;POTENT;QUINAZOLINES;BMS-354825;DASATINIB;CARCINOMA;RECEPTOR | Issue Date | Mar-2013 | Publisher | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER | Journal | European Journal of Medicinal Chemistry | Volume | 61 | Start page | 122 | End page | 131 | ISSN | 0223-5234 | DOI | 10.1016/j.ejmech.2012.09.039 | PubMed ID | 23063746 | Scopus ID | 2-s2.0-84874930935 | Web of science ID | WOS:000316537200012 |
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