Synthesis, Antimicrobial and In Silico EGFR Inhibitory Activity Evaluation of Sulfonylamino Pyrrolidine Derivatives
A series of novel sulfonylamino pyrrolidine derivatives were synthesized, characterized and evaluated for their antimicrobial activity. All compounds exhibited moderate activity against the microorganisms tested. The compounds were evaluated in silico for their ability to inhibit epidermal growth fa...
Gespeichert in:
Veröffentlicht in: | Pharmaceutical chemistry journal 2016-10, Vol.50 (7), p.443-450 |
---|---|
Hauptverfasser: | , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | A series of novel sulfonylamino pyrrolidine derivatives were synthesized, characterized and evaluated for their antimicrobial activity. All compounds exhibited moderate activity against the microorganisms tested. The compounds were evaluated
in silico
for their ability to inhibit epidermal growth factor receptor (EGFR). Docking
in silico
demonstrated that the sulfonylamino pyrrolidine derivatives represent a new class of EGFR inhibitors and bind at the ATP binding pocket of the tyrosine kinase domain of EGFR. The free energy of binding and inhibition constant (
k
i
) of the docked compounds were evaluated. |
---|---|
ISSN: | 0091-150X 1573-9031 |
DOI: | 10.1007/s11094-016-1467-1 |