Handling drug-target selectivity: A study on ureido containing Carbonic Anhydrase inhibitors
Küçük Resim Yok
Tarih
2021
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Elsevier Masson s.r.l.
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
Here we report the synthesis of a series of taurine substituted sulfonamide derivatives 1-29 having the ureido moiety installed at the tail section as selective inhibitors of the tumor associated human (h) Carbonic Anhydrase (CA; EC 4.2.1.1) IX and XII. The series was deeply investigated for their kinetic features which demonstrated a strong dependence on the ureido moiety. High resolution X-ray crystallographic investigation on selected ligand adducts complexed with hCA II and hCA IX-mimic revealed a strong correlation between the ureido moiety and the amino acid residues Q92 and Q67 in both the hCA II and hCA IX-mimic, contributing to highly stabilized ligand-protein complex. © 2020 Elsevier Masson SAS
Açıklama
Anahtar Kelimeler
Carbonic anhydrase inhibitors (CAIs), Carbonic anhydrase IX, Taurine, Ureido
Kaynak
European Journal of Medicinal Chemistry
WoS Q Değeri
Scopus Q Değeri
Q1
Cilt
212
