Evaluation of indole esters as inhibitors of p60(c-Src) receptor tyrosine kinase and investigation of the inhibition using receptor docking studies
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.18, sa.6, ss.485-490, 2003 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 18 Sayı: 6
- Basım Tarihi: 2003
- Doi Numarası: 10.1080/14756360310001612211
- Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.485-490
- Anahtar Kelimeler: tyrosine kinase, inhibition, docking, indole esters, active site, enzyme interaction, p60(c-Src), GROWTH-FACTOR RECEPTOR, DISCOVERY
- Ankara Üniversitesi Adresli: Hayır
Özet
Several indole esters were tested as inhibitors of tyrosine kinase p60(c-Src) . Compound (4) was found fairly active against the enzyme with IC50 =1.34 muM. DOCK methodology was used to asses our inhibitors for their inhibitory potency against tyrosine kinase. The docking results showed that compounds (4), (25) and (26) were bound to the active site of the enzyme Lys 295 of p60(c-Src) tyrosine kinase. Both activity and docking studies showed a parallel result, with compound (4) having a better interaction with the enzyme active site and also greater activity than the other compounds, indicating a potential role as new lead inhibitor.