ChemInform Abstract: Synthesis and in vitro EGFR (ErbB1) Tyrosine Kinase Inhibitory Activity of 4-N-Substituted 6-Aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines.

ChemInform ◽  
2012 ◽  
Vol 43 (15) ◽  
pp. no-no
Author(s):  
Svein Jacob Kaspersen ◽  
Christopher Soerum ◽  
Veronica Willassen ◽  
Erik Fuglseth ◽  
Eli Kjoebli ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Inhibitory Activity ◽  
Kinase Inhibitory Activity

scholarly journals Synthesis and In Vitro Protein Tyrosine Kinase Inhibitory Activity of Furan-2-yl(phenyl)methanone Derivatives

Molecules ◽  
2011 ◽  
Vol 16 (6) ◽  
pp. 4897-4911 ◽  
Author(s):  
Fei Lang Zheng ◽  
Shu Rong Ban ◽  
Xiu E Feng ◽  
Cheng Xiao Zhao ◽  
Wenhan Lin ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Inhibitory Activity ◽  
Protein Tyrosine Kinase ◽  
Protein Tyrosine ◽  
Kinase Inhibitory Activity ◽  
Vitro Protein

Synthesis and in vitro EGFR (ErbB1) tyrosine kinase inhibitory activity of 4-N-substituted 6-aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines

2011 ◽  
Vol 46 (12) ◽  
pp. 6002-6014 ◽  
Author(s):  
Svein Jacob Kaspersen ◽  
Christopher Sørum ◽  
Veronica Willassen ◽  
Erik Fuglseth ◽  
Eli Kjøbli ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Inhibitory Activity ◽  
Kinase Inhibitory Activity

scholarly journals Identification of Vinyl Sulfone Derivatives as EGFR Tyrosine Kinase Inhibitor: In Vitro and In Silico Studies

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2211
Author(s):  
Thitinan Aiebchun ◽  
Panupong Mahalapbutr ◽  
Atima Auepattanapong ◽  
Onnicha Khaikate ◽  
Supaphorn Seetaha ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Inhibitory Activity ◽  
In Silico ◽  
Kinase Inhibitor ◽  
Kinase Assay ◽  
Vinyl Sulfone ◽  
Egfr Tyrosine Kinase ◽  
In Silico Studies ◽  
Sulfone Derivatives

Epidermal growth factor receptor (EGFR), overexpressed in many types of cancer, has been proved as a high potential target for targeted cancer therapy due to its role in regulating proliferation and survival of cancer cells. In the present study, a series of designed vinyl sulfone derivatives was screened against EGFR tyrosine kinase (EGFR-TK) using in silico and in vitro studies. The molecular docking results suggested that, among 78 vinyl sulfones, there were eight compounds that could interact well with the EGFR-TK at the ATP-binding site. Afterwards, these screened compounds were tested for the inhibitory activity towards EGFR-TK using ADP-Glo™ kinase assay, and we found that only VF16 compound exhibited promising inhibitory activity against EGFR-TK with the IC50 value of 7.85 ± 0.88 nM. In addition, VF16 showed a high cytotoxicity with IC50 values of 33.52 ± 2.57, 54.63 ± 0.09, and 30.38 ± 1.37 µM against the A431, A549, and H1975 cancer cell lines, respectively. From 500-ns MD simulation, the structural stability of VF16 in complex with EGFR-TK was quite stable, suggesting that this compound could be a novel small molecule inhibitor targeting EGFR-TK.

New Cytotoxic Bisindole Alkaloids with Protein Tyrosine Kinase Inhibitory Activity from a Myxomycete Lycogala epidendrum.

ChemInform ◽  
2005 ◽  
Vol 36 (42) ◽  
Author(s):  
Takahiro Hosoya ◽  
Yukinori Yamamoto ◽  
Yoshimasa Uehara ◽  
Masahiko Hayashi ◽  
Kanki Komiyama ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Inhibitory Activity ◽  
Protein Tyrosine Kinase ◽  
Protein Tyrosine ◽  
Kinase Inhibitory Activity

Water-soluble HPMA copolymer–wortmannin conjugate retains phosphoinositide 3-kinase inhibitory activity in vitro and in vivo

2001 ◽  
Vol 74 (1-3) ◽  
pp. 275-281 ◽  
Author(s):  
L. Varticovski ◽  
Zheng-Rong Lu ◽  
Kahlil Mitchell ◽  
Isabel de Aos ◽  
Jindrich Kopeček
Keyword(s):  
Inhibitory Activity ◽  
Water Soluble ◽  
Hpma Copolymer ◽  
Phosphoinositide 3 Kinase ◽  
Kinase Inhibitory Activity
Sign in / Sign up

Export Citation Format

Share Document