Home / Publications / Rational design and synthesis of novel Syk-kinase inhibitors

Rational design and synthesis of novel Syk-kinase inhibitors

Alexey A Zeifman 1
Alexey A Zeifman
Ilya Yur'evich Titov 1, 2
Ilya Yur'evich Titov
Igor Svitanko 2
Igor Svitanko
Tatiana Vladimirovna Rakitina 3, 4
Tatiana Vladimirovna Rakitina
Aleksey Valer'evich Lipkin 4, 5
Aleksey Valer'evich Lipkin
Viktor Sergeevich Stroylov 1, 2
Viktor Sergeevich Stroylov
Oleg Valentinovich Stroganov 1, 2
Oleg Valentinovich Stroganov
Fedor Nikolaevich Novikov 1
Fedor Nikolaevich Novikov
Ghermes Grigor'evich Chilov 1, 2
Ghermes Grigor'evich Chilov
Published 2012-02-27
CommunicationVolume 22, Issue 2, 73-74
10
Share
Cite this
GOST
 | 
Cite this
GOST Copy
Zeifman A. A. et al. Rational design and synthesis of novel Syk-kinase inhibitors // Mendeleev Communications. 2012. Vol. 22. No. 2. pp. 73-74.
GOST all authors (up to 50) Copy
Zeifman A. A., Titov I. Y., Svitanko I., Rakitina T. V., Lipkin A. V., Stroylov V. S., Stroganov O. V., Novikov F. N., Chilov G. G. Rational design and synthesis of novel Syk-kinase inhibitors // Mendeleev Communications. 2012. Vol. 22. No. 2. pp. 73-74.
RIS
 | 
Cite this
RIS Copy
TY - JOUR
DO - 10.1016/j.mencom.2012.03.006
UR - https://mendcomm.colab.ws/publications/10.1016/j.mencom.2012.03.006
TI - Rational design and synthesis of novel Syk-kinase inhibitors
T2 - Mendeleev Communications
AU - Zeifman, Alexey A
AU - Titov, Ilya Yur'evich
AU - Svitanko, Igor
AU - Rakitina, Tatiana Vladimirovna
AU - Lipkin, Aleksey Valer'evich
AU - Stroylov, Viktor Sergeevich
AU - Stroganov, Oleg Valentinovich
AU - Novikov, Fedor Nikolaevich
AU - Chilov, Ghermes Grigor'evich
PY - 2012
DA - 2012/02/27
PB - Mendeleev Communications
SP - 73-74
IS - 2
VL - 22
ER -
BibTex
 | 
Cite this
BibTex (up to 50 authors) Copy
@article{2012_Zeifman,
author = {Alexey A Zeifman and Ilya Yur'evich Titov and Igor Svitanko and Tatiana Vladimirovna Rakitina and Aleksey Valer'evich Lipkin and Viktor Sergeevich Stroylov and Oleg Valentinovich Stroganov and Fedor Nikolaevich Novikov and Ghermes Grigor'evich Chilov},
title = {Rational design and synthesis of novel Syk-kinase inhibitors},
journal = {Mendeleev Communications},
year = {2012},
volume = {22},
publisher = {Mendeleev Communications},
month = {Feb},
url = {https://mendcomm.colab.ws/publications/10.1016/j.mencom.2012.03.006},
number = {2},
pages = {73--74},
doi = {10.1016/j.mencom.2012.03.006}
}
MLA
Cite this
MLA Copy
Zeifman, Alexey A., et al. “Rational design and synthesis of novel Syk-kinase inhibitors.” Mendeleev Communications, vol. 22, no. 2, Feb. 2012, pp. 73-74. https://mendcomm.colab.ws/publications/10.1016/j.mencom.2012.03.006.

Abstract

Molecular modeling and subsequent synthesis of novel Syk-kinase inhibitors, 7H-pyrrolo[2,3-d]pyrimidine and 1,3,5-triazine derivatives, have been carried out. The best of the obtained compounds demonstrated to inhibit Syk-kinase activity at IC50 = 230±10 nM

References

1.
Identification of the Syk kinase inhibitor R112 by a human mast cell screen
ROSSI A., HERLAAR E., BRASELMANN S., HUYNH S., TAYLOR V., FRANCES R., ISSAKANI S., ARGADE A., SINGH R., PAYAN D.
Journal of Allergy and Clinical Immunology, 2006
2.
An Oral Spleen Tyrosine Kinase (Syk) Inhibitor for Rheumatoid Arthritis
Weinblatt M.E., Kavanaugh A., Genovese M.C., Musser T.K., Grossbard E.B., Magilavy D.B.
New England Journal of Medicine, 2010
3.
Rheumatoid arthritis
Lee D.M., Weinblatt M.E.
The Lancet, 2001
4.
Mouse models of non-Hodgkin lymphoma reveal Syk as an important therapeutic target
Young R.M., Hardy I.R., Clarke R.L., Lundy N., Pine P., Turner B.C., Potter T.A., Refaeli Y.
Blood, 2009
5.
Virtual Screening Methods that Complement HTS
Stahura F., Bajorath J.
Combinatorial Chemistry and High Throughput Screening, 2004
6.
Virtual screening and fast automated docking methods
7.
Spleen tyrosine kinases: biology, therapeutic targets and drugs
Riccaboni M., Bianchi I., Petrillo P.
Drug Discovery Today, 2010
8.
Improving performance of docking-based virtual screening by structural filtration
Novikov F.N., Stroylov V.S., Stroganov O.V., Chilov G.G.
Journal of Molecular Modeling, 2009
9.
S. Bhamidipati, R. Singh, T. Sun, E. Masuda, Rigel Pharmaceuticals Inc., Patent WO2008064274, 2008.
10.
R. Singh, A. Argade, D. Payan, S. Molineaux, S. Holland, J. Clough, H. Keim, S. Bhamidipati, C. Sylvain and H. Li, A. Rossi, Rigel Pharmaceuticals Inc., Patent US2006058292, 2006.
11.
Lead Finder: An Approach To Improve Accuracy of Protein−Ligand Docking, Binding Energy Estimation, and Virtual Screening
Stroganov O.V., Novikov F.N., Stroylov V.S., Kulkov V., Chilov G.G.
Journal of Chemical Information and Modeling, 2008
12.
Structural Insights for Design of Potent Spleen Tyrosine Kinase Inhibitors from Crystallographic Analysis of Three Inhibitor Complexes
Villaseñor A.G., Kondru R., Ho H., Wang S., Papp E., Shaw D., Barnett J.W., Browner M.F., Kuglstatter A.
Chemical Biology and Drug Design, 2009
13.
TSAR, a new graph-theoretical approach to computational modeling of protein side-chain flexibility: Modeling of ionization properties of proteins
Stroganov O.V., Novikov F.N., Zeifman A.A., Stroylov V.S., Chilov G.G.
Proteins: Structure, Function and Genetics, 2011
14.
CSAR Scoring Challenge Reveals the Need for New Concepts in Estimating Protein–Ligand Binding Affinity
Novikov F.N., Zeifman A.A., Stroganov O.V., Stroylov V.S., Kulkov V., Chilov G.G.
Journal of Chemical Information and Modeling, 2011