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Novel fragment-like inhibitors of EphA2 obtained by experimental screening and modelling

Viktor Sergeevich Stroylov 1
Viktor Sergeevich Stroylov
, 
Tatiana Vladimirovna Rakitina 2, 3
Tatiana Vladimirovna Rakitina
, 
Fedor Nikolaevich Novikov 1
Fedor Nikolaevich Novikov
, 
Oleg Valentinovich Stroganov 1, 4
Oleg Valentinovich Stroganov
, 
Ghermes Grigor'evich Chilov 1, 4
Ghermes Grigor'evich Chilov
, 
Aleksey Valer'evich Lipkin 3, 5
Aleksey Valer'evich Lipkin
10.1016/j.mencom.2010.09.007
Published 2010-09-09
Communication , Volume 20, Issue 5, 263-265
10
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Stroylov V. S. et al. Novel fragment-like inhibitors of EphA2 obtained by experimental screening and modelling // Mendeleev Communications. 2010. Vol. 20. No. 5. pp. 263-265.
GOST all authors (up to 50) Copy
Stroylov V. S., Rakitina T. V., Novikov F. N., Stroganov O. V., Chilov G. G., Lipkin A. V. Novel fragment-like inhibitors of EphA2 obtained by experimental screening and modelling // Mendeleev Communications. 2010. Vol. 20. No. 5. pp. 263-265.
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TY - JOUR
DO - 10.1016/j.mencom.2010.09.007
UR - https://mendcomm.colab.ws/publications/10.1016/j.mencom.2010.09.007
TI - Novel fragment-like inhibitors of EphA2 obtained by experimental screening and modelling
T2 - Mendeleev Communications
AU - Stroylov, Viktor Sergeevich
AU - Rakitina, Tatiana Vladimirovna
AU - Novikov, Fedor Nikolaevich
AU - Stroganov, Oleg Valentinovich
AU - Chilov, Ghermes Grigor'evich
AU - Lipkin, Aleksey Valer'evich
PY - 2010
DA - 2010/09/09
PB - Mendeleev Communications
SP - 263-265
IS - 5
VL - 20
ER -
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@article{2010_Stroylov,
author = {Viktor Sergeevich Stroylov and Tatiana Vladimirovna Rakitina and Fedor Nikolaevich Novikov and Oleg Valentinovich Stroganov and Ghermes Grigor'evich Chilov and Aleksey Valer'evich Lipkin},
title = {Novel fragment-like inhibitors of EphA2 obtained by experimental screening and modelling},
journal = {Mendeleev Communications},
year = {2010},
volume = {20},
publisher = {Mendeleev Communications},
month = {Sep},
url = {https://mendcomm.colab.ws/publications/10.1016/j.mencom.2010.09.007},
number = {5},
pages = {263--265},
doi = {10.1016/j.mencom.2010.09.007}
}
MLA
Cite this
MLA Copy
Stroylov, Viktor Sergeevich, et al. “Novel fragment-like inhibitors of EphA2 obtained by experimental screening and modelling.” Mendeleev Communications, vol. 20, no. 5, Sep. 2010, pp. 263-265. https://mendcomm.colab.ws/publications/10.1016/j.mencom.2010.09.007.

Abstract

A set of novel fragment-like catechol derivatives were identified as EphA2 inhibitors and were further profiled against a panel of 19 tyrosine kinases. In addition to EphA2, the recovered hits were active against EGFR, FGFR1, FGFR2, Abl and PDGFR-a, and according to molecular modelling studies catechol moiety was capable of forming two or more correlated hydrogen bonds with the kinase hinge region, suggesting prospects of its further optimization as an EphA2 inhibitor.

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