4-Amino-2-arylamino-6-(2,6-dichlorophenyl)-pyrido[2,3- d ]pyrimidin-7-(8 H)-ones as BCR kinase inhibitors for B lymphoid malignancies

Raimon Puig De La Bellacasa; Gaël Roué; Patricia Balsas; Patricia Pérez-Galán; Jordi Teixidó; Dolors Colomer; José I. Borrell

doi:10.1016/j.ejmech.2014.09.018

4-Amino-2-arylamino-6-(2,6-dichlorophenyl)-pyrido[2,3- d ]pyrimidin-7-(8 H)-ones as BCR kinase inhibitors for B lymphoid malignancies

Raimon Puig De La Bellacasa, Gaël Roué, Patricia Balsas, Patricia Pérez-Galán, Jordi Teixidó, Dolors Colomer, José I. Borrell^*

^*Corresponding author for this work

Research output: Indexed journal article › Article › peer-review

23 Citations (Scopus)

Abstract

A new family of 4-aminopyrido[2,3-d]pyrimidines active against non-Hodgkin's lymphomas (NHLs) is described. Among these compounds, 19 inhibits the most upstream tyrosine kinases in the B cell receptor (BCR) signaling pathway which are involved in the mature B cell neoplasms. Thus, 19 showed antiproliferative activity at 24 h and 48 h against a panel of 20 NHLs cell lines with GI₅₀ ranging from 1.3 to 6.9 Î.

Original language	English
Pages (from-to)	664-675
Number of pages	12
Journal	European Journal of Medicinal Chemistry
Volume	86
DOIs	https://doi.org/10.1016/j.ejmech.2014.09.018
Publication status	Published - 30 Oct 2014

Keywords

7-oxopyrido[2,3-d]pyrimidines
B-cell receptor
Kinases
Non-Hodgkin's lymphomas
Small molecule inhibitor

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10.1016/j.ejmech.2014.09.018

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@article{14573a1e0ec242d0b65331b72161211b,

title = "4-Amino-2-arylamino-6-(2,6-dichlorophenyl)-pyrido[2,3- d ]pyrimidin-7-(8 H)-ones as BCR kinase inhibitors for B lymphoid malignancies",

abstract = "A new family of 4-aminopyrido[2,3-d]pyrimidines active against non-Hodgkin's lymphomas (NHLs) is described. Among these compounds, 19 inhibits the most upstream tyrosine kinases in the B cell receptor (BCR) signaling pathway which are involved in the mature B cell neoplasms. Thus, 19 showed antiproliferative activity at 24 h and 48 h against a panel of 20 NHLs cell lines with GI50 ranging from 1.3 to 6.9 {\^I}.",

keywords = "7-oxopyrido[2,3-d]pyrimidines, B-cell receptor, Kinases, Non-Hodgkin's lymphomas, Small molecule inhibitor",

author = "{Puig De La Bellacasa}, Raimon and Ga{\"e}l Rou{\'e} and Patricia Balsas and Patricia P{\'e}rez-Gal{\'a}n and Jordi Teixid{\'o} and Dolors Colomer and Borrell, {Jos{\'e} I.}",

note = "Funding Information: The authors appreciate the financial support from the Spanish Ministerio de Econom{\'i}a y Competitividad projects SAF2010-C21617-C02 (J.I.B.), SAF 09/9503 and SAF 12/31242 (D.C.), SAF 11/29326 (P.P.-G.), Redes Tem{\'a}ticas de Investigaci{\'o}n Cooperativa de C{\'a}ncer from the Instituto de Salud Carlos III ( RD2006/20/014 and RD12/0036/0004 ) and Generalitat de Catalunya 2009SGR967 (D.C.), Fondo de Investigaci{\'o}n Sanitaria, European Regional Development Fund (ERDF) “Una manera de hacer Europa” grants PI09/0060 and PI12/01847 (G.R.). R. Puig de la Bellacasa wants to thank Generalitat de Catalunya for a grant within the Talent empresa (TEM) 2009 program (2009 TEM 00128). Publisher Copyright: {\textcopyright} 2014 Elsevier Masson SAS. All rights reserved.",

year = "2014",

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doi = "10.1016/j.ejmech.2014.09.018",

language = "English",

volume = "86",

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AU - Puig De La Bellacasa, Raimon

AU - Roué, Gaël

AU - Balsas, Patricia

AU - Pérez-Galán, Patricia

AU - Teixidó, Jordi

AU - Colomer, Dolors

AU - Borrell, José I.

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PY - 2014/10/30

Y1 - 2014/10/30

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AB - A new family of 4-aminopyrido[2,3-d]pyrimidines active against non-Hodgkin's lymphomas (NHLs) is described. Among these compounds, 19 inhibits the most upstream tyrosine kinases in the B cell receptor (BCR) signaling pathway which are involved in the mature B cell neoplasms. Thus, 19 showed antiproliferative activity at 24 h and 48 h against a panel of 20 NHLs cell lines with GI50 ranging from 1.3 to 6.9 Î.

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KW - Kinases

KW - Non-Hodgkin's lymphomas

KW - Small molecule inhibitor

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ER -

4-Amino-2-arylamino-6-(2,6-dichlorophenyl)-pyrido[2,3- d ]pyrimidin-7-(8 H)-ones as BCR kinase inhibitors for B lymphoid malignancies

Abstract

Keywords

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