5-aryl-pyrazolo[3,4-b]pyridazines: Potent inhibitors of glycogen synthase kinase-3 (GSK-3)

J. Witherington; V. Bordas; David Haigh; D.M.B. Hickey; R.J. Ife; A.D. Rawlings; B.P. Slingsby; D.G. Smith; R.W. Ward

doi:10.1016/S0960-894X(03)00135-5

5-aryl-pyrazolo[3,4-b]pyridazines: Potent inhibitors of glycogen synthase kinase-3 (GSK-3)

J. Witherington, V. Bordas, David Haigh, D.M.B. Hickey, R.J. Ife, A.D. Rawlings, B.P. Slingsby, D.G. Smith, R.W. Ward

Research output: Contribution to journal › Article › peer-review

Abstract

Introduction of a nitrogen atom into the 6-position of a series of pyrazolo[3,4-b]pyridines led to a dramatic improvement in the potency of GSK-3 inhibition. Rationalisation of the binding mode suggested participation of a putative structural water molecule, which was subsequently confirmed by X-ray crystallography. (C) 2003 Elsevier Science Ltd. All rights reserved.

Original language	English
Pages (from-to)	1581-1584
Number of pages	4
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	13
Issue number	9
DOIs	https://doi.org/10.1016/S0960-894X(03)00135-5
Publication status	Published - 05 May 2003

ASJC Scopus subject areas

Biochemistry
Molecular Biology
Organic Chemistry
Drug Discovery
Pharmaceutical Science

Access to Document

10.1016/S0960-894X(03)00135-5

Cite this

@article{2c06ceea6d534169b1aea0c2c6c3d12e,

title = "5-aryl-pyrazolo[3,4-b]pyridazines: Potent inhibitors of glycogen synthase kinase-3 (GSK-3)",

abstract = "Introduction of a nitrogen atom into the 6-position of a series of pyrazolo[3,4-b]pyridines led to a dramatic improvement in the potency of GSK-3 inhibition. Rationalisation of the binding mode suggested participation of a putative structural water molecule, which was subsequently confirmed by X-ray crystallography. (C) 2003 Elsevier Science Ltd. All rights reserved.",

author = "J. Witherington and V. Bordas and David Haigh and D.M.B. Hickey and R.J. Ife and A.D. Rawlings and B.P. Slingsby and D.G. Smith and R.W. Ward",

year = "2003",

month = may,

day = "5",

doi = "10.1016/S0960-894X(03)00135-5",

language = "English",

volume = "13",

pages = "1581--1584",

journal = "Bioorganic & Medicinal Chemistry Letters",

issn = "1464-3405",

publisher = "Elsevier Ltd",

number = "9",

}

TY - JOUR

T1 - 5-aryl-pyrazolo[3,4-b]pyridazines: Potent inhibitors of glycogen synthase kinase-3 (GSK-3)

AU - Witherington, J.

AU - Bordas, V.

AU - Haigh, David

AU - Hickey, D.M.B.

AU - Ife, R.J.

AU - Rawlings, A.D.

AU - Slingsby, B.P.

AU - Smith, D.G.

AU - Ward, R.W.

PY - 2003/5/5

Y1 - 2003/5/5

N2 - Introduction of a nitrogen atom into the 6-position of a series of pyrazolo[3,4-b]pyridines led to a dramatic improvement in the potency of GSK-3 inhibition. Rationalisation of the binding mode suggested participation of a putative structural water molecule, which was subsequently confirmed by X-ray crystallography. (C) 2003 Elsevier Science Ltd. All rights reserved.

AB - Introduction of a nitrogen atom into the 6-position of a series of pyrazolo[3,4-b]pyridines led to a dramatic improvement in the potency of GSK-3 inhibition. Rationalisation of the binding mode suggested participation of a putative structural water molecule, which was subsequently confirmed by X-ray crystallography. (C) 2003 Elsevier Science Ltd. All rights reserved.

UR - http://www.scopus.com/inward/record.url?scp=0037420823&partnerID=8YFLogxK

U2 - 10.1016/S0960-894X(03)00135-5

DO - 10.1016/S0960-894X(03)00135-5

M3 - Article

SN - 1464-3405

VL - 13

SP - 1581

EP - 1584

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 9

ER -

5-aryl-pyrazolo[3,4-b]pyridazines: Potent inhibitors of glycogen synthase kinase-3 (GSK-3)

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this