MEK (MAPKK) inhibitors. Part 2: structure–activity relationships of 4-anilino-3-cyano-6,7-dialkoxyquinolines

Zhang, Nan; Wu, Botao; Eudy, Nancy H.; Wang, A. Yanong; Ye, Fei; Powell, Dennis; Wissner, Allan; Feldberg, Larry; Kim, Steven C.; Mallon, Robert; Kovacs, Eleonora D.; Toral‐Barza, Lourdes; Kohler, Constance

doi:10.1016/s0960-894x(01)00238-4

Cited by 28 publications

(12 citation statements)

References 35 publications

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“…Researchers from Wyeth have extensively published and presented on cyanoquinoline-derived ATP-competitive MEK inhibitors [28][29][30][31][32][33][34][35]. Several authors have already reviewed portions of the Wyeth program [13,36].…”

Section: Atp-competitive Mek Inhibitorsmentioning

confidence: 99%

Progress Towards Therapeutic Small Molecule MEK Inhibitors for Use in Cancer Therapy

Wallace

Lyssikatos²,

Yeh³

et al. 2005

CTMC

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This paper reviews recent progress in the design and evaluation of MEK inhibitors as cancer therapeutics. Activation of the Ras / Raf / MEK / MAP kinase pathway has been implicated in uncontrolled cell proliferation and tumor growth. Mutated, oncogenic forms of Ras are found in 50% of colon, 90% of pancreatic and 30% of lung cancers. Recently, B-Raf mutations have been identified in more than 60% of malignant melanomas and from 40-70% of papillary thyroid cancers. MEK, a dual specificity kinase, is a key player in this pathway; it is downstream of both Ras and Raf and activates ERK1/2 through phosphorylation of key tyrosine and threonine residues. Representative examples of both ATP competitive and non-competitive inhibitors as well as natural product based inhibitors will be discussed.

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Section: Atp-competitive Mek Inhibitorsmentioning

confidence: 99%

Progress Towards Therapeutic Small Molecule MEK Inhibitors for Use in Cancer Therapy

Wallace

Lyssikatos²,

Yeh³

et al. 2005

CTMC

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“…Representative examples of this class of inhibitors are cyanoquinoline (compound 7, Fig. 3 ) [ 18 ] and resorcyclic acid (compound 8, Fig. 3 ) [ 19 ] derivatives.…”

Section: Modulators Of the Ras/raf/mek Signaling Cascadementioning

confidence: 99%

Protein and lipid kinase inhibitors as targeted anticancer agents of the Ras/Raf/MEK and PI3K/PKB pathways

García‐Echeverría

2008

Purinergic Signalling

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The identification and characterization of the components of individual signal transduction cascades, and advances in our understanding on how these biological signals are integrated in cancer initiation and progression, have provided new strategies for therapeutic intervention in solid tumors and hematological malignancies. To this end, pharmaceutical efforts have been directed to target different components of the Ras/Raf/MEK and PI3K/PKB pathways. This review article covers recent salient achievements in the identification and development of Raf, MEK, and PI3K inhibitors.

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“…As MEK inhibitors, compounds of these classes are fully expected to be competitive with ATP [39] and, as such, will be challenged to match the selectivity of the non-competitive MEK inhibitors currently being advanced. The licensing by AstraZeneca of ARRY-142886 suggests a realisation of this and again make it unlikely that a clinical candidate will come from the applications.…”

Section: Expert Opinionmentioning

confidence: 99%

Methylenedioxyanilino-quinazolines and -cyanoquinolines as inhibitors of MEK and/or Src

2004

Expert Opinion on Therapeutic Patents

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MEK (MAPKK) inhibitors. Part 2: structure–activity relationships of 4-anilino-3-cyano-6,7-dialkoxyquinolines

Cited by 28 publications

References 35 publications

Progress Towards Therapeutic Small Molecule MEK Inhibitors for Use in Cancer Therapy

Progress Towards Therapeutic Small Molecule MEK Inhibitors for Use in Cancer Therapy

Protein and lipid kinase inhibitors as targeted anticancer agents of the Ras/Raf/MEK and PI3K/PKB pathways

Methylenedioxyanilino-quinazolines and -cyanoquinolines as inhibitors of MEK and/or Src

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