PMID

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Article Title

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Discovery of novel inhibitors of Aurora kinases with indazole scaffold: In silico fragment-based and knowledge-based drug design.

Taiwan National Health Research Institutes

Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening.

University of Berne

Discovery of antitumor anthra[2,3-b]furan-3-carboxamides: Optimization of synthesis and evaluation of antitumor properties.

Mendeleyev University of Chemical Technology

Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2).

Icahn School of Medicine At Mount Sinai

Synthesis and evaluation of novel 1H-pyrrolo[2,3-b]pyridine-5-carboxamide derivatives as potent and orally efficacious immunomodulators targeting JAK3.

Astellas Pharma

SAR156497, an exquisitely selective inhibitor of aurora kinases.

Sanofi

Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor.

National Taiwan University

In vitro and in vivo characterization of a benzofuran derivative, a potential anticancer agent, as a novel Aurora B kinase inhibitor.

Fudan University

Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.

Sun Yat-Sen University

Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3.

Califia Bio

Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole-benzimidazole derivatives as potent Aurora A/B kinase inhibitors.

Xuzhou Medical College

Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index.

Ambit Biosciences

Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate.

The Institute of Cancer Research

Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase.

Glaxosmithkline

Discovery of potent and bioavailable GSK-3beta inhibitors.

Roche Palo Alto

A quantitative analysis of kinase inhibitor selectivity.

Ambit Biosciences

The selectivity of protein kinase inhibitors: a further update.

University of Dundee

Discovery and development of aurora kinase inhibitors as anticancer agents.

Vertex Pharmaceuticals

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.

Harvard Medical School

Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold.

National Health Research Institutes

Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors.

Astrazeneca

Comprehensive analysis of kinase inhibitor selectivity.

Ambit Biosciences

Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors.

Ambit Biosciences

3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors.

Mitsubishi Tanabe Pharma

Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.

Martin-Luther-University Halle-Wittenberg

Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.

The Institute of Cancer Research

Thieno[3,2-c]pyrazoles: a novel class of Aurora inhibitors with favorable antitumor activity.

Nerviano Medical Sciences Oncology

AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).

Ambit Biosciences

The discovery of the potent aurora inhibitor MK-0457 (VX-680).

Vertex Pharmaceuticals

Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.

Glaxosmithkline

Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases.

The Institute of Cancer Research

An integrated computational approach to the phenomenon of potent and selective inhibition of aurora kinases B and C by a series of 7-substituted indirubins.

University of Athens

Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.

Bristol-Myers Squibb

Novel Aurora A and Protein Kinase C (?, ?1, ?2, and ?) Multitarget Inhibitors: Impact of Selenium Atoms on the Potency and Selectivity.

Mcgill University

Anticancer potential of indirubins in medicinal chemistry: Biological activity, structural modification, and structure-activity relationship.

Zunyi Medical University

Design, synthesis, and biological evaluation of novel pyrazolo [3,4-d]pyrimidine derivatives as potent PLK4 inhibitors for the treatment of TRIM37-amplified breast cancer.

Shenyang Pharmaceutical University

A small molecule-kinase interaction map for clinical kinase inhibitors.

Ambit Biosciences

Development and Therapeutic Potential of NUAKs Inhibitors.

University of Science and Technology (Ust)

Design, synthesis, and Structure-Activity Relationships (SAR) of 3-vinylindazole derivatives as new selective tropomyosin receptor kinases (Trk) inhibitors.

Jinan University

Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.

Beijing Normal University

The synthesis and anti-tumour properties of novel 4-substituted phthalazinones as Aurora B kinase inhibitors.

Lanzhou University

Discovery of novel 2,4-disubstituted pyrimidines as Aurora kinase inhibitors.

Lanzhou University

Discovery and optimization of heteroaryl piperazines as potent and selective PI3K? inhibitors.

Merck

Discovery of 4

TBA

Discovery of Inhibitors of Aurora/PLK Targets as Anticancer Agents.

Chengdu University

ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.

University of Florida

Synthesis and identification of 2,4-bisanilinopyrimidines bearing 2,2,6,6-tetramethylpiperidine-N-oxyl as potential Aurora A inhibitors.

Lanzhou University

A comprehensive review on Aurora kinase: Small molecule inhibitors and clinical trial studies.

Nirma University

ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.

Vertex Pharmaceuticals

ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.

Vertex Pharmaceuticals

Characterization of a highly selective inhibitor of the Aurora kinases.

Harvard Medical School

Discovery of N1-(4-((7-Cyclopentyl-6-(dimethylcarbamoyl)-7 H-pyrrolo[2,3- d]pyrimidin-2-yl)amino)phenyl)- N8-hydroxyoctanediamide as a Novel Inhibitor Targeting Cyclin-dependent Kinase 4/9 (CDK4/9) and Histone Deacetlyase1 (HDAC1) against Malignant Cancer.

Nankai University

Synthesis and biological evaluation of fused oxepinocoumarins as free radicals scavengers.

Aristotle University of Thessaloniki

[125I]Tyr10-cortistatin14 labels all five somatostatin receptors.

Novartis Pharma

Anchored plasticity opens doors for selective inhibitor design in nitric oxide synthase.

The Scripps Research Institute

Use of binding enthalpy to drive an allosteric transition.

University of Maryland