PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after…
A novel compound with therapeutic potential for the treatment of solid tumors and other diseases where angiogenesis plays an important role, PTK787/ZK 222584 is very well tolerated and does not impair wound healing.
Use of a pharmacophore model for the design of EGF-R tyrosine kinase inhibitors: 4-(phenylamino)pyrazolo[3,4-d]pyrimidines.
- P. Traxler, G. Bold, P. Furet
- Biology, ChemistryJournal of Medicinal Chemistry
- 24 October 1997
4-(Phenylamino)-1H-pyrazolo[3,4-d]pyrimidines represent a new class of highly potent tyrosine kinase inhibitors which preferentially inhibit the EGF-mediated signal transduction pathway and have the potential for further evaluation as anticancer agents.
Tyrosine kinase inhibitors: From rational design to clinical trials
- P. Traxler, G. Bold, J. Zimmermann
- Biology, ChemistryMedicinal research reviews (Print)
- 1 November 2001
Three successful examples of drug design at Novartis using a tyrosine kinase as a molecular target are described and promising data from phase I and II clinical trials in CML patients support the fact that the STI571 represents a new treatment modality for CML.
Purification and characterization of dihydrodipicolinate synthase from pea.
- C. Dereppe, G. Bold, O. Ghisalba, E. Ebert, H. Schär
- Chemistry, BiologyPlant Physiology
- 1 March 1992
Dihydrodipicolinate synthase from pea is highly specific for the substrates pyruvate and l-aspartate-beta-semialdehyde; it follows Michaelis-Menten kinetics for both substrates.
Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors.
- P. Manley, P. Furet, K. Thierauch
- Chemistry, BiologyJournal of Medicinal Chemistry
- 20 November 2002
The anthranilamides 5 and 7 represent a new structural class of VEGFR kinase inhibitors, which possess potent antiangiogenic and antitumor properties, in a mouse orthotopic model of melanoma.
Inhibition of chronic and acute skin inflammation by treatment with a vascular endothelial growth factor receptor tyrosine kinase inhibitor.
- C. Halin, H. Fahrngruber, M. Detmar
- Biology, MedicineAmerican Journal of Pathology
- 1 July 2008
Results demonstrate for the first time that VEGF receptor tyrosine-kinase inhibitors might be used to treat patients with inflammatory skin disorders such as psoriasis.
Identification of a new chemical class of potent angiogenesis inhibitors based on conformational considerations and database searching.
- P. Furet, G. Bold, F. Hofmann, P. Manley, T. Meyer, K. Altmann
- Biology, ChemistryBioorganic & Medicinal Chemistry Letters
- 15 September 2003
PTK 787 / ZK 222584 , a Novel and Potent Inhibitor of Vascular Endothelial Growth Factor Receptor Tyrosine Kinases , Impairs Vascular Endothelial Growth Factor-induced Responses and Tumor Growth…
A novel compound with therapeutic potential for the treatment of solid tumors and other diseases where angiogenesis plays an important role, PTK787/ZK 222584 is very well tolerated and does not impair wound healing.
Synthesis and biological evaluation of highly potent analogues of epothilones B and D.
- K. Altmann, G. Bold, G. Caravatti, A. Flörsheimer, V. Guagnano, M. Wartmann
- Chemistry, BiologyBioorganic & Medicinal Chemistry Letters
- 18 December 2000
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