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A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clinical candidate CEP-7055.
Gingrich DE, Reddy DR, Iqbal MA, Singh J, Aimone LD, Angeles TS, Albom M, Yang S, Ator MA, Meyer SL, Robinson C, Ruggeri BA, Dionne CA, Vaught JL, Mallamo JP, Hudkins RL. Gingrich DE, et al. Among authors: yang s. J Med Chem. 2003 Dec 4;46(25):5375-88. doi: 10.1021/jm0301641. J Med Chem. 2003. PMID: 14640546
Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases.
Dandu R, Zulli AL, Bacon ER, Underiner T, Robinson C, Chang H, Miknyoczki S, Grobelny J, Ruggeri BA, Yang S, Albom MS, Angeles TS, Aimone LD, Hudkins RL. Dandu R, et al. Among authors: yang s. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1916-21. doi: 10.1016/j.bmcl.2008.02.001. Epub 2008 Feb 7. Bioorg Med Chem Lett. 2008. PMID: 18308565
CEP-7055: a novel, orally active pan inhibitor of vascular endothelial growth factor receptor tyrosine kinases with potent antiangiogenic activity and antitumor efficacy in preclinical models.
Ruggeri B, Singh J, Gingrich D, Angeles T, Albom M, Yang S, Chang H, Robinson C, Hunter K, Dobrzanski P, Jones-Bolin S, Pritchard S, Aimone L, Klein-Szanto A, Herbert JM, Bono F, Schaeffer P, Casellas P, Bourie B, Pili R, Isaacs J, Ator M, Hudkins R, Vaught J, Mallamo J, Dionne C. Ruggeri B, et al. Among authors: yang s. Cancer Res. 2003 Sep 15;63(18):5978-91. Cancer Res. 2003. PMID: 14522925
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