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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: chang h. 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
Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group.
Milkiewicz KL, Aimone LD, Albom MS, Angeles TS, Chang H, Grobelny JV, Husten J, Losardo C, Miknyoczki S, Murthy S, Rolon-Steele D, Underiner TL, Weinberg LR, Worrell CS, Zeigler KS, Dorsey BD. Milkiewicz KL, et al. Among authors: chang h. Bioorg Med Chem. 2011 Nov 1;19(21):6274-84. doi: 10.1016/j.bmc.2011.09.006. Epub 2011 Sep 13. Bioorg Med Chem. 2011. PMID: 21967808
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent.
Hudkins RL, Becknell NC, Zulli AL, Underiner TL, Angeles TS, Aimone LD, Albom MS, Chang H, Miknyoczki SJ, Hunter K, Jones-Bolin S, Zhao H, Bacon ER, Mallamo JP, Ator MA, Ruggeri BA. Hudkins RL, et al. Among authors: chang h. J Med Chem. 2012 Jan 26;55(2):903-13. doi: 10.1021/jm201449n. Epub 2012 Jan 6. J Med Chem. 2012. PMID: 22148921
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: chang h. Cancer Res. 2003 Sep 15;63(18):5978-91. Cancer Res. 2003. PMID: 14522925
Antiangiogenic and antitumor efficacy of EphA2 receptor antagonist.
Dobrzanski P, Hunter K, Jones-Bolin S, Chang H, Robinson C, Pritchard S, Zhao H, Ruggeri B. Dobrzanski P, et al. Among authors: chang h. Cancer Res. 2004 Feb 1;64(3):910-9. doi: 10.1158/0008-5472.can-3430-2. Cancer Res. 2004. PMID: 14871820
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