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Page 1
Synthesis and biological activity of analogues of the antimicrotubule agent N,beta,beta-trimethyl-L-phenylalanyl-N(1)-[(1S,2E)-3-carboxy-1-isopropylbut-2-enyl]- N(1),3-dimethyl-L-valinamide (HTI-286).
Zask A, Birnberg G, Cheung K, Kaplan J, Niu C, Norton E, Suayan R, Yamashita A, Cole D, Tang Z, Krishnamurthy G, Williamson R, Khafizova G, Musto S, Hernandez R, Annable T, Yang X, Discafani C, Beyer C, Greenberger LM, Loganzo F, Ayral-Kaloustian S. Zask A, et al. Among authors: discafani c. J Med Chem. 2004 Sep 9;47(19):4774-86. doi: 10.1021/jm040056u. J Med Chem. 2004. PMID: 15341492
HTI-286, a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.
Loganzo F, Discafani CM, Annable T, Beyer C, Musto S, Hari M, Tan X, Hardy C, Hernandez R, Baxter M, Singanallore T, Khafizova G, Poruchynsky MS, Fojo T, Nieman JA, Ayral-Kaloustian S, Zask A, Andersen RJ, Greenberger LM. Loganzo F, et al. Among authors: discafani cm. Cancer Res. 2003 Apr 15;63(8):1838-45. Cancer Res. 2003. PMID: 12702571
Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).
Wissner A, Overbeek E, Reich MF, Floyd MB, Johnson BD, Mamuya N, Rosfjord EC, Discafani C, Davis R, Shi X, Rabindran SK, Gruber BC, Ye F, Hallett WA, Nilakantan R, Shen R, Wang YF, Greenberger LM, Tsou HR. Wissner A, et al. Among authors: discafani c. J Med Chem. 2003 Jan 2;46(1):49-63. doi: 10.1021/jm020241c. J Med Chem. 2003. PMID: 12502359
2-(Quinazolin-4-ylamino)-[1,4]benzoquinones as covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2.
Wissner A, Floyd MB, Johnson BD, Fraser H, Ingalls C, Nittoli T, Dushin RG, Discafani C, Nilakantan R, Marini J, Ravi M, Cheung K, Tan X, Musto S, Annable T, Siegel MM, Loganzo F. Wissner A, et al. Among authors: discafani c. J Med Chem. 2005 Dec 1;48(24):7560-81. doi: 10.1021/jm050559f. J Med Chem. 2005. PMID: 16302797
27 results