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Biotransformation of Daclatasvir In Vitro and in Nonclinical Species: Formation of the Main Metabolite by Pyrrolidine δ-Oxidation and Rearrangement.

Autor: Li W; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Zhao W; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Liu X; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Huang X; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Lopez OD; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Leet JE; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Fancher RM; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Nguyen V; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Goodrich J; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Easter J; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Hong Y; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Caceres-Cortes J; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Chang SY; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Ma L; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Belema M; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Hamann LG; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Gao M; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Zhu M; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Shu YZ; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Humphreys WG; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut., Johnson BM; Departments of Pharmaceutical Candidate Optimization (W.L., W.Z., X.L., X.H., R.M.F., J.C.-C., S.Y.C., L.M., M.Z., Y.-Z.S., W.G.H., B.M.J.), Synthesis and Analysis Technology Team (J.E.L.), Virology (M.G.), and Chemistry (O.D.L., V.N., J.G., J.E., Y.H., M.B., L.G.H.), Bristol-Myers Squibb Company, Wallingford, Connecticut benjamin.m.johnson@bms.com.

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals [Drug Metab Dispos] 2016 Jun; Vol. 44 (6), pp. 809-20. Date of Electronic Publication: 2016 Mar 30.

HPLC biogram analysis: a powerful tool used for hit confirmation in early drug discovery.

Autor: Leet JE; Bristol-Myers Squibb Company, Wallingford, CT, USA john.leet@bms.com., Belcastro JV; Bristol-Myers Squibb Company, Wallingford, CT, USA., Dowling CJ; Bristol-Myers Squibb Company, Wallingford, CT, USA., Nemeth GA; Bristol-Myers Squibb Company, Tampa, FL, USA., Weller HN; Bristol-Myers Squibb Company, Princeton, NJ, USA.

Publikováno v: Journal of biomolecular screening [J Biomol Screen] 2015 Jun; Vol. 20 (5), pp. 681-7. Date of Electronic Publication: 2015 Feb 13.

Isolation and structures of axistatins 1-3 from the Republic of Palau marine sponge Agelas axifera Hentschel .

Autor: Pettit GR; Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, P.O. Box 871604, Tempe, Arizona 85287-1604, USA. bpettit@asu.edu, Tang Y, Zhang Q, Bourne GT, Arm CA, Leet JE, Knight JC, Pettit RK, Chapuis JC, Doubek DL, Ward FJ, Weber C, Hooper JN

Publikováno v: Journal of natural products [J Nat Prod] 2013 Mar 22; Vol. 76 (3), pp. 420-4. Date of Electronic Publication: 2013 Feb 14.