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Webb Lab: Publications

    2011

  • Fan L, Lagisetti C, Edwards CC, Webb TR, Potter PM. Sudemycins, Novel Small Molecule Analogues of FR901464, induce Alternative Gene Splicing. ACS Chem. Biol. Mar 7, 2011. (epub) PMID: 21344922

  • Goronga T, Boyd VA, Lagisetti C, Jeffries C, Webb TR. Radiosynthesis of antitumor spliceosome modulators. Appl. Radiat. Isot. 69(9): 1231-1234, 2011. PMID: 21531567

  • Slavish PJ, Price JE, Jiang Q, Cui X, Morris SW, Webb TR. Synthesis of an Aryloxy Oxo Pyrimidinone Library that Displays ALK-selective Inhibition in an Insulin Receptor Superfamily Kinase Panel. Bioorg. Med. Chem. Lett. 21: 4592-4596, 2011.

  • Gundluru MK, Pourpak A., Cui X., Morris SM, Webb, TR. Design, synthesis and initial biological evaluation of a novel pladienolide analog scaffold Med. Chem. Commun., 2011, 6 (6), pp 582–589, DOI: 10.1039/C1MD00040C

  • Slavish, PJ, Price JE, Jiang Q, Cui X, Morris SW, Webb TR. Synthesis of an Aryloxy Oxo Pyrimidinone Library that Displays ALK-selective Inhibition in an Insulin Receptor Superfamily Kinase Panel. Bioorg. Med. Chem. Lett., 2011 21, 4592-4596.

  • Goronga T, Boyd VA, Lagisetti C, Jeffries C, Webb TR. Radiosynthesis of antitumor spliceosome modulators. Appl. Radiat. Isot. 69(9): 1231-1234, 2011. PMCID: PMC3105125 (Available 9/1/2012)

  • Fan L, Lagisetti C, Edwards CC, Webb TR, Potter PM. Sudemycins, Novel Small Molecule Analogues of FR901464, induce Alternative Gene Splicing. ACS Chem. Biol. 2011, 6 (6), pp 582–589, PMID: 21344922


  • 2010

  • Slavish PJ, Price JE, Hanumesh P, Webb TR. Efficient synthesis of pyrazolopyrimidine libraries. J Comb Chem 12(6):807-809, 2010. PMID: 20804211.

  • Young BM, Hyatt JL, Bouck DC, Chen T, Hanumesh P, Price J, Boyd VA, Potter PM, Webb TR. Structure-Activity Relationships of Substituted 1-Pyridyl-2-phenyl-1,2-ethanediones: Potent, Selective Carboxylesterase Inhibitors. J. Med. Chem. 53(24): 8709-8715, 2010. PMCID: PMC3022373 (available on 12/1/2011)

  • Kasinathan RS, Goronga T, Messerli SM, Webb TR, Greenberg RM. Modulation of a Schistosoma mansoni multidrug transporter by the antischistosomal drug praziquantel. FASEB J. 24(1):128-135, 2010. PMCID: PMC2797036


  • 2009

  • Aragon AD, Imani RA, Blackburn VR, Cupit PM, Melman SD, Goronga T, Webb TR, Loker ES, Cunningham C. Towards an understanding of the mechanism of action of praziquantel. Mol. Biochem. Parasitol. 164(1):57-65, 2009. PMCID: PMC2886009

  • Webb TR, Slavish J, George RE, Look AT, Xue L, Jiang Q, Cui X, Rentrop WB, Morris SW. Anaplastic Lymphoma Kinase: role in cancer pathogenesis and small-molecule inhibitor development for therapy. Expert Rev. Anticancer Ther. 9(3):331-356, 2009. PMCID: PMC2780428

  • Slavish PJ, Jiang Q, Cui X, Morris SW, Webb TR. Design and synthesis of a novel tyrosine kinase inhibitor template. Bioorg. Med. Chem. 17(9):3308-3316, 2009. PMCID: PMC2696309

  • Lee JY, Im I, Webb TR, McGrath D, Song MR, Kim YC. Combinatorial synthesis and biological evaluation of peptide-binding GPCR-targeted library. Bioorg. Chem. 37(3):90-95, 2009. PMID: 19467690

  • Boyd VA, Mason J, Hanumesh P, Price J, Russell CJ, Webb TR. 2-Substituted-4,5-dihydroxypyrimidine-6-carboxamide antiviral targeted libraries. J. Comb. Chem. 2009 Nov-Dec; 11(6): 1100-4.PMID: 19754047

  • Lagisetti C, Pourpak A, Goronga T, Jiang Q, Cui Xiaoli, Hyle J, Lahti J, Morris S, Webb T. Synthetic mRNA Splicing Modulator Compounds with In Vivo Anti-tumor Activity. J. Med. Chem. 52 (22): 6979-6990, 2009. PMCID: 19877647


  • 2008

  • George RE, Sanda T, Hanna M, Frohling S, Luther II W, Zhang J, Ahn Y, Zhou W, London WB, McGrady P, Xue L, Zozulya S, Gregor VE, Webb TR, Gray NS, Gilliland DG, Diller L, Greulich H, Morris SW, Myerson M, Look AT. Activating mutations in ALK provide a therapeutic target in neuroblastoma: Nature, 455:975-978, 2008. PMCID: PMC2587486

  • Lagisetti C, Pourpak A, Jiang Q, Cui X, Goronga T, Morris SW, Webb TR. Anti-tumor compounds based on a natural product consensus pharmacophore. J. Med. Chem. 51(19):6220-6224, 2008. NIHMSID: NIHMS86341.

  • Webb TR, Venegas RE, Wang J, Deschenes A. Generation of new synthetic scaffolds using framework libraries selected and refined via medicinal chemist synthetic expertise. J. Chem. Inf. Model. 48(4):882-888, 2008. PMID: 18335978


  • 2007

  • Webb TR, McGrath D, Wang J, Li R, Jiang L, Sviridov S. Application of a novel design paradigm to generate general nonpeptide combinatorial scaffolds mimicking beta turns: Part II; Synthesis of agonists of melanocortin receptors. J. Comb. Chem. 9:704-710, 2007. PMID: 17429950


  • 2006

  • Zhu T, Yan Z, Chucholowski A, Webb TR, Li R. Polymer-supported synthesis of pyridone-focused libraries as inhibitors of anaplastic lymphoma kinase. J. Combinat. Chem. 8(3):401-409, 2006. PMID: 16677010

  • Li R, Xue L, Zhu T, Jiang Q, Cui X, Yan Z, McGee D, Wang J, Gantla V, Pickens JC, McGrath D, Chucholowski A, Morris SW, Webb TR. Design and synthesis of 5-Aryl-Pyridone-Carboxamides as Inhibitors of Anaplastic Lymphoma Kinase (ALK). J. Med. Chem. 49(3):1006-1015, 2006. PMID: 16451066


  • 2005

  • Webb TR. Current directions in the evolution of compound libraries. Curr. Opin. Drug Discovery Develop. 8(3):303-308, 2005. PMID: 15892244

  • Gurova KV, Hill JE, Prokvolit A, Burdelya LG, Guo C, Samoylova E, Khodyakova AV, Ganapathi R, Ganapathi M, Tararova ND, Bosykh D, Lvovsky D, Webb TR, Didonato J, Gudkov AV. Small molecule, reactivating p53 in renal cell carcinoma, reveals a new NF-κB-dependent mechanism of p53 suppression in tumors. Proc. Natl. Acad. Sci. USA. 102(48):17448-17453, 2005. PMID: 16287968


  • 2004

  • Webb TR, Moran T, Huang CQ, McCarthy JR, Grigoriadis DE, Chen C. Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor. Bioorg. Med. Chem. Lett. 14(15):3869-73, 2004. PMID: 15225687

  • Webb, T. R., Some principles related to chemogenomics in compound library and template design for GPCRs. Methods and Principles in Medicinal Chemistry, 2004, 22, (Chemogenomics in Drug Discovery), 313-324.

  • Khasanov AB, Ramirez-Weinhouse MM, Webb TR, Thiruvazhi M. Novel asymmetric approach to proline-derived Spiro-β-lactams. J.Org. Chem. 69:5766-5769, 2004. PMID: 15307755

  • Chen C, Wilcoxen KM, Huang CQ, Xie Y-F, McCarthy JR, Webb TR, Zhu Y-F, Saunders J, Liu X-J, Chen T-K, Bozigian H, Grigoriadis DE. Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure-activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists. J. Med. Chem. 47:4787-4798, 2004. PMID: 15341493

  • Im I, Webb TR, Gong Y-D, Kim J-I, Kim Y-C. Solid-phase synthesis of tetrahydro-1,4-benzodiazepine-2-one derivatives as a β-turn peptidomimic library. J. Combinat. Chem. 6(2):207-213, 2004. PMID: 15002968


  • 2003

  • Webb TR, Lvovskiy D, Kim S-A, Ji X,; Melman N, Linden J, Jacobson KA. Quinazolines as adenosine receptor antagonists: SAR and selectivity for A2B receptors. Bioorg. Med.Chem. 11(1):77-85, 2003. PMID: 12467710

  • Huang CQ, Wilcoxen K, McCarthy JR, Haddach M, Webb TR, Gu J, Xie Y-F, Grigoriadis DE, Chen C. Synthesis and SAR of 8-arylquinolines as potent corticotropin releasing factor 1 (CRF1) receptor antagonists. Bioorg. Med. Chem. Lett. 13:3375-3379, 2003. PMID: 12951129

  • Chianelli D, Kim Y-C, Lvovskiy D, Webb TR. Application of a novel design paradigm to generate general nonpeptide combinatorial scaffolds mimicking beta turns: synthesis of ligands for somatostatin receptors. Bioorg. Med. Chem. 11(23):5059-5068, 2003. PMID: 14604669


  • 2001

  • Webb TR, Lvovskiy, D., Melman, N., Ji, X., Linden, J., Jacobson, K. A., Discovery of new antagonists of the adenosine A2B receptor. Abstracts of Papers, 221st ACS National Meeting, San Diego, CA, United States, April 1-5, 2001 2001, MEDI-030.


    2000

  • Webb TR, Melman N, Lvovskiy D, Ji X, Jacobson K A. The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family. Bioorg. Med. Chem. Lett., 10 (1):31-34, 2000. PMID: 10636237


  • 1996

  • Whitten JP, Xie YF, Erickson PE, Webb TR, Souza EB, Grigoriadis DE, McCarthy JR. Rapid microscale synthesis, a new method for lead optimization using robotics and solution phase chemistry: application to the synthesis and optimization of corticotropin releasing factor 1 receptor antagonists. J. Med. Chem. 39:4354-4357, 1996. PMID: 8893828

  • Chen C, Dagnino R, De Souza EB, Grigoriadis DE, Huang CQ, Kim K, Liu Z, Moran T, Webb TR, Whitten J, Zie YF, McCarthy JR. Design and synthesis of a series of non-peptide high-affinity human corticotropin-releasing factor-1 receptor antagonists. J. Med. Chem. 39:4358-4360, 1996. PMID: 8893829


  • 1994

  • Dagnino, R., Jr., Webb TR, Improved synthesis of arginine peptide aldehydes. Tetrahedron Letters 1994, 35, (14), 2125-8.


  • 1993

  • Reiner, J., Dagnino, R., Jr., Goldman, E., Webb TR, Facile determination of the optical purity of a-N-Boc-amino aldehydes. Tetrahedron Letters 1993, 34, (34), 5425-8.


  • 1992

  • Murphy, A. M., Dagnino, R., Jr., Vallar, P. L., Trippe, A. J., Sherman, S. L., Lumpkin, R. H., Tamura, S. Y., Webb, T. R., Automated synthesis of peptide C-terminal aldehydes. Journal of the American Chemical Society 1992, 114, (8), 3156-7.


  • 1991

  • Webb, T. R., Eigenbrot, C., Conformationally restricted arginine analogs. Journal of Organic Chemistry 1991, 56, (9), 3009-16.


  • 1990

  • Rawson, T. E., Webb, T. R., The synthesis of 5'-homo-2'-deoxycytidine. Nucleosides & Nucleotides 1990, 9, (1), 89-96.


  • 1988

  • Webb, T. R., Mitsuya, H., Broder, S., 1-(2,3-Anhydro-b-D-lyxofuranosyl)cytosine derivatives as potential inhibitors of the human immunodeficiency virus. Journal of Medicinal Chemistry 1988, 31, (7), 1475-9.

  • Webb, T. R., The direct conversion of 5'-O-trityl-3'-keto-2'-deoxythymidine to 1-(2-deoxy-3-methyl-b-D-xylosyl)thymine. Tetrahedron Letters 1988, 29, (31), 3769-72.


  • 1987

  • Webb, T. R., Jhurani, P., Ng, P. G., Template-primer analogs as substrates for DNA polymerase. Nucleic Acids Research 1987, 15, (10), 3997-4006.

  • Matteucci, M. D., Webb, T. R., Synthesis and crosslinking properties of a deoxyoligonucleotide containing N6,N6-ethanodeoxyadenosine. Tetrahedron Letters 1987, 28, (22), 2469-72.

  • Bischofberger, N., Ng, P. G., Webb, T. R., Matteucci, M. D., Cleavage of single stranded oligonucleotides by EcoRI restriction endonuclease. Nucleic Acids Research 1987, 15, (2), 709-16.


  • 1986

  • Webb, T. R., Matteucci, M. D., Sequence-specific cross-linking of deoxyoligonucleotides via hybridization-triggered alkylation. Journal of the American Chemical Society 1986, 108, (10), 2764-5.

  • Webb, T. R., Matteucci, M. D., Hybridization triggered cross-linking of deoxyoligonucleotides. Nucleic Acids Research 1986, 14, (19), 7661-74.


  • 1985

  • Webb, TR, Regioselective synthesis of 2-substituted pyridines via Grignard addition to 1-(alkoxycarboxy)pyridinium salts. Tetrahedron Letters 1985, 26, (27), 3191-4.


  • 1984

  • Webb, TR, A simple synthesis of potassium (+-)-3-methoxy-4-hydroxyphenylethyleneglycol-4-sulfate. Synthesis 1984, (3), 213-14.

  • McMurry, J. E., Webb, T. R., Synthesis of a tricyclic aphidicolin analog which inhibits DNA synthesis in vitro. Journal of Medicinal Chemistry 1984, 27, (10), 1367-9.

  • Grzeskowiak, K., Webb, T. R., Orgel, L. E., Template-directed synthesis with 2-aminoadenosine. Journal of Molecular Evolution 1984, 21, (1), 81-3.


  • 1983

  • Webb, T. R., A simple synthesis of 5-amino-4-imidazolecarboxamide riboside-5'-triphosphate: the proposed alarmone for 10-formyl-tetrahydrofolate deficiency. Nucleosides & Nucleotides 1983, 2, (3), 291-4.


  • 1981

  • Webb, T. R., Orgel, L. E., Template directed reactions of 2-aminoadenylic acid derivatives. Nucleic Acids Research 1982, 10, (14), 4413-22.


  • 1977

  • Bartlett, P. A., Green, F. R., III, Webb, T. R., A mild, oxidative nitro-to-carbonyl conversion and a new prostaglandin synthon. Tetrahedron Letters 1977, (4), 331-4.


United States Patents

  • 7,074,797 Pyrazolopyrimidines as CRF receptor antagonists
  • 6,872,827 Somatostatin Analogue Compounds
  • 6,664,261 Pyrazolopyrimidines as CRF antagonists
  • 6,469,166 Thiophenopyrimidines
  • 6,255,310 Thiophenopyrimidines
  • 6,211,195 CRF antagonistic thiophenopyridines
  • 5,955,576 Inhibitors of thrombosis
  • 5,886,146 Inhibitors of thrombosis
  • 5,883,077 Inhibitors of factor Xa
  • 5,869,454 Arginine keto-amide enzyme inhibitors
  • 5,795,905 CRF receptor antagonists and methods relating thereto
  • 5,739,112 Inhibitors of factor Xa
  • 5,731,413 Method for synthesis of peptidyl aldehydes
  • 5,714,580 Trypsin Inhibitors
  • 5,670,479 α-Ketoamide derivatives as inhibitors of thrombosis
  • 5,656,600 α-Ketoamide derivatives as inhibitors of thrombosis
  • 5,597,804 N-Sulfonylarginine keto-amide compounds
  • 5,514,777 Methods of synthesis of peptidyl aldehydes
  • 5,534,498 Trypsin inhibitors
  • 5,514,777 Methods of synthesis of peptidyl argininals
  • 5,492,895 Inhibitors of thrombosis
  • 5,371,072 Asp-Pro-Arg a-keto-amide enzyme inhibitors
  • 5,367,072 Reagents for automated synthesis of peptide analogs
  • 5,283,293 Reagents for automated synthesis of peptide analogs
  • 5,120,859 Chimeric amino acid analogues
  • 4,659,774 Support for solid-phase synthesis