Format
Sort by
Items per page

Send to

Choose Destination

Search results

Items: 1 to 50 of 74

1.

Antitumor activity and apoptotic action of coelomic fluid from the earthworm Dendrobaena veneta against A549 human lung cancer cells.

Fiołka MJ, Rzymowska J, Bilska S, Lewtak K, Dmoszyńska-Graniczka M, Grzywnowicz K, Kaźmierski W, Urbanik-Sypniewska T.

APMIS. 2019 Jun;127(6):435-448. doi: 10.1111/apm.12941. Epub 2019 Mar 28.

PMID:
30803036
2.

Biological and Structural Characterization of Rotamers of C-C Chemokine Receptor Type 5 (CCR5) Inhibitor GSK214096.

Kazmierski WM, Danehower S, Duan M, Ferris RG, Elitzin V, Minick D, Sharp M, Stewart E, Villeneuve M.

ACS Med Chem Lett. 2014 Oct 28;5(12):1296-9. doi: 10.1021/ml5004124. eCollection 2014 Dec 11.

3.

Novel spiroketal pyrrolidine GSK2336805 potently inhibits key hepatitis C virus genotype 1b mutants: from lead to clinical compound.

Kazmierski WM, Maynard A, Duan M, Baskaran S, Botyanszki J, Crosby R, Dickerson S, Tallant M, Grimes R, Hamatake R, Leivers M, Roberts CD, Walker J.

J Med Chem. 2014 Mar 13;57(5):2058-73. doi: 10.1021/jm4013104. Epub 2014 Feb 26.

PMID:
24568313
4.

Preclinical characterization of GSK2336805, a novel inhibitor of hepatitis C virus replication that selects for resistance in NS5A.

Walker J, Crosby R, Wang A, Woldu E, Vamathevan J, Voitenleitner C, You S, Remlinger K, Duan M, Kazmierski W, Hamatake R.

Antimicrob Agents Chemother. 2014;58(1):38-47. doi: 10.1128/AAC.01363-13. Epub 2013 Oct 14.

5.

Pharmacological disruption of hepatitis C NS5A protein intra- and intermolecular conformations.

Bhattacharya D, Ansari IH, Hamatake R, Walker J, Kazmierski WM, Striker R.

J Gen Virol. 2014 Feb;95(Pt 2):363-72. doi: 10.1099/vir.0.054569-0. Epub 2013 Aug 30.

PMID:
23997183
6.

Synthesis and antiviral activity of novel HCV NS3 protease inhibitors with P4 capping groups.

Li X, Liu Y, Zhang YK, Plattner JJ, Baker SJ, Bu W, Liu L, Zhou Y, Ding CZ, Zhang S, Kazmierski WM, Hamatake R, Duan M, Wright LL, Smith GK, Jarvest RL, Ji JJ, Cooper JP, Tallant MD, Crosby RM, Creech K, Wang A.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7351-6. doi: 10.1016/j.bmcl.2012.10.075. Epub 2012 Oct 22.

PMID:
23142614
7.

Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants.

Kazmierski WM, Hamatake R, Duan M, Wright LL, Smith GK, Jarvest RL, Ji JJ, Cooper JP, Tallant MD, Crosby RM, Creech K, Wang A, Li X, Zhang S, Zhang YK, Liu Y, Ding CZ, Zhou Y, Plattner JJ, Baker SJ, Bu W, Liu L.

J Med Chem. 2012 Apr 12;55(7):3021-6. doi: 10.1021/jm201278q. Epub 2012 Apr 3.

PMID:
22471376
8.

Discovery of novel P3-oxo inhibitor of hepatitis C virus NS3/4A serine protease.

Duan M, Kazmierski W, Crosby R, Gartland M, Ji J, Tallant M, Wang A, Hamatake R, Wright L, Wu M, Zhang YK, Ding CZ, Li X, Liu Y, Zhang S, Zhou Y, Plattner JJ, Baker SJ.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2993-6. doi: 10.1016/j.bmcl.2012.02.039. Epub 2012 Feb 22.

PMID:
22425454
9.

Discovery of a novel series of cyclic urea as potent CCR5 antagonists.

Duan M, Kazmierski WM, Tallant M, Jun JH, Edelstein M, Ferris R, Todd D, Wheelan P, Xiong Z.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6381-5. doi: 10.1016/j.bmcl.2011.08.096. Epub 2011 Aug 28.

PMID:
21930378
10.

Discovery of novel pyridyl carboxamides as potent CCR5 antagonists and optimization of their pharmacokinetic profile in rats.

Duan M, Kazmierski WM, Chong PY, Deanda F, Edelstein M, Ferris R, Peckham J, Wheelan P, Xiong Z, Zhang H, Nishizawa R, Takaoka Y.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6470-5. doi: 10.1016/j.bmcl.2011.08.080. Epub 2011 Aug 23.

PMID:
21920742
11.

TARGETING THE NS5A PROTEIN OF HCV: AN EMERGING OPTION.

Cordek DG, Bechtel JT, Maynard AT, Kazmierski WM, Cameron CE.

Drugs Future. 2011 Sep;36(9):691-711.

12.

Novel 4,4-disubstituted piperidine-based C-C chemokine receptor-5 inhibitors with high potency against human immunodeficiency virus-1 and an improved human ether-a-go-go related gene (hERG) profile.

Kazmierski WM, Anderson DL, Aquino C, Chauder BA, Duan M, Ferris R, Kenakin T, Koble CS, Lang DG, McIntyre MS, Peckham J, Watson C, Wheelan P, Spaltenstein A, Wire MB, Svolto A, Youngman M.

J Med Chem. 2011 Jun 9;54(11):3756-67. doi: 10.1021/jm200279v. Epub 2011 May 17.

PMID:
21539377
13.

Synthesis and SAR of acyclic HCV NS3 protease inhibitors with novel P4-benzoxaborole moieties.

Li X, Zhang S, Zhang YK, Liu Y, Ding CZ, Zhou Y, Plattner JJ, Baker SJ, Bu W, Liu L, Kazmierski WM, Duan M, Grimes RM, Wright LL, Smith GK, Jarvest RL, Ji JJ, Cooper JP, Tallant MD, Crosby RM, Creech K, Ni ZJ, Zou W, Wright J.

Bioorg Med Chem Lett. 2011 Apr 1;21(7):2048-54. doi: 10.1016/j.bmcl.2011.02.006. Epub 2011 Feb 23.

PMID:
21353550
14.

Synthesis and evaluation of 2-phenyl-1,4-butanediamine-based CCR5 antagonists for the treatment of HIV-1.

Tallant MD, Duan M, Freeman GA, Ferris RG, Edelstein MP, Kazmierski WM, Wheelan PJ.

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1394-8. doi: 10.1016/j.bmcl.2011.01.030. Epub 2011 Jan 11.

PMID:
21292480
15.

Spirodiketopiperazine-based CCR5 antagonist: discovery of an antiretroviral drug candidate.

Nishizawa R, Nishiyama T, Hisaichi K, Minamoto C, Matsunaga N, Takaoka Y, Nakai H, Jenkinson S, Kazmierski WM, Tada H, Sagawa K, Shibayama S, Fukushima D, Maeda K, Mitsuya H.

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1141-5. doi: 10.1016/j.bmcl.2010.12.109. Epub 2010 Dec 28.

PMID:
21256008
16.

Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease.

Ding CZ, Zhang YK, Li X, Liu Y, Zhang S, Zhou Y, Plattner JJ, Baker SJ, Liu L, Duan M, Jarvest RL, Ji J, Kazmierski WM, Tallant MD, Wright LL, Smith GK, Crosby RM, Wang AA, Ni ZJ, Zou W, Wright J.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7317-22. doi: 10.1016/j.bmcl.2010.10.071. Epub 2010 Oct 21.

PMID:
21067923
17.

Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): modification of the acyl portion.

Duan M, Peckham J, Edelstein M, Ferris R, Kazmierski WM, Spaltenstein A, Wheelan P, Xiong Z.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7401-4. doi: 10.1016/j.bmcl.2010.10.042. Epub 2010 Oct 21.

PMID:
21055933
18.

Synthesis of new acylsulfamoyl benzoxaboroles as potent inhibitors of HCV NS3 protease.

Li X, Zhang YK, Liu Y, Zhang S, Ding CZ, Zhou Y, Plattner JJ, Baker SJ, Liu L, Bu W, Kazmierski WM, Wright LL, Smith GK, Jarvest RL, Duan M, Ji JJ, Cooper JP, Tallant MD, Crosby RM, Creech K, Ni ZJ, Zou W, Wright J.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7493-7. doi: 10.1016/j.bmcl.2010.10.007. Epub 2010 Oct 30.

PMID:
21041080
19.

Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (I): optimization of the amine portion.

Duan M, Peckham J, Edelstein M, Ferris R, Kazmierski WM, Spaltenstein A, Wheelan P, Xiong Z.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7397-400. doi: 10.1016/j.bmcl.2010.10.033. Epub 2010 Oct 12.

PMID:
21035337
20.

Novel macrocyclic HCV NS3 protease inhibitors derived from α-amino cyclic boronates.

Li X, Zhang YK, Liu Y, Ding CZ, Zhou Y, Li Q, Plattner JJ, Baker SJ, Zhang S, Kazmierski WM, Wright LL, Smith GK, Grimes RM, Crosby RM, Creech KL, Carballo LH, Slater MJ, Jarvest RL, Thommes P, Hubbard JA, Convery MA, Nassau PM, McDowell W, Skarzynski TJ, Qian X, Fan D, Liao L, Ni ZJ, Pennicott LE, Zou W, Wright J.

Bioorg Med Chem Lett. 2010 Oct 1;20(19):5695-700. doi: 10.1016/j.bmcl.2010.08.022. Epub 2010 Aug 10.

PMID:
20801653
21.

Synthesis and evaluation of novel alpha-amino cyclic boronates as inhibitors of HCV NS3 protease.

Li X, Zhang YK, Liu Y, Ding CZ, Li Q, Zhou Y, Plattner JJ, Baker SJ, Qian X, Fan D, Liao L, Ni ZJ, White GV, Mordaunt JE, Lazarides LX, Slater MJ, Jarvest RL, Thommes P, Ellis M, Edge CM, Hubbard JA, Somers D, Rowland P, Nassau P, McDowell B, Skarzynski TJ, Kazmierski WM, Grimes RM, Wright LL, Smith GK, Zou W, Wright J, Pennicott LE.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3550-6. doi: 10.1016/j.bmcl.2010.04.129. Epub 2010 May 20.

PMID:
20493689
22.

4,4-Disubstituted cyclohexylamine based CCR5 chemokine receptor antagonists as anti-HIV-1 agents.

Duan M, Aquino C, Dorsey GF Jr, Ferris R, Kazmierski WM.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):4988-92. doi: 10.1016/j.bmcl.2009.07.074. Epub 2009 Jul 18.

PMID:
19664920
23.

[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring.

Duan M, Aquino C, Ferris R, Kazmierski WM, Kenakin T, Koble C, Wheelan P, Watson C, Youngman M.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1610-3. doi: 10.1016/j.bmcl.2009.02.014. Epub 2009 Feb 10.

PMID:
19233649
24.

The relative activity of "function sparing" HIV-1 entry inhibitors on viral entry and CCR5 internalization: is allosteric functional selectivity a valuable therapeutic property?

Muniz-Medina VM, Jones S, Maglich JM, Galardi C, Hollingsworth RE, Kazmierski WM, Ferris RG, Edelstein MP, Chiswell KE, Kenakin TP.

Mol Pharmacol. 2009 Mar;75(3):490-501. doi: 10.1124/mol.108.052555. Epub 2008 Dec 8.

PMID:
19064629
25.

Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1.

Kazmierski WM, Aquino C, Chauder BA, Deanda F, Ferris R, Jones-Hertzog DK, Kenakin T, Koble CS, Watson C, Wheelan P, Yang H, Youngman M.

J Med Chem. 2008 Oct 23;51(20):6538-46. doi: 10.1021/jm800598a. Epub 2008 Sep 24.

PMID:
18811134
26.

New, potent P1/P2-morpholinone-based HIV-protease inhibitors.

Kazmierski WM, Furfine E, Spaltenstein A, Wright LL.

Bioorg Med Chem Lett. 2006 Oct 1;16(19):5226-30. Epub 2006 Aug 10.

PMID:
16904316
27.

Peptide, peptidomimetic and small-molecule drug discovery targeting HIV-1 host-cell attachment and entry through gp120, gp41, CCR5 and CXCR4.

Kazmierski WM, Kenakin TP, Gudmundsson KS.

Chem Biol Drug Des. 2006 Jan;67(1):13-26. Review.

PMID:
16492145
28.

Discovery of next generation inhibitors of HIV protease.

Spaltenstein A, Kazmierski WM, Miller JF, Samano V.

Curr Top Med Chem. 2005;5(16):1589-607. Review.

PMID:
16375744
29.

The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor.

Watson C, Jenkinson S, Kazmierski W, Kenakin T.

Mol Pharmacol. 2005 Apr;67(4):1268-82. Epub 2005 Jan 11.

PMID:
15644495
30.

Discovery of potent pyrrolidone-based HIV-1 protease inhibitors with enhanced drug-like properties.

Kazmierski WM, Andrews W, Furfine E, Spaltenstein A, Wright L.

Bioorg Med Chem Lett. 2004 Nov 15;14(22):5689-92.

PMID:
15482949
31.

Potent inhibitors of the HIV-1 protease incorporating cyclic urea P1-P2 scaffold.

Kazmierski WM, Furfine E, Gray-Nunez Y, Spaltenstein A, Wright L.

Bioorg Med Chem Lett. 2004 Nov 15;14(22):5685-7.

PMID:
15482948
32.

Novel prodrug approach to amprenavir-based HIV-1 protease inhibitors via O-->N acyloxy migration of P1 moiety.

Kazmierski WM, Bevans P, Furfine E, Spaltenstein A, Yang H.

Bioorg Med Chem Lett. 2003 Aug 4;13(15):2523-6.

PMID:
12852957
33.

Recent progress in discovery of small-molecule CCR5 chemokine receptor ligands as HIV-1 inhibitors.

Kazmierski W, Bifulco N, Yang H, Boone L, DeAnda F, Watson C, Kenakin T.

Bioorg Med Chem. 2003 Jul 3;11(13):2663-76. Review. Erratum in: Bioorg Med Chem. 2003 Sep 1;11(18):4155.

PMID:
12788340
34.

CCR5 chemokine receptors: gatekeepers of HIV-1 infection.

Kazmierski WM, Boone L, Lawrence W, Watson C, Kenakin T.

Curr Drug Targets Infect Disord. 2002 Sep;2(3):265-78. Review.

PMID:
12462129
35.

Novel spirocyclic pyrrolidones as P2/P1 mimetics in potent inhibitors of HIV-1 protease.

Kazmierski WM, Furfine E, Spaltenstein A, Wright LL.

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3431-3.

PMID:
12419377
36.

Total synthesis and semi-synthetic approaches to analogues of antibacterial natural product althiomycin.

Zarantonello P, Leslie CP, Ferritto R, Kazmierski WM.

Bioorg Med Chem Lett. 2002 Feb 25;12(4):561-5.

PMID:
11844672
37.

A solid-phase approach to analogues of the antibiotic mureidomycin.

Bozzoli A, Kazmierski W, Kennedy G, Pasquarello A, Pecunioso A.

Bioorg Med Chem Lett. 2000 Dec 18;10(24):2759-63.

PMID:
11133085
38.

Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.

Spaltenstein A, Almond MR, Bock WJ, Cleary DG, Furfine ES, Hazen RJ, Kazmierski WM, Salituro FG, Tung RD, Wright LL.

Bioorg Med Chem Lett. 2000 Jun 5;10(11):1159-62.

PMID:
10866371
39.

Cyclic Aromatic Amino Acids with Constrained χ(1) and χ (2) Dihedral Angles.

Tourwé D, Iterbeke K, Kazmierski WM, Tóth G.

Methods Mol Med. 1999;23:321-38. doi: 10.1385/0-89603-517-4:321.

PMID:
21380905
40.

Synthesis of Dipeptides with Ψ[CH(2)0] Amide Bond Mimetics.

Kazmierski WM, Fritch PC.

Methods Mol Med. 1999;23:281-91. doi: 10.1385/0-89603-517-4:281.

PMID:
21380903
41.

N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 2. Structure-activity relationship and optimization of the phenyl alkyl ether moiety.

Collins JL, Blanchard SG, Boswell GE, Charifson PS, Cobb JE, Henke BR, Hull-Ryde EA, Kazmierski WM, Lake DH, Leesnitzer LM, Lehmann J, Lenhard JM, Orband-Miller LA, Gray-Nunez Y, Parks DJ, Plunkett KD, Tong WQ.

J Med Chem. 1998 Dec 3;41(25):5037-54.

PMID:
9836621
42.

Iron chelates bind nitric oxide and decrease mortality in an experimental model of septic shock.

Kazmierski WM, Wolberg G, Wilson JG, Smith SR, Williams DS, Thorp HH, Molina L.

Proc Natl Acad Sci U S A. 1996 Aug 20;93(17):9138-41.

43.

Inhibitors of human immunodeficiency virus type 1 derived from gp41 transmembrane protein: structure--activity studies.

Kazmierski WM, Hazen RJ, Aulabaugh A, StClair MH.

J Med Chem. 1996 Jul 5;39(14):2681-9.

PMID:
8709097
44.

Efficacy of treatment with the iron (III) complex of diethylenetriamine pentaacetic acid in mice and primates inoculated with live lethal dose 100 Escherichia coli.

Molina L, Studenberg S, Wolberg G, Kazmierski W, Wilson J, Tadepalli A, Chang AC, Kosanke S, Hinshaw L.

J Clin Invest. 1996 Jul 1;98(1):192-8.

45.

A topographical model of mu-opioid and brain somatostatin receptor selective ligands. NMR and molecular dynamics studies.

Kazmierski WM, Ferguson RD, Lipkowski AW, Hruby VJ.

Int J Pept Protein Res. 1995 Sep-Oct;46(3-4):265-78.

PMID:
8537180
46.

Efficient synthesis of metal binding peptides incorporating aminodiacetic acid based ligands.

Kazmierski WM.

Int J Pept Protein Res. 1995 Mar;45(3):241-7.

PMID:
7775016
47.

Recent advances in the design and synthesis of small-molecule mimetic drugs.

Kazmierski WM.

Trends Biotechnol. 1994 Jun;12(6):216-8. No abstract available.

PMID:
7765067
48.

Unexpected antinociceptive potency of cyclic [D-Tca1]CTAP: potential for a novel mechanism of action.

Horan PJ, Wild KD, Kazmierski WM, Ferguson R, Hruby VJ, Weber SJ, Davis TP, Fang L, Knapp RJ, Yamamura HI, et al.

Eur J Pharmacol. 1993 Mar 16;233(1):53-62.

PMID:
8386089
49.

Preparation of large peptide libraries with one peptide per bead and their use for the discovery of peptides that bind to acceptors.

Hruby VJ, Lam KS, Lebl M, Kazmierski W, Hersh EM, Salmon SE.

NIDA Res Monogr. 1993;134:75-83. Review. No abstract available.

PMID:
8289888
50.

Constrained phenylalanine analogues. Preferred conformation of the 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic) residue.

Valle G, Kazmierski WM, Crisma M, Bonora GM, Toniolo C, Hruby VJ.

Int J Pept Protein Res. 1992 Sep-Oct;40(3-4):222-32.

PMID:
1335996

Supplemental Content

Loading ...
Support Center