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Items: 33

1.

Discovery of novel pan-genotypic HCV NS5A inhibitors containing a novel tetracyclic core.

Yu W, Hu B, Zhong B, Hao J, Lei Z, Agrawal S, Rokosz L, Liu R, Chen S, Asante-Appiah E, Kozlowski JA.

Bioorg Med Chem Lett. 2019 Mar 1;29(5):700-706. doi: 10.1016/j.bmcl.2019.01.031. Epub 2019 Jan 25.

PMID:
30711390
2.

In Vitro Antiviral Profile of Ruzasvir, a Potent and Pangenotype Inhibitor of Hepatitis C Virus NS5A.

Asante-Appiah E, Liu R, Curry S, McMonagle P, Agrawal S, Carr D, Rokosz L, Lahser F, Bystol K, Chase R, Black S, Ferrari E, Ingravallo P, Tong L, Yu W, Kozlowski J.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01280-18. doi: 10.1128/AAC.01280-18. Print 2018 Nov.

PMID:
30150466
3.

Discovery of MK-6169, a Potent Pan-Genotype Hepatitis C Virus NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Substitutions.

Yu W, Tong L, Selyutin O, Chen L, Hu B, Zhong B, Hao J, Ji T, Zan S, Yin J, Ruck RT, Curry S, McMonagle P, Agrawal S, Rokosz L, Carr D, Ingravallo P, Bystol K, Lahser F, Liu R, Chen S, Feng KI, Cartwright M, Asante-Appiah E, Kozlowski JA.

J Med Chem. 2018 May 10;61(9):3984-4003. doi: 10.1021/acs.jmedchem.7b01927. Epub 2018 May 1.

PMID:
29681153
4.

Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms.

Tong L, Yu W, Chen L, Selyutin O, Dwyer MP, Nair AG, Mazzola R, Kim JH, Sha D, Yin J, Ruck RT, Davies IW, Hu B, Zhong B, Hao J, Ji T, Zan S, Liu R, Agrawal S, Xia E, Curry S, McMonagle P, Bystol K, Lahser F, Carr D, Rokosz L, Ingravallo P, Chen S, Feng KI, Cartwright M, Asante-Appiah E, Kozlowski JA.

J Med Chem. 2017 Jan 12;60(1):290-306. doi: 10.1021/acs.jmedchem.6b01310. Epub 2016 Nov 15.

5.

Discovery of Chromane Containing Hepatitis C Virus (HCV) NS5A Inhibitors with Improved Potency against Resistance-Associated Variants.

Yu W, Tong L, Hu B, Zhong B, Hao J, Ji T, Zan S, Coburn CA, Selyutin O, Chen L, Rokosz L, Agrawal S, Liu R, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Chen S, Kozlowski JA.

J Med Chem. 2016 Nov 23;59(22):10228-10243. Epub 2016 Nov 9.

PMID:
27792320
6.

Substituted tetracyclic indole core derivatives of HCV NS5A inhibitor MK-8742.

Yu W, Zhou G, Coburn CA, Zeng Q, Tong L, Dwyer MP, Hu B, Zhong B, Hao J, Ji T, Zan S, Chen L, Mazzola R, Kim JH, Sha D, Selyutin O, Rosenblum SB, Lavey B, Nair AG, Heon Kim S, Keertikar KM, Rokosz L, Agrawal S, Liu R, Xia E, Zhai Y, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Chen S, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4851-4856. doi: 10.1016/j.bmcl.2016.08.002. Epub 2016 Aug 2.

PMID:
27568086
7.

Discovery of potent macrocyclic HCV NS5A inhibitors.

Yu W, Vibulbhan B, Rosenblum SB, Martin GS, Vellekoop AS, Holst CL, Coburn CA, Wong M, Selyutin O, Ji T, Zhong B, Hu B, Chen L, Dwyer MP, Jiang Y, Nair AG, Tong L, Zeng Q, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Fells J, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3793-9. doi: 10.1016/j.bmcl.2016.05.042. Epub 2016 May 17.

PMID:
27282743
8.

Alkyl substituted aminal derivatives of HCV NS5A inhibitor MK-8742.

Yu W, Coburn CA, Nair AG, Wong M, Tong L, Dwyer MP, Hu B, Zhong B, Hao J, Yang DY, Selyutin O, Jiang Y, Rosenblum SB, Kim SH, Lavey BJ, Zhou G, Rizvi R, Shankar BB, Zeng Q, Chen L, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Nomeir A, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3800-5. doi: 10.1016/j.bmcl.2016.05.041. Epub 2016 May 14.

PMID:
27282742
9.

Discovery of novel quinolinone adenosine A2B antagonists.

McGuinness BF, Ho KK, Stauffer TM, Rokosz LL, Mannava N, Kultgen SG, Saionz K, Klon A, Chen W, Desai H, Rogers WL, Webb M, Yin J, Jiang Y, Li T, Yan H, Jing K, Zhang S, Majumdar KK, Srivastava V, Saha S.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7414-20. doi: 10.1016/j.bmcl.2010.10.030. Epub 2010 Nov 4.

PMID:
21055932
10.

Discovery of 2-aminoimidazopyridine adenosine A(2A) receptor antagonists.

McGuinness BF, Cole AG, Dong G, Brescia MR, Shao Y, Henderson I, Rokosz LL, Stauffer TM, Mannava N, Kimble EF, Hicks C, White N, Wines PG, Quadros E.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6845-9. doi: 10.1016/j.bmcl.2010.08.064. Epub 2010 Aug 19.

PMID:
20869242
11.

Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.

Paruch K, Dwyer MP, Alvarez C, Brown C, Chan TY, Doll RJ, Keertikar K, Knutson C, McKittrick B, Rivera J, Rossman R, Tucker G, Fischmann T, Hruza A, Madison V, Nomeir AA, Wang Y, Kirschmeier P, Lees E, Parry D, Sgambellone N, Seghezzi W, Schultz L, Shanahan F, Wiswell D, Xu X, Zhou Q, James RA, Paradkar VM, Park H, Rokosz LR, Stauffer TM, Guzi TJ.

ACS Med Chem Lett. 2010 May 17;1(5):204-8. doi: 10.1021/ml100051d. eCollection 2010 Aug 12.

12.

Synthesis and SAR studies of trisubstituted purinones as potent and selective adenosine A2A receptor antagonists.

Shao Y, Cole AG, Brescia MR, Qin LY, Duo J, Stauffer TM, Rokosz LL, McGuinness BF, Henderson I.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1399-402. doi: 10.1016/j.bmcl.2009.01.042. Epub 2009 Jan 19.

PMID:
19181527
13.

Synthesis of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A(2A) receptor antagonists.

Cole AG, Stauffer TM, Rokosz LL, Metzger A, Dillard LW, Zeng W, Henderson I.

Bioorg Med Chem Lett. 2009 Jan 15;19(2):378-81. doi: 10.1016/j.bmcl.2008.11.066. Epub 2008 Nov 24.

PMID:
19059776
14.

Kinase inhibitors as drugs for chronic inflammatory and immunological diseases: progress and challenges.

Rokosz LL, Beasley JR, Carroll CD, Lin T, Zhao J, Appell KC, Webb ML.

Expert Opin Ther Targets. 2008 Jul;12(7):883-903. doi: 10.1517/14728222.12.7.883 . Review.

PMID:
18554156
15.

Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.

Lai G, Merritt JR, He Z, Feng D, Chao J, Czarniecki MF, Rokosz LL, Stauffer TM, Rindgen D, Taveras AG.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1864-8. doi: 10.1016/j.bmcl.2008.02.010. Epub 2008 Feb 10.

PMID:
18304809
16.

Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.

Paruch K, Dwyer MP, Alvarez C, Brown C, Chan TY, Doll RJ, Keertikar K, Knutson C, McKittrick B, Rivera J, Rossman R, Tucker G, Fischmann TO, Hruza A, Madison V, Nomeir AA, Wang Y, Lees E, Parry D, Sgambellone N, Seghezzi W, Schultz L, Shanahan F, Wiswell D, Xu X, Zhou Q, James RA, Paradkar VM, Park H, Rokosz LR, Stauffer TM, Guzi TJ.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6220-3. Epub 2007 Sep 8.

PMID:
17904841
17.

Discovery and development of melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.

Rokosz LL.

Expert Opin Drug Discov. 2007 Oct;2(10):1301-27. doi: 10.1517/17460441.2.10.1301.

PMID:
23484528
18.

Design, synthesis, and evaluation of tetrahydroquinoline and pyrrolidine sulfonamide carbamates as gamma-secretase inhibitors.

Guo T, Gu H, Hobbs DW, Rokosz LL, Stauffer TM, Jacob B, Clader JW.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3010-3. Epub 2007 Mar 23.

PMID:
17418571
19.

Discovery of tetralin ureas as potent melanin concentrating hormone 1 receptor antagonists.

Guo T, Gu H, Hobbs DW, Busler DE, Rokosz LL.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1718-21. Epub 2006 Dec 24.

PMID:
17251014
20.

Discovery and preliminary evaluation of 5-(4-phenylbenzyl)oxazole-4-carboxamides as prostacyclin receptor antagonists.

Brescia MR, Rokosz LL, Cole AG, Stauffer TM, Lehrach JM, Auld DS, Henderson I, Webb ML.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1211-5. Epub 2006 Dec 12.

PMID:
17239589
21.

Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.

Dwyer MP, Yu Y, Chao J, Aki C, Chao J, Biju P, Girijavallabhan V, Rindgen D, Bond R, Mayer-Ezel R, Jakway J, Hipkin RW, Fossetta J, Gonsiorek W, Bian H, Fan X, Terminelli C, Fine J, Lundell D, Merritt JR, Rokosz LL, Kaiser B, Li G, Wang W, Stauffer T, Ozgur L, Baldwin J, Taveras AG.

J Med Chem. 2006 Dec 28;49(26):7603-6.

PMID:
17181143
22.

Biological examination of melanin concentrating hormone receptor 1: multi-tasking from the hypothalamus.

Rokosz LL, Hobbs DW.

Timely Top Med Cardiovasc Dis. 2006 Sep 1;10:E23.

PMID:
17066150
23.

Biological examination of melanin concentrating hormone receptor 1: multi-tasking from the hypothalamus.

Rokosz LL, Hobbs DW.

Drug News Perspect. 2006 Jun;19(5):273-86. Review.

PMID:
16941049
24.

Exploring structure-activity relationships of tricyclic farnesyltransferase inhibitors using ECLiPS libraries.

Rokosz LL, Huang CY, Reader JC, Stauffer TM, Southwick EC, Li G, Chelsky D, Baldwin JJ.

Comb Chem High Throughput Screen. 2006 Aug;9(7):545-58.

PMID:
16925514
25.

Synthesis and structure-activity relationships of 3,4-diaminocyclobut-3-ene-1,2-dione CXCR2 antagonists.

Merritt JR, Rokosz LL, Nelson KH Jr, Kaiser B, Wang W, Stauffer TM, Ozgur LE, Schilling A, Li G, Baldwin JJ, Taveras AG, Dwyer MP, Chao J.

Bioorg Med Chem Lett. 2006 Aug 1;16(15):4107-10. Epub 2006 May 11.

PMID:
16697193
26.

Guiding farnesyltransferase inhibitors from an ECLiPS library to the catalytic zinc.

Huang CY, Stauffer TM, Strickland CL, Reader JC, Huang H, Li G, Cooper AB, Doll RJ, Ganguly AK, Baldwin JJ, Rokosz LL.

Bioorg Med Chem Lett. 2006 Feb;16(3):507-11. Epub 2005 Nov 10.

PMID:
16289818
27.

Surfing the piperazine core of tricyclic farnesyltransferase inhibitors.

Rokosz LL, Huang CY, Reader JC, Stauffer TM, Chelsky D, Sigal NH, Ganguly AK, Baldwin JJ.

Bioorg Med Chem Lett. 2005 Dec 15;15(24):5537-43. Epub 2005 Oct 3.

PMID:
16202593
28.

Discovery and SAR of biaryl piperidine MCH1 receptor antagonists through solid-phase encoded combinatorial synthesis.

Guo T, Shao Y, Qian G, Rokosz LL, Stauffer TM, Hunter RC, Babu SD, Gu H, Hobbs DW.

Bioorg Med Chem Lett. 2005 Aug 15;15(16):3696-700.

PMID:
15978811
29.

Discovery and SAR of 4-amino-2-biarylbutylurea MCH 1 receptor antagonists through solid-phase parallel synthesis.

Guo T, Hunter RC, Gu H, Rokosz LL, Stauffer TM, Hobbs DW.

Bioorg Med Chem Lett. 2005 Aug 15;15(16):3691-5.

PMID:
15953726
30.

Stromelysin-1: three-dimensional structure of the inhibited catalytic domain and of the C-truncated proenzyme.

Becker JW, Marcy AI, Rokosz LL, Axel MG, Burbaum JJ, Fitzgerald PM, Cameron PM, Esser CK, Hagmann WK, Hermes JD, et al.

Protein Sci. 1995 Oct;4(10):1966-76.

31.

Reconstitution of active human calcineurin from recombinant subunits expressed in bacteria.

Rokosz LL, O'Keefe SJ, Parsons JN, Cameron PM, Burbaum JJ.

Protein Expr Purif. 1995 Oct;6(5):655-64.

PMID:
8535159
32.

Regulation of calcineurin phosphatase activity and interaction with the FK-506.FK-506 binding protein complex.

Parsons JN, Wiederrecht GJ, Salowe S, Burbaum JJ, Rokosz LL, Kincaid RL, O'Keefe SJ.

J Biol Chem. 1994 Jul 29;269(30):19610-6.

33.

Human cytoplasmic 3-hydroxy-3-methylglutaryl coenzyme A synthase: expression, purification, and characterization of recombinant wild-type and Cys129 mutant enzymes.

Rokosz LL, Boulton DA, Butkiewicz EA, Sanyal G, Cueto MA, Lachance PA, Hermes JD.

Arch Biochem Biophys. 1994 Jul;312(1):1-13.

PMID:
7913309

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