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Papers authored by Doweyko A

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Discovery of novel dihydro-9,10-ethano-anthracene carboxamides as glucocorticoid receptor modulators.

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Yang BV, Vaccaro W, Doweyko AM, Doweyko LM, Huynh T, Tortolani D, Nadler SG, McKay L, Somerville J, Holloway DA, Habte S, Weinstein DS, and Barrish JC

Bioorganic & medicinal chemistry letters 19(8):2139-43, 2009 Apr 15 - Who cited this? | PubMed ID: 19321341 | Fulltext

Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.

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Zhang H, Ryono DE, Devasthale P, Wang W, O'Malley K, Farrelly D, Gu L, Harrity T, Cap M, Chu C, Locke K, Zhang L, Lippy J, Kunselman L, Morgan N, Flynn N,

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Bioorganic & medicinal chemistry letters 19(5):1451-6, 2009 Mar 1 - Who cited this? | PubMed ID: 19201606 | Fulltext

Is QSAR relevant to drug discovery?.

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Doweyko AM

IDrugs : the investigational drugs journal 11(12):894-9, 2008 Dec - Who cited this? | PubMed ID: 19051151 | Fulltext

Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.

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Das J, Moquin RV, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly K, Doweyko AM, Sack JS, Zhang H, Kiefer SE, Kish K, McKinnon M, Barrish JC, Dodd JH, Schieven GL,

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Bioorganic & medicinal chemistry letters 18(8):2652-7, 2008 Apr 15 - Who cited this? | PubMed ID: 18359226 | Fulltext

Synthesis and SAR of new pyrrolo[2,1-f][1,2,4]triazines as potent p38 alpha MAP kinase inhibitors.

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Wrobleski ST, Lin S, Hynes J, Wu H, Pitt S, Shen DR, Zhang R, Gillooly KM, Shuster DJ, McIntyre KW, Doweyko AM, Kish KF, Tredup JA, Duke GJ, Sack JS, McKinnon M,

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Bioorganic & medicinal chemistry letters 18(8):2739-44, 2008 Apr 15 - Who cited this? | PubMed ID: 18364256 | Fulltext

Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.

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Wang W, Devasthale P, Farrelly D, Gu L, Harrity T, Cap M, Chu C, Kunselman L, Morgan N, Ponticiello R, Zebo R, Zhang L, Locke K, Lippy J, O'Malley K, Hosagrahara V,

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Bioorganic & medicinal chemistry letters 18(6):1939, 2008 Mar 15 - Who cited this? | PubMed ID: 18291645 | Fulltext

Benzothiazole based inhibitors of p38alpha MAP kinase.

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Liu C, Lin J, Pitt S, Zhang RF, Sack JS, Kiefer SE, Kish K, Doweyko AM, Zhang H, Marathe PH, Trzaskos J, Mckinnon M, Dodd JH, Barrish JC, Schieven GL, and Leftheris K

Bioorganic & medicinal chemistry letters 18(6):1874-9, 2008 Mar 15 - Who cited this? | PubMed ID: 18296051 | Fulltext

The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.

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Hynes J, Wu H, Pitt S, Shen DR, Zhang R, Schieven GL, Gillooly KM, Shuster DJ, Taylor TL, Yang X, McIntyre KW, McKinnon M, Zhang H, Marathe PH, Doweyko AM, Kish K,

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Bioorganic & medicinal chemistry letters 18(6):1762-7, 2008 Mar 15 - Who cited this? | PubMed ID: 18313298 | Fulltext

QSAR: dead or alive?.

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Doweyko AM

Journal of computer-aided molecular design 22(2):81-9, 2008 Feb - Who cited this? | PubMed ID: 18189157 | Fulltext

Design, Synthesis, and Anti-inflammatory Properties of Orally Active 4-(Phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha Mitogen-Activated Protein Kinase Inhibitors.

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Hynes J, Dyckman AJ, Lin S, Wrobleski ST, Wu H, Gillooly KM, Kanner SB, Lonial H, Loo D, McIntyre KW, Pitt S, Shen DR, Shuster DJ, Yang X, Zhang R, Behnia K,

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Journal of medicinal chemistry 51(1):4-16, 2008 Jan 10 - Who cited this? | PubMed ID: 18072718 | Fulltext

Estimation of hERG inhibition of drug candidates using multivariate property and pharmacophore SAR.

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Johnson SR, Yue H, Conder ML, Shi H, Doweyko AM, Lloyd J, and Levesque P

Bioorganic & medicinal chemistry 15(18):6182-92, 2007 Sep 15 - Who cited this? | PubMed ID: 17596950 | Fulltext

Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.

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Murali Dhar TG, Wrobleski ST, Lin S, Furch JA, Nirschl DS, Fan Y, Todderud G, Pitt S, Doweyko AM, Sack JS, Mathur A, McKinnon M, Barrish JC, Dodd JH, Schieven GL, and Leftheris K

Bioorganic & medicinal chemistry letters 17(18):5019-24, 2007 Sep 15 - Who cited this? | PubMed ID: 17664068 | Fulltext

Discovery of tertiary aminoacids as dual PPARalpha/gamma agonists-I.

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Devasthale PV, Chen S, Jeon Y, Qu F, Ryono DE, Wang W, Zhang H, Cheng L, Farrelly D, Golla R, Grover G, Ma Z, Moore L, Seethala R, Sun W, Doweyko AM,

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Bioorganic & medicinal chemistry letters 17(8):2312-6, 2007 Apr 15 - Who cited this? | PubMed ID: 17292606 | Fulltext

2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatin.

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Das J, Chen P, Norris D, Padmanabha R, Lin J, Moquin RV, Shen Z, Cook LS, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, McIntyre KW, Shuster DJ,

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Journal of medicinal chemistry 49(23):6819, 2006 Nov 16 - Who cited this? | PubMed ID: 17154512 | Fulltext

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.

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Das J, Furch JA, Liu C, Moquin RV, Lin J, Spergel SH, McIntyre KW, Shuster DJ, O'Day KD, Penhallow B, Hung CY, Doweyko AM, Kamath A, Zhang H, Marathe P, Kanner SB,

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Bioorganic & medicinal chemistry letters 16(14):3706, 2006 Jul 15 - Who cited this? | PubMed ID: 16682193 | Fulltext

Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors.

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Das J, Liu C, Moquin RV, Lin J, Furch JA, Spergel SH, Doweyko AM, McIntyre KW, Shuster DJ, O'Day KD, Penhallow B, Hung CY, Kanner SB, Lin TA, Dodd JH, Barrish JC,

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Bioorganic & medicinal chemistry letters 16(9):2411, 2006 May 1 - Who cited this? | PubMed ID: 16481166 | Fulltext

A novel method to simulate the hydrophobic effect and its application to the ranking of host/guest complexes.

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Doweyko AM and Johnson SR

Journal of chemical information and modeling 46(6):2563-73, 2006 - Who cited this? | PubMed ID: 17125196 | Fulltext

A new class of high affinity thyromimetics containing a phenyl-naphthylene core.

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Hangeland JJ, Friends TJ, Doweyko AM, Mellström K, Sandberg J, Grynfarb M, and Ryono DE

Bioorganic & medicinal chemistry letters 15(20):4579-84, 2005 Oct 15 - Who cited this? | PubMed ID: 16099653 | Fulltext

5-Cyanopyrimidine derivatives as a novel class of potent, selective, and orally active inhibitors of p38alpha MAP kinase.

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Liu C, Wrobleski ST, Lin J, Ahmed G, Metzger A, Wityak J, Gillooly KM, Shuster DJ, McIntyre KW, Pitt S, Shen DR, Zhang RF, Zhang H, Doweyko AM, Diller D, Henderson I,

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Journal of medicinal chemistry 48(20):6261-70, 2005 Oct 6 - Who cited this? | PubMed ID: 16190753 | Fulltext

Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.

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Devasthale PV, Chen S, Jeon Y, Qu F, Shao C, Wang W, Zhang H, Cap M, Farrelly D, Golla R, Grover G, Harrity T, Ma Z, Moore L, Ren J, Seethala R,

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Journal of medicinal chemistry 48(6):2248-50, 2005 Mar 24 - Who cited this? | PubMed ID: 15771468 | Fulltext

Structural comparison of p38 inhibitor-protein complexes: a review of recent p38 inhibitors having unique binding interactions.

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Wrobleski ST and Doweyko AM

Current topics in medicinal chemistry 5(10):1005-16, 2005 - Who cited this? | PubMed ID: 16178743 | Fulltext

Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

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Lombardo LJ, Lee FY, Chen P, Norris D, Barrish JC, Behnia K, Castaneda S, Cornelius LA, Das J, Doweyko AM, Fairchild C, Hunt JT, Inigo I, Johnston K, Kamath A, Kan D,

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Journal of medicinal chemistry 47(27):6658-61, 2004 Dec 30 - Who cited this? | PubMed ID: 15615512 | Fulltext

Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.

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Chen P, Norris D, Das J, Spergel SH, Wityak J, Leith L, Zhao R, Chen BC, Pitt S, Pang S, Shen DR, Zhang R, De Fex HF, Doweyko AM, McIntyre KW, Shuster DJ,

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Bioorganic & medicinal chemistry letters 14(24):6061-6, 2004 Dec 20 - Who cited this? | PubMed ID: 15546730 | Fulltext

The discovery of orally active triaminotriazine aniline amides as inhibitors of p38 MAP kinase.

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Leftheris K, Ahmed G, Chan R, Dyckman AJ, Hussain Z, Ho K, Hynes J, Letourneau J, Li W, Lin S, Metzger A, Moriarty KJ, Riviello C, Shimshock Y, Wen J, Wityak J,

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Journal of medicinal chemistry 47(25):6283-91, 2004 Dec 2 - Who cited this? | PubMed ID: 15566298 | Fulltext

Selective Itk inhibitors block T-cell activation and murine lung inflammation.

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Lin TA, McIntyre KW, Das J, Liu C, O'Day KD, Penhallow B, Hung CY, Whitney GS, Shuster DJ, Yang X, Townsend R, Postelnek J, Spergel SH, Lin J, Moquin RV, Furch JA,

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Biochemistry 43(34):11056-62, 2004 Aug 31 - Who cited this? | PubMed ID: 15323564 | Fulltext

Imidazoquinoxaline Src-family kinase p56Lck inhibitors: SAR, QSAR, and the discovery of (S)-N-(2-chloro-6-methylphenyl)-2-(3-methyl-1-piperazinyl)imidazo- [1,5-a]pyrido[3,2-e]pyrazin-6-amine (BMS-279700) as a potent and orally active inhibitor with excellent in vivo antiinflammatory activity.

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Chen P, Doweyko AM, Norris D, Gu HH, Spergel SH, Das J, Moquin RV, Lin J, Wityak J, Iwanowicz EJ, McIntyre KW, Shuster DJ, Behnia K, Chong S, de Fex H, Pang S,

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Journal of medicinal chemistry 47(18):4517-29, 2004 Aug 26 - Who cited this? | PubMed ID: 15317463 | Fulltext

Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta.

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Hangeland JJ, Doweyko AM, Dejneka T, Friends TJ, Devasthale P, Mellström K, Sandberg J, Grynfarb M, Sack JS, Einspahr H, Färnegårdh M, Husman B, Ljunggren J, Koehler K, Sheppard C, Malm J,

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Bioorganic & medicinal chemistry letters 14(13):3549-53, 2004 Jul 5 - Who cited this? | PubMed ID: 15177471 | Fulltext

3D-QSAR illusions.

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Doweyko AM

Journal of computer-aided molecular design 18(7-9):587-96, 2004 - Who cited this? | PubMed ID: 15729857 | Fulltext

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).

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Wityak J, Das J, Moquin RV, Shen Z, Lin J, Chen P, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, Schieven GL, Kanner SB, and Barrish JC

Bioorganic & medicinal chemistry letters 13(22):4007-10, 2003 Nov 17 - Who cited this? | PubMed ID: 14592495 | Fulltext

Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors.

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Das J, Moquin RV, Lin J, Liu C, Doweyko AM, DeFex HF, Fang Q, Pang S, Pitt S, Shen DR, Schieven GL, Barrish JC, and Wityak J

Bioorganic & medicinal chemistry letters 13(15):2587-90, 2003 Aug 4 - Who cited this? | PubMed ID: 12852972 | Fulltext

Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117.

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Das J, Lin J, Moquin RV, Shen Z, Spergel SH, Wityak J, Doweyko AM, DeFex HF, Fang Q, Pang S, Pitt S, Shen DR, Schieven GL, and Barrish JC

Bioorganic & medicinal chemistry letters 13(13):2145-9, 2003 Jul 7 - Who cited this? | PubMed ID: 12798323 | Fulltext

In silico ADME/Tox: why models fail.

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Stouch TR, Kenyon JR, Johnson SR, Chen XQ, Doweyko A, and Li Y

Journal of computer-aided molecular design 17(2-4):83-92, 2003 - Who cited this? | PubMed ID: 13677477 | Fulltext

Discovery and initial SAR of imidazoquinoxalines as inhibitors of the Src-family kinase p56(Lck).

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Chen P, Norris D, Iwanowicz EJ, Spergel SH, Lin J, Gu HH, Shen Z, Wityak J, Lin TA, Pang S, De Fex HF, Pitt S, Shen DR, Doweyko AM, Bassolino DA, Roberge JY,

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Bioorganic & medicinal chemistry letters 12(10):1361-4, 2002 May 20 - Who cited this? | PubMed ID: 11992777 | Fulltext

3D-QSAR using 'multiconformer' alignment: the use of HASL in the analysis of 5-HT1A thienopyrimidinone ligands.

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Guccione S, Doweyko AM, Chen H, Barretta GU, and Balzano F

Journal of computer-aided molecular design 14(7):647-57, 2000 Oct - Who cited this? | PubMed ID: 11008886 | Fulltext

Comparison of 3D quantitative structure-activity relationship methods: analysis of the in vitro antimalarial activity of 154 artemisinin analogues by hypothetical active-site lattice and comparative molecular field analysis.

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Woolfrey JR, Avery MA, and Doweyko AM

Journal of computer-aided molecular design 12(2):165-81, 1998 Mar - Who cited this? | PubMed ID: 9690175 | Fulltext

Antiulcer agents. 6. Analysis of the in vitro biochemical and in vivo gastric antisecretory activity of substituted imidazo[1,2-a]pyridines and related analogues using comparative molecular field analysis and hypothetical active site lattice methodologies.

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Kaminski JJ and Doweyko AM

Journal of medicinal chemistry 40(4):427-36, 1997 Feb 14 - Who cited this? | PubMed ID: 9046332 | Fulltext

Three-dimensional pharmacophores from binding data.

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Doweyko AM

Journal of medicinal chemistry 37(12):1769-78, 1994 Jun 10 - Who cited this? | PubMed ID: 8021917 | Fulltext

An application of 3D-QSAR to the analysis of the sequence specificity of DNA alkylation by uracil mustard.

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Doweyko AM and Mattes WB

Biochemistry 31(39):9388-92, 1992 Oct 6 - Who cited this? | PubMed ID: 1327114 | Fulltext

The hypothetical active site lattice. An approach to modelling active sites from data on inhibitor molecules.

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Doweyko AM

Journal of medicinal chemistry 31(7):1396-406, 1988 Jul - Who cited this? | PubMed ID: 3290487 | Fulltext

Quantitative structure-activity relationships for 2-[(phenylmethyl)sulfonyl]pyridine 1-oxide herbicides.

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Doweyko AM, Bell AR, Minatelli JA, and Relyea DI

Journal of medicinal chemistry 26(4):475-8, 1983 Apr - Who cited this? | PubMed ID: 6834380 | Fulltext

Synthesis and evaluation of alpha-hydroxythiol esters as antitumor agents and glyoxalase I inhibitors.

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Hall SS, Doweyko LM, Doweyko AM, and Zilenovski JS

Journal of medicinal chemistry 20(10):1239-42, 1977 Oct - Who cited this? | PubMed ID: 903914 | Fulltext

Glyoxalase I enzyme studies. 2. Nuclear magnetic resonance evidence for an enediol-proton transfer mechanism.

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Hall SS, Doweyko AM, and Jordan F

Journal of the American Chemical Society 98(23):7460-1, 1976 Nov 10 - Who cited this? | PubMed ID: 977876 | Fulltext

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