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Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 8, 2014, Pages 1968-1973

Thiophene carboxamide inhibitors of JAK2 as potential treatments for myleoproliferative neoplasms

(15) Haidle, Andrew M a Zabierek, Anna A a Childers, Kaleen K a Rosenstein, Craig a Mathur, Anjili a Altman, Michael D a Chan, Grace a Xu, Lin a Bachman, Eric a Mo, Jan Rung a Bouthillette, Melaney a Rush, Thomas a Tempest, Paul a Marshall, C Gary a Young, Jonathan R a

a MERCK RESEARCH LABORATORIES (United States)

Author keywords

Bioisostere; Inhibitor; JAK2; Metabolite identification; Polycythemia vera; Protein kinase; Thiophene

Indexed keywords

AMIDE; JANUS KINASE 2; JANUS KINASE 2 INHIBITOR; PYRIDINE DERIVATIVE; STAT5 PROTEIN; THIOPHENE DERIVATIVE; UREA;

ARTICLE; CHEMICAL MODIFICATION; DRUG POTENCY; DRUG SELECTIVITY; ENZYME INHIBITION; IN VITRO STUDY; IN VIVO STUDY; MYELOPROLIFERATIVE NEOPLASM; NONHUMAN; STRUCTURE ACTIVITY RELATION;

BIOISOSTERE; INHIBITOR; JAK2; METABOLITE IDENTIFICATION; POLYCYTHEMIA VERA; PROTEIN KINASE; THIOPHENE;

AMINOIMIDAZOLE CARBOXAMIDE; ANIMALS; ANTINEOPLASTIC AGENTS; DISEASE MODELS, ANIMAL; ENZYME ACTIVATION; HUMANS; JANUS KINASE 2; LEUKEMIA, MYELOID, ACUTE; MICROSOMES; MODELS, BIOLOGICAL; MOLECULAR STRUCTURE; PROTEIN KINASE INHIBITORS; RATS; THIOPHENES;

EID: 84897514343 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2014.02.064 Document Type: Article

Times cited : (7)

References (29)

1
- 84897131066
- K. Gabler, I. Behrmann, and C. Haan JAK-STAT 2 2013 e25025
- (2013) JAK-STAT , vol.2 , pp. 25025
- Gabler, K.¹ Behrmann, I.² Haan, C.³

2
- 84897488278
- E.J. Baxter, L.M. Scott, P.J. Campbell, C. East, N. Fourouclas, S. Swanton, G.S. Vassiliou, A.J. Bench, E.M. Boyd, N. Curtin, M.A. Scott, W.N. Erber, and A.R. Green Lancet 1054 2005 365
- (2005) Lancet , vol.1054 , pp. 365
- Baxter, E.J.¹ Scott, L.M.² Campbell, P.J.³ East, C.⁴ Fourouclas, N.⁵ Swanton, S.⁶ Vassiliou, G.S.⁷ Bench, A.J.⁸ Boyd, E.M.⁹ Curtin, N.¹⁰ Scott, M.A.¹¹ Erber, W.N.¹² Green, A.R.¹³

3
- 17844383458
- C. James, V. Ugo, J.P. Le Couedic, J. Staerk, F. Delhommeau, C. Lacout, L. Garcon, H. Raslova, R. Berger, A. Bennaceur-Griscelli, J.L. Villeval, S.N. Constantinescu, N. Casadevall, and W. Vainchenker Nature 434 2005 1144
- (2005) Nature , vol.434 , pp. 1144
- James, C.¹ Ugo, V.² Le Couedic, J.P.³ Staerk, J.⁴ Delhommeau, F.⁵ Lacout, C.⁶ Garcon, L.⁷ Raslova, H.⁸ Berger, R.⁹ Bennaceur-Griscelli, A.¹⁰ Villeval, J.L.¹¹ Constantinescu, S.N.¹² Casadevall, N.¹³ Vainchenker, W.¹⁴

4
- 17644424955
- R. Kralovics, F. Passamonti, A.S. Buser, S.S. Teo, R. Tiedt, J.R. Passweg, A. Tichelli, M. Cazzola, and R.C.N. Skoda Engl. J. Med. 352 2005 1779
- (2005) Engl. J. Med. , vol.352 , pp. 1779
- Kralovics, R.¹ Passamonti, F.² Buser, A.S.³ Teo, S.S.⁴ Tiedt, R.⁵ Passweg, J.R.⁶ Tichelli, A.⁷ Cazzola, M.⁸ Skoda, R.C.N.⁹

5
- 20244369569
- R.L. Levine, M. Wadleigh, J. Cools, B.L. Ebert, G. Wernig, B.J. Huntly, T.J. Boggon, I. Wlodarska, J.J. Clark, S. Moore, J. Adelsperger, S. Koo, J.C. Lee, S. Gabriel, T. Mercher, A. D'Andrea, S. Frohling, K. Dohner, P. Marynen, P. Vandenberghe, R.A. Mesa, A. Tefferi, J.D. Griffin, M.J. Eck, W.R. Sellers, M. Meyerson, T.R. Golub, S.J. Lee, and D.G. Gilliland Cancer Cell 7 2005 387
- (2005) Cancer Cell , vol.7 , pp. 387
- Levine, R.L.¹ Wadleigh, M.² Cools, J.³ Ebert, B.L.⁴ Wernig, G.⁵ Huntly, B.J.⁶ Boggon, T.J.⁷ Wlodarska, I.⁸ Clark, J.J.⁹ Moore, S.¹⁰ Adelsperger, J.¹¹ Koo, S.¹² Lee, J.C.¹³ Gabriel, S.¹⁴ Mercher, T.¹⁵ D'Andrea, A.¹⁶ Frohling, S.¹⁷ Dohner, K.¹⁸ Marynen, P.¹⁹ Vandenberghe, P.²⁰ more..

6
- 20744460045
- R. Zhao, S. Xing, Z. Li, X. Fu, Q. Li, S.B. Krantz, and Z.J. Zhao J. Biol. Chem. 280 2005 22788
- (2005) J. Biol. Chem. , vol.280 , pp. 22788
- Zhao, R.¹ Xing, S.² Li, Z.³ Fu, X.⁴ Li, Q.⁵ Krantz, S.B.⁶ Zhao, Z.J.⁷

7
- 34548240698
- R.L. Levine, A. Pardanani, A. Tefferi, and D.G. Gilliland Nat. Rev. Cancer 7 2007 673
- (2007) Nat. Rev. Cancer , vol.7 , pp. 673
- Levine, R.L.¹ Pardanani, A.² Tefferi, A.³ Gilliland, D.G.⁴

8
- 77950684805
- A. Quintas-Cardama, K. Vaddi, P. Liu, T. Manshouri, J. Li, P.A. Scherle, E. Caulder, X. Wen, Y. Li, P. Waeltz, M. Rupar, T. Burn, Y. Lo, J. Kelley, M. Covington, S. Shepard, J.D. Rodgers, P. Haley, H. Kantarjian, J.S. Fridman, and S. Vertovsek Blood 115 2010 3109
- (2010) Blood , vol.115 , pp. 3109
- Quintas-Cardama, A.¹ Vaddi, K.² Liu, P.³ Manshouri, T.⁴ Li, J.⁵ Scherle, P.A.⁶ Caulder, E.⁷ Wen, X.⁸ Li, Y.⁹ Waeltz, P.¹⁰ Rupar, M.¹¹ Burn, T.¹² Lo, Y.¹³ Kelley, J.¹⁴ Covington, M.¹⁵ Shepard, S.¹⁶ Rodgers, J.D.¹⁷ Haley, P.¹⁸ Kantarjian, H.¹⁹ Fridman, J.S.²⁰ Vertovsek, S.²¹ more..

9
- 80054958188
- J. Lim, B. Taoka, R.D. Otte, K. Spencer, C.J. Dinsmore, M.D. Altman, G. Chan, C. Rosenstein, S. Sharma, H.-P. Su, A.A. Szewczak, L. Xu, H. Yin, J. Zugay-Murphy, C.G. Marshall, and J.R. Young J. Med. Chem. 54 2011 7334
- (2011) J. Med. Chem. , vol.54 , pp. 7334
- Lim, J.¹ Taoka, B.² Otte, R.D.³ Spencer, K.⁴ Dinsmore, C.J.⁵ Altman, M.D.⁶ Chan, G.⁷ Rosenstein, C.⁸ Sharma, S.⁹ Su, H.-P.¹⁰ Szewczak, A.A.¹¹ Xu, L.¹² Yin, H.¹³ Zugay-Murphy, J.¹⁴ Marshall, C.G.¹⁵ Young, J.R.¹⁶

10
- 78449308759
- T. Siu, E.S. Kozina, J. Jung, C. Rosenstein, A. Mathur, M.D. Altman, G. Chan, L. Xu, E. Bachman, J.-R. Mo, M. Bouthillette, T. Rush, C.J. Dinsmore, C.G. Marshall, and J.R. Young Bioorg. Med. Chem. Lett. 20 2010 7421
- (2010) Bioorg. Med. Chem. Lett. , vol.20 , pp. 7421
- Siu, T.¹ Kozina, E.S.² Jung, J.³ Rosenstein, C.⁴ Mathur, A.⁵ Altman, M.D.⁶ Chan, G.⁷ Xu, L.⁸ Bachman, E.⁹ Mo, J.-R.¹⁰ Bouthillette, M.¹¹ Rush, T.¹² Dinsmore, C.J.¹³ Marshall, C.G.¹⁴ Young, J.R.¹⁵

11
- 34447627350
- A. Pardanani, J. Hood, T. Lasho, R.L. Levine, M.B. Martin, G. Noronha, C. Finke, C.C. Mak, R. Mesa, H. Zhu, R. Soll, D.G. Gilliland, and A. Tefferi Leukemia 21 2007 1658
- (2007) Leukemia , vol.21 , pp. 1658
- Pardanani, A.¹ Hood, J.² Lasho, T.³ Levine, R.L.⁴ Martin, M.B.⁵ Noronha, G.⁶ Finke, C.⁷ Mak, C.C.⁸ Mesa, R.⁹ Zhu, H.¹⁰ Soll, R.¹¹ Gilliland, D.G.¹² Tefferi, A.¹³

12
- 47049098437
- E.O. Hexner, C. Serdikoff, M. Jan, C.R. Swider, C. Robinson, S. Yang, T. Angeles, S.G. Emerson, M. Carroll, B. Ruggeri, and P. Dobrzanski Blood 111 2008 5663
- (2008) Blood , vol.111 , pp. 5663
- Hexner, E.O.¹ Serdikoff, C.² Jan, M.³ Swider, C.R.⁴ Robinson, C.⁵ Yang, S.⁶ Angeles, T.⁷ Emerson, S.G.⁸ Carroll, M.⁹ Ruggeri, B.¹⁰ Dobrzanski, P.¹¹

13
- 70349200694
- C.J. Burns, D.G. Bourke, L. Andrau, X. Bu, S.A. Charman, A.C. Donohue, E. Fantino, M. Farrugia, J.T. Feutrill, M. Joffe, M.R. Kling, M. Kurek, T.L. Nero, T. Nguyen, J.T. Palmer, I. Phillips, D.M. Shackleford, H. Sikanyika, M. Styles, S. Su, H. Treutlein, J. Zeng, and A.F. Wilks Bioorg. Med. Chem. Lett. 19 2009 5887
- (2009) Bioorg. Med. Chem. Lett. , vol.19 , pp. 5887
- Burns, C.J.¹ Bourke, D.G.² Andrau, L.³ Bu, X.⁴ Charman, S.A.⁵ Donohue, A.C.⁶ Fantino, E.⁷ Farrugia, M.⁸ Feutrill, J.T.⁹ Joffe, M.¹⁰ Kling, M.R.¹¹ Kurek, M.¹² Nero, T.L.¹³ Nguyen, T.¹⁴ Palmer, J.T.¹⁵ Phillips, I.¹⁶ Shackleford, D.M.¹⁷ Sikanyika, H.¹⁸ Styles, M.¹⁹ Su, S.²⁰ more..

14
- 78651064537
- S. Ioannidis, M.L. Lamb, T. Wang, L. Almeida, M.H. Block, A.M. Davies, B. Peng, M. Su, H.-J. Zhang, E. Hoffmann, C. Rivard, I. Green, T. Howard, H. Pollard, J. Read, M. Alimzhanov, G. Bebernitz, K. Bell, M. Ye, D. Huszar, and M. Zinda J. Med. Chem. 54 2011 262
- (2011) J. Med. Chem. , vol.54 , pp. 262
- Ioannidis, S.¹ Lamb, M.L.² Wang, T.³ Almeida, L.⁴ Block, M.H.⁵ Davies, A.M.⁶ Peng, B.⁷ Su, M.⁸ Zhang, H.-J.⁹ Hoffmann, E.¹⁰ Rivard, C.¹¹ Green, I.¹² Howard, T.¹³ Pollard, H.¹⁴ Read, J.¹⁵ Alimzhanov, M.¹⁶ Bebernitz, G.¹⁷ Bell, K.¹⁸ Ye, M.¹⁹ Huszar, D.²⁰ Zinda, M.²¹ more..

15
- 0034804745
- L.D. Notarangelo, P. Mella, A. Jones, G. de Saint Basile, G. Savoldi, T. Cranston, M. Vihinen, and R.F. Schumacher Hum. Mutat. 18 2001 255
- (2001) Hum. Mutat. , vol.18 , pp. 255
- Notarangelo, L.D.¹ Mella, P.² Jones, A.³ De Saint Basile, G.⁴ Savoldi, G.⁵ Cranston, T.⁶ Vihinen, M.⁷ Schumacher, R.F.⁸

16
- 34447548576
- C. Abad-Zapatero Expert Opin. Drug Discov. 2 2007 469
- (2007) Expert Opin. Drug Discov. , vol.2 , pp. 469
- Abad-Zapatero, C.¹

17
- 0032795192
- D.E. Clark J. Pharm. Sci. 88 1999 807
- (1999) J. Pharm. Sci. , vol.88 , pp. 807
- Clark, D.E.¹

18
- 33746614110
- B. Lippa, J. Morris, M. Corbett, T.A. Kwan, M.C. Noe, S.L. Snow, T.G. Gant, M. Mangiaracina, H.A. Coffey, B. Foster, E.A. Knauth, and M.D. Wessel Bioorg. Med. Chem. Lett. 16 2006 3444
- (2006) Bioorg. Med. Chem. Lett. , vol.16 , pp. 3444
- Lippa, B.¹ Morris, J.² Corbett, M.³ Kwan, T.A.⁴ Noe, M.C.⁵ Snow, S.L.⁶ Gant, T.G.⁷ Mangiaracina, M.⁸ Coffey, H.A.⁹ Foster, B.¹⁰ Knauth, E.A.¹¹ Wessel, M.D.¹²

19
- 33847090263
- R.E. Rosenfield Jr., R. Parthasarathy, and J.D. Dunitz J. Am. Chem. Soc. 99 1977 4860
- (1977) J. Am. Chem. Soc. , vol.99 , pp. 4860
- Rosenfield, Jr.R.E.¹ Parthasarathy, R.² Dunitz, J.D.³

20
- 13944252481
- A.C. Pierce, E. ter Haar, H.M. Binch, D.P. Kay, S.R. Patel, and P. Li J. Med. Chem. 48 2005 1278
- (2005) J. Med. Chem. , vol.48 , pp. 1278
- Pierce, A.C.¹ Ter Haar, E.² Binch, H.M.³ Kay, D.P.⁴ Patel, S.R.⁵ Li, P.⁶

21
- 0037156334
- J.E. Thompson, R.M. Cubbon, R.T. Cummings, L.S. Wicker, R. Frankshun, B.R. Cunningham, P.M. Cameron, P.T. Meinke, N. Liverton, Y. Weng, and J.A. DeMartino Bioorg. Med. Chem. Lett. 12 2002 1219
- (2002) Bioorg. Med. Chem. Lett. , vol.12 , pp. 1219
- Thompson, J.E.¹ Cubbon, R.M.² Cummings, R.T.³ Wicker, L.S.⁴ Frankshun, R.⁵ Cunningham, B.R.⁶ Cameron, P.M.⁷ Meinke, P.T.⁸ Liverton, N.⁹ Weng, Y.¹⁰ Demartino, J.A.¹¹

22
- 30144436273
- I.S. Lucet, E. Fantino, M. Styles, R. Bamert, O. Patel, S.E. Broughton, M. Walter, C.J. Burns, H. Treutlein, A.F. Wilks, and J. Rossjohn Blood 107 2006 176
- (2006) Blood , vol.107 , pp. 176
- Lucet, I.S.¹ Fantino, E.² Styles, M.³ Bamert, R.⁴ Patel, O.⁵ Broughton, S.E.⁶ Walter, M.⁷ Burns, C.J.⁸ Treutlein, H.⁹ Wilks, A.F.¹⁰ Rossjohn, J.¹¹

23
- 84860875380
- K. Gewald, E. Schinke, and H. Böttcher Chem. Ber. 99 1966 94
- (1966) Chem. Ber. , vol.99 , pp. 94
- Gewald, K.¹ Schinke, E.² Böttcher, H.³

24
- 0038579438
- X. Huang, K.W. Anderson, D. Zim, L. Jiang, A. Klapars, and S.L. Buchwald J. Am. Chem. Soc. 125 2003 6653
- (2003) J. Am. Chem. Soc. , vol.125 , pp. 6653
- Huang, X.¹ Anderson, K.W.² Zim, D.³ Jiang, L.⁴ Klapars, A.⁵ Buchwald, S.L.⁶

25
- 49849094738
- J.D. Hughes, J. Blagg, D.A. Price, S. Bailey, G.A. DeCrescenzo, R.V. Devraj, E. Ellsworth, Y.M. Fobian, M.E. Gibbs, R.W. Gilles, N. Greene, E. Huang, T. Krieger-Burke, J. Loesel, T. Wager, L. Whiteley, and Y. Zhang Bioorg. Med. Chem. Lett. 18 2008 4872
- (2008) Bioorg. Med. Chem. Lett. , vol.18 , pp. 4872
- Hughes, J.D.¹ Blagg, J.² Price, D.A.³ Bailey, S.⁴ Decrescenzo, G.A.⁵ Devraj, R.V.⁶ Ellsworth, E.⁷ Fobian, Y.M.⁸ Gibbs, M.E.⁹ Gilles, R.W.¹⁰ Greene, N.¹¹ Huang, E.¹² Krieger-Burke, T.¹³ Loesel, J.¹⁴ Wager, T.¹⁵ Whiteley, L.¹⁶ Zhang, Y.¹⁷

26
- 78650496072
- 35S-labeled MK-0499, a known hERG blocker
- 35S-labeled MK-0499, a known hERG blocker: W.A. Schmalhofer, A.M. Swensen, B.S. Thomas, J.P. Felix, R.J. Haedo, K. Solly, L. Kiss, G.J. Kaczorowski, and M.L. Garcia Assay Drug Dev. Technol. 8 2010 714
- (2010) Assay Drug Dev. Technol. , vol.8 , pp. 714
- Schmalhofer, W.A.¹ Swensen, A.M.² Thomas, B.S.³ Felix, J.P.⁴ Haedo, R.J.⁵ Solly, K.⁶ Kiss, L.⁷ Kaczorowski, G.J.⁸ Garcia, M.L.⁹

27
- 52949138265
- I.M. Bell, and M.T. Bilodeau Curr. Top. Med. Chem. 8 2008 1128
- (2008) Curr. Top. Med. Chem. , vol.8 , pp. 1128
- Bell, I.M.¹ Bilodeau, M.T.²

28
- 67349271581
- A. Mathur, J. Mo, M. Kraus, E. O'Hare, P. Sinclair, J. Young, S. Zhao, Y. Wang, J. Kopinja, X. Qu, J. Reilly, D. Walker, L. Xu, D. Aleksandrowicz, G. Marshall, M.L. Scott, N.E. Kohl, and E. Bachman Biochem. Pharmacol. 78 2009 382
- (2009) Biochem. Pharmacol. , vol.78 , pp. 382
- Mathur, A.¹ Mo, J.² Kraus, M.³ O'Hare, E.⁴ Sinclair, P.⁵ Young, J.⁶ Zhao, S.⁷ Wang, Y.⁸ Kopinja, J.⁹ Qu, X.¹⁰ Reilly, J.¹¹ Walker, D.¹² Xu, L.¹³ Aleksandrowicz, D.¹⁴ Marshall, G.¹⁵ Scott, M.L.¹⁶ Kohl, N.E.¹⁷ Bachman, E.¹⁸

29
- 84861314074
- M. Kraus, Y. Wang, D. Aleksandrowicz, E. Bachman, A.A. Szewczak, D. Walker, L. Xu, M. Bouthillette, K.M. Childers, B. Dolinski, A.M. Haidle, J. Kopinja, L. Lee, L. Lim, K.D. Little, Y. Ma, A. Mathur, J. Mo, E. O'Hare, R.D. Otte, B.M. Taoka, W. Wang, Y. Hong, A.A. Zabierek, W. Zhang, S. Zhao, J. Zhu, J. Young, and C.G. Marshall PLoS ONE 7 2012 e37207
- (2012) PLoS ONE , vol.7 , pp. 37207
- Kraus, M.¹ Wang, Y.² Aleksandrowicz, D.³ Bachman, E.⁴ Szewczak, A.A.⁵ Walker, D.⁶ Xu, L.⁷ Bouthillette, M.⁸ Childers, K.M.⁹ Dolinski, B.¹⁰ Haidle, A.M.¹¹ Kopinja, J.¹² Lee, L.¹³ Lim, L.¹⁴ Little, K.D.¹⁵ Ma, Y.¹⁶ Mathur, A.¹⁷ Mo, J.¹⁸ O'Hare, E.¹⁹ Otte, R.D.²⁰ more..

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