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Items: 44

1.

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.

McDaniel KF, Wang L, Soltwedel T, Fidanze SD, Hasvold LA, Liu D, Mantei RA, Pratt JK, Sheppard GS, Bui MH, Faivre EJ, Huang X, Li L, Lin X, Wang R, Warder SE, Wilcox D, Albert DH, Magoc TJ, Rajaraman G, Park CH, Hutchins CW, Shen JJ, Edalji RP, Sun CC, Martin R, Gao W, Wong S, Fang G, Elmore SW, Shen Y, Kati WM.

J Med Chem. 2017 Oct 26;60(20):8369-8384. doi: 10.1021/acs.jmedchem.7b00746. Epub 2017 Oct 12.

PMID:
28949521
2.

Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies.

Bui MH, Lin X, Albert DH, Li L, Lam LT, Faivre EJ, Warder SE, Huang X, Wilcox D, Donawho CK, Sheppard GS, Wang L, Fidanze S, Pratt JK, Liu D, Hasvold L, Uziel T, Lu X, Kohlhapp F, Fang G, Elmore SW, Rosenberg SH, McDaniel KF, Kati WM, Shen Y.

Cancer Res. 2017 Jun 1;77(11):2976-2989. doi: 10.1158/0008-5472.CAN-16-1793. Epub 2017 Apr 17.

3.

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.

Wang L, Pratt JK, Soltwedel T, Sheppard GS, Fidanze SD, Liu D, Hasvold LA, Mantei RA, Holms JH, McClellan WJ, Wendt MD, Wada C, Frey R, Hansen TM, Hubbard R, Park CH, Li L, Magoc TJ, Albert DH, Lin X, Warder SE, Kovar P, Huang X, Wilcox D, Wang R, Rajaraman G, Petros AM, Hutchins CW, Panchal SC, Sun C, Elmore SW, Shen Y, Kati WM, McDaniel KF.

J Med Chem. 2017 May 11;60(9):3828-3850. doi: 10.1021/acs.jmedchem.7b00017. Epub 2017 Apr 21.

PMID:
28368119
4.

Methylpyrrole inhibitors of BET bromodomains.

Hasvold LA, Sheppard GS, Wang L, Fidanze SD, Liu D, Pratt JK, Mantei RA, Wada CK, Hubbard R, Shen Y, Lin X, Huang X, Warder SE, Wilcox D, Li L, Buchanan FG, Smithee L, Albert DH, Magoc TJ, Park CH, Petros AM, Panchal SC, Sun C, Kovar P, Soni NB, Elmore SW, Kati WM, McDaniel KF.

Bioorg Med Chem Lett. 2017 May 15;27(10):2225-2233. doi: 10.1016/j.bmcl.2017.02.057. Epub 2017 Feb 24.

PMID:
28268136
5.

MCL-1 Is a Key Determinant of Breast Cancer Cell Survival: Validation of MCL-1 Dependency Utilizing a Highly Selective Small Molecule Inhibitor.

Xiao Y, Nimmer P, Sheppard GS, Bruncko M, Hessler P, Lu X, Roberts-Rapp L, Pappano WN, Elmore SW, Souers AJ, Leverson JD, Phillips DC.

Mol Cancer Ther. 2015 Aug;14(8):1837-47. doi: 10.1158/1535-7163.MCT-14-0928. Epub 2015 May 26.

6.

Correction to Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity.

Bruncko M, Wang L, Sheppard GS, Phillips DC, Tahir SK, Xue J, Erickson S, Fidanze S, Fry E, Hasvold L, Jenkins GJ, Jin S, Judge RA, Kovar PJ, Madar D, Nimmer P, Park C, Petros AM, Rosenberg SH, Smith ML, Song X, Sun C, Tao ZF, Wang X, Xiao Y, Zhang H, Tse C, Leverson JD, Elmore SW, Souers AJ.

J Med Chem. 2015 May 14;58(9):4089. doi: 10.1021/acs.jmedchem.5b00616. Epub 2015 May 1. No abstract available.

PMID:
25933255
7.

Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy.

Leverson JD, Phillips DC, Mitten MJ, Boghaert ER, Diaz D, Tahir SK, Belmont LD, Nimmer P, Xiao Y, Ma XM, Lowes KN, Kovar P, Chen J, Jin S, Smith M, Xue J, Zhang H, Oleksijew A, Magoc TJ, Vaidya KS, Albert DH, Tarrant JM, La N, Wang L, Tao ZF, Wendt MD, Sampath D, Rosenberg SH, Tse C, Huang DC, Fairbrother WJ, Elmore SW, Souers AJ.

Sci Transl Med. 2015 Mar 18;7(279):279ra40. doi: 10.1126/scitranslmed.aaa4642.

PMID:
25787766
8.

Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.

Bruncko M, Wang L, Sheppard GS, Phillips DC, Tahir SK, Xue J, Erickson S, Fidanze S, Fry E, Hasvold L, Jenkins GJ, Jin S, Judge RA, Kovar PJ, Madar D, Nimmer P, Park C, Petros AM, Rosenberg SH, Smith ML, Song X, Sun C, Tao ZF, Wang X, Xiao Y, Zhang H, Tse C, Leverson JD, Elmore SW, Souers AJ.

J Med Chem. 2015 Mar 12;58(5):2180-94. doi: 10.1021/jm501258m. Epub 2015 Feb 26. Erratum in: J Med Chem. 2015 May 14;58(9):4089.

PMID:
25679114
9.

Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax).

Leverson JD, Zhang H, Chen J, Tahir SK, Phillips DC, Xue J, Nimmer P, Jin S, Smith M, Xiao Y, Kovar P, Tanaka A, Bruncko M, Sheppard GS, Wang L, Gierke S, Kategaya L, Anderson DJ, Wong C, Eastham-Anderson J, Ludlam MJ, Sampath D, Fairbrother WJ, Wertz I, Rosenberg SH, Tse C, Elmore SW, Souers AJ.

Cell Death Dis. 2015 Jan 15;6:e1590. doi: 10.1038/cddis.2014.561.

10.

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.

Tao ZF, Hasvold L, Wang L, Wang X, Petros AM, Park CH, Boghaert ER, Catron ND, Chen J, Colman PM, Czabotar PE, Deshayes K, Fairbrother WJ, Flygare JA, Hymowitz SG, Jin S, Judge RA, Koehler MF, Kovar PJ, Lessene G, Mitten MJ, Ndubaku CO, Nimmer P, Purkey HE, Oleksijew A, Phillips DC, Sleebs BE, Smith BJ, Smith ML, Tahir SK, Watson KG, Xiao Y, Xue J, Zhang H, Zobel K, Rosenberg SH, Tse C, Leverson JD, Elmore SW, Souers AJ.

ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93. doi: 10.1021/ml5001867. eCollection 2014 Oct 9.

11.

Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL.

Koehler MF, Bergeron P, Choo EF, Lau K, Ndubaku C, Dudley D, Gibbons P, Sleebs BE, Rye CS, Nikolakopoulos G, Bui C, Kulasegaram S, Kersten WJ, Smith BJ, Czabotar PE, Colman PM, Huang DC, Baell JB, Watson KG, Hasvold L, Tao ZF, Wang L, Souers AJ, Elmore SW, Flygare JA, Fairbrother WJ, Lessene G.

ACS Med Chem Lett. 2014 Mar 21;5(6):662-7. doi: 10.1021/ml500030p. eCollection 2014 Jun 12.

12.

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.

Souers AJ, Leverson JD, Boghaert ER, Ackler SL, Catron ND, Chen J, Dayton BD, Ding H, Enschede SH, Fairbrother WJ, Huang DC, Hymowitz SG, Jin S, Khaw SL, Kovar PJ, Lam LT, Lee J, Maecker HL, Marsh KC, Mason KD, Mitten MJ, Nimmer PM, Oleksijew A, Park CH, Park CM, Phillips DC, Roberts AW, Sampath D, Seymour JF, Smith ML, Sullivan GM, Tahir SK, Tse C, Wendt MD, Xiao Y, Xue JC, Zhang H, Humerickhouse RA, Rosenberg SH, Elmore SW.

Nat Med. 2013 Feb;19(2):202-8. doi: 10.1038/nm.3048. Epub 2013 Jan 6.

PMID:
23291630
13.

The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo.

Chen J, Jin S, Abraham V, Huang X, Liu B, Mitten MJ, Nimmer P, Lin X, Smith M, Shen Y, Shoemaker AR, Tahir SK, Zhang H, Ackler SL, Rosenberg SH, Maecker H, Sampath D, Leverson JD, Tse C, Elmore SW.

Mol Cancer Ther. 2011 Dec;10(12):2340-9. doi: 10.1158/1535-7163.MCT-11-0415. Epub 2011 Sep 13.

14.

Mcl-1 is critical for survival in a subgroup of non-small-cell lung cancer cell lines.

Zhang H, Guttikonda S, Roberts L, Uziel T, Semizarov D, Elmore SW, Leverson JD, Lam LT.

Oncogene. 2011 Apr 21;30(16):1963-8. doi: 10.1038/onc.2010.559. Epub 2010 Dec 6.

PMID:
21132008
15.

N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors.

Bruncko M, Tahir SK, Song X, Chen J, Ding H, Huth JR, Jin S, Judge RA, Madar DJ, Park CH, Park CM, Petros AM, Tse C, Rosenberg SH, Elmore SW.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7503-6. doi: 10.1016/j.bmcl.2010.10.010. Epub 2010 Oct 12.

PMID:
21106457
16.

Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity.

Wilson WH, O'Connor OA, Czuczman MS, LaCasce AS, Gerecitano JF, Leonard JP, Tulpule A, Dunleavy K, Xiong H, Chiu YL, Cui Y, Busman T, Elmore SW, Rosenberg SH, Krivoshik AP, Enschede SH, Humerickhouse RA.

Lancet Oncol. 2010 Dec;11(12):1149-59. doi: 10.1016/S1470-2045(10)70261-8. Epub 2010 Nov 18.

17.

Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR.

Petros AM, Huth JR, Oost T, Park CM, Ding H, Wang X, Zhang H, Nimmer P, Mendoza R, Sun C, Mack J, Walter K, Dorwin S, Gramling E, Ladror U, Rosenberg SH, Elmore SW, Fesik SW, Hajduk PJ.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6587-91. doi: 10.1016/j.bmcl.2010.09.033. Epub 2010 Sep 15.

PMID:
20870405
18.

Identification of expression signatures predictive of sensitivity to the Bcl-2 family member inhibitor ABT-263 in small cell lung carcinoma and leukemia/lymphoma cell lines.

Tahir SK, Wass J, Joseph MK, Devanarayan V, Hessler P, Zhang H, Elmore SW, Kroeger PE, Tse C, Rosenberg SH, Anderson MG.

Mol Cancer Ther. 2010 Mar;9(3):545-57. doi: 10.1158/1535-7163.MCT-09-0651. Epub 2010 Feb 23.

19.

The Bcl-2 inhibitor ABT-263 enhances the response of multiple chemotherapeutic regimens in hematologic tumors in vivo.

Ackler S, Mitten MJ, Foster K, Oleksijew A, Refici M, Tahir SK, Xiao Y, Tse C, Frost DJ, Fesik SW, Rosenberg SH, Elmore SW, Shoemaker AR.

Cancer Chemother Pharmacol. 2010 Oct;66(5):869-80. doi: 10.1007/s00280-009-1232-1. Epub 2010 Jan 23.

PMID:
20099064
20.

The Bcl-2 family antagonist ABT-737 significantly inhibits multiple animal models of autoimmunity.

Bardwell PD, Gu J, McCarthy D, Wallace C, Bryant S, Goess C, Mathieu S, Grinnell C, Erickson J, Rosenberg SH, Schwartz AJ, Hugunin M, Tarcsa E, Elmore SW, McRae B, Murtaza A, Wang LC, Ghayur T.

J Immunol. 2009 Jun 15;182(12):7482-9. doi: 10.4049/jimmunol.0802813.

21.

ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo.

Ackler S, Xiao Y, Mitten MJ, Foster K, Oleksijew A, Refici M, Schlessinger S, Wang B, Chemburkar SR, Bauch J, Tse C, Frost DJ, Fesik SW, Rosenberg SH, Elmore SW, Shoemaker AR.

Mol Cancer Ther. 2008 Oct;7(10):3265-74. doi: 10.1158/1535-7163.MCT-08-0268.

22.

Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.

Park CM, Bruncko M, Adickes J, Bauch J, Ding H, Kunzer A, Marsh KC, Nimmer P, Shoemaker AR, Song X, Tahir SK, Tse C, Wang X, Wendt MD, Yang X, Zhang H, Fesik SW, Rosenberg SH, Elmore SW.

J Med Chem. 2008 Nov 13;51(21):6902-15. doi: 10.1021/jm800669s. Epub 2008 Oct 8.

PMID:
18841882
23.

Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models.

Shoemaker AR, Mitten MJ, Adickes J, Ackler S, Refici M, Ferguson D, Oleksijew A, O'Connor JM, Wang B, Frost DJ, Bauch J, Marsh K, Tahir SK, Yang X, Tse C, Fesik SW, Rosenberg SH, Elmore SW.

Clin Cancer Res. 2008 Jun 1;14(11):3268-77. doi: 10.1158/1078-0432.CCR-07-4622.

24.

ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor.

Tse C, Shoemaker AR, Adickes J, Anderson MG, Chen J, Jin S, Johnson EF, Marsh KC, Mitten MJ, Nimmer P, Roberts L, Tahir SK, Xiao Y, Yang X, Zhang H, Fesik S, Rosenberg SH, Elmore SW.

Cancer Res. 2008 May 1;68(9):3421-8. doi: 10.1158/0008-5472.CAN-07-5836.

25.

Discovery and design of novel HSP90 inhibitors using multiple fragment-based design strategies.

Huth JR, Park C, Petros AM, Kunzer AR, Wendt MD, Wang X, Lynch CL, Mack JC, Swift KM, Judge RA, Chen J, Richardson PL, Jin S, Tahir SK, Matayoshi ED, Dorwin SA, Ladror US, Severin JM, Walter KA, Bartley DM, Fesik SW, Elmore SW, Hajduk PJ.

Chem Biol Drug Des. 2007 Jul;70(1):1-12.

PMID:
17630989
26.

Discovery of a novel small molecule binding site of human survivin.

Wendt MD, Sun C, Kunzer A, Sauer D, Sarris K, Hoff E, Yu L, Nettesheim DG, Chen J, Jin S, Comess KM, Fan Y, Anderson SN, Isaac B, Olejniczak ET, Hajduk PJ, Rosenberg SH, Elmore SW.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3122-9. Epub 2007 Mar 16.

PMID:
17391963
27.

Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737.

Tahir SK, Yang X, Anderson MG, Morgan-Lappe SE, Sarthy AV, Chen J, Warner RB, Ng SC, Fesik SW, Elmore SW, Rosenberg SH, Tse C.

Cancer Res. 2007 Feb 1;67(3):1176-83.

28.

Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.

Bruncko M, Oost TK, Belli BA, Ding H, Joseph MK, Kunzer A, Martineau D, McClellan WJ, Mitten M, Ng SC, Nimmer PM, Oltersdorf T, Park CM, Petros AM, Shoemaker AR, Song X, Wang X, Wendt MD, Zhang H, Fesik SW, Rosenberg SH, Elmore SW.

J Med Chem. 2007 Feb 22;50(4):641-62. Epub 2007 Jan 26.

PMID:
17256834
29.

Bcl-2 family proteins are essential for platelet survival.

Zhang H, Nimmer PM, Tahir SK, Chen J, Fryer RM, Hahn KR, Iciek LA, Morgan SJ, Nasarre MC, Nelson R, Preusser LC, Reinhart GA, Smith ML, Rosenberg SH, Elmore SW, Tse C.

Cell Death Differ. 2007 May;14(5):943-51. Epub 2007 Jan 5.

30.

Design, synthesis, and computational studies of inhibitors of Bcl-XL.

Park CM, Oie T, Petros AM, Zhang H, Nimmer PM, Henry RF, Elmore SW.

J Am Chem Soc. 2006 Dec 20;128(50):16206-12.

PMID:
17165773
31.

A small-molecule inhibitor of Bcl-XL potentiates the activity of cytotoxic drugs in vitro and in vivo.

Shoemaker AR, Oleksijew A, Bauch J, Belli BA, Borre T, Bruncko M, Deckwirth T, Frost DJ, Jarvis K, Joseph MK, Marsh K, McClellan W, Nellans H, Ng S, Nimmer P, O'Connor JM, Oltersdorf T, Qing W, Shen W, Stavropoulos J, Tahir SK, Wang B, Warner R, Zhang H, Fesik SW, Rosenberg SH, Elmore SW.

Cancer Res. 2006 Sep 1;66(17):8731-9.

32.

Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo.

Wendt MD, Shen W, Kunzer A, McClellan WJ, Bruncko M, Oost TK, Ding H, Joseph MK, Zhang H, Nimmer PM, Ng SC, Shoemaker AR, Petros AM, Oleksijew A, Marsh K, Bauch J, Oltersdorf T, Belli BA, Martineau D, Fesik SW, Rosenberg SH, Elmore SW.

J Med Chem. 2006 Feb 9;49(3):1165-81.

PMID:
16451081
33.

Discovery of a potent inhibitor of the antiapoptotic protein Bcl-xL from NMR and parallel synthesis.

Petros AM, Dinges J, Augeri DJ, Baumeister SA, Betebenner DA, Bures MG, Elmore SW, Hajduk PJ, Joseph MK, Landis SK, Nettesheim DG, Rosenberg SH, Shen W, Thomas S, Wang X, Zanze I, Zhang H, Fesik SW.

J Med Chem. 2006 Jan 26;49(2):656-63.

PMID:
16420051
34.

An inhibitor of Bcl-2 family proteins induces regression of solid tumours.

Oltersdorf T, Elmore SW, Shoemaker AR, Armstrong RC, Augeri DJ, Belli BA, Bruncko M, Deckwerth TL, Dinges J, Hajduk PJ, Joseph MK, Kitada S, Korsmeyer SJ, Kunzer AR, Letai A, Li C, Mitten MJ, Nettesheim DG, Ng S, Nimmer PM, O'Connor JM, Oleksijew A, Petros AM, Reed JC, Shen W, Tahir SK, Thompson CB, Tomaselli KJ, Wang B, Wendt MD, Zhang H, Fesik SW, Rosenberg SH.

Nature. 2005 Jun 2;435(7042):677-81. Epub 2005 May 15.

35.

Non-peptidic small molecule inhibitors of XIAP.

Park CM, Sun C, Olejniczak ET, Wilson AE, Meadows RP, Betz SF, Elmore SW, Fesik SW.

Bioorg Med Chem Lett. 2005 Feb 1;15(3):771-5.

PMID:
15664855
36.

Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.

Oost TK, Sun C, Armstrong RC, Al-Assaad AS, Betz SF, Deckwerth TL, Ding H, Elmore SW, Meadows RP, Olejniczak ET, Oleksijew A, Oltersdorf T, Rosenberg SH, Shoemaker AR, Tomaselli KJ, Zou H, Fesik SW.

J Med Chem. 2004 Aug 26;47(18):4417-26.

PMID:
15317454
37.

Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.

Elmore SW, Pratt JK, Coghlan MJ, Mao Y, Green BE, Anderson DD, Stashko MA, Lin CW, Falls D, Nakane M, Miller L, Tyree CM, Miner JN, Lane B.

Bioorg Med Chem Lett. 2004 Apr 5;14(7):1721-7.

PMID:
15026058
38.

The pursuit of differentiated ligands for the glucocorticoid receptor.

Coghlan MJ, Elmore SW, Kym PR, Kort ME.

Curr Top Med Chem. 2003;3(14):1617-35. Review.

PMID:
14683518
39.

Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.

Kym PR, Kort ME, Coghlan MJ, Moore JL, Tang R, Ratajczyk JD, Larson DP, Elmore SW, Pratt JK, Stashko MA, Falls HD, Lin CW, Nakane M, Miller L, Tyree CM, Miner JN, Jacobson PB, Wilcox DM, Nguyen P, Lane BC.

J Med Chem. 2003 Mar 13;46(6):1016-30.

PMID:
12620078
40.

A novel antiinflammatory maintains glucocorticoid efficacy with reduced side effects.

Coghlan MJ, Jacobson PB, Lane B, Nakane M, Lin CW, Elmore SW, Kym PR, Luly JR, Carter GW, Turner R, Tyree CM, Hu J, Elgort M, Rosen J, Miner JN.

Mol Endocrinol. 2003 May;17(5):860-9. Epub 2003 Feb 13.

PMID:
12586843
41.

Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.

Elmore SW, Coghlan MJ, Anderson DD, Pratt JK, Green BE, Wang AX, Stashko MA, Lin CW, Tyree CM, Miner JN, Jacobson PB, Wilcox DM, Lane BC.

J Med Chem. 2001 Dec 6;44(25):4481-91.

PMID:
11728194
42.

Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.

Coghlan MJ, Kym PR, Elmore SW, Wang AX, Luly JR, Wilcox D, Stashko M, Lin CW, Miner J, Tyree C, Nakane M, Jacobson P, Lane BC.

J Med Chem. 2001 Aug 30;44(18):2879-85.

PMID:
11520196
43.

Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).

Meyer MD, Altenbach RJ, Basha FZ, Carroll WA, Condon S, Elmore SW, Kerwin JF Jr, Sippy KB, Tietje K, Wendt MD, Hancock AA, Brune ME, Buckner SA, Drizin I.

J Med Chem. 2000 Apr 20;43(8):1586-603.

PMID:
10780916
44.

Synthesis and pharmacological characterization of 3-[2-((3aR,9bR)-cis-6-methoxy-2,3,3a,4,5,9b-hexahydro-1H-benz[e] isoindol-2-yl)ethyl]pyrido-[3',4':4,5]thieno[3,2-d]pyrimidine-2,4 (1H,3H)-dione (A-131701): a uroselective alpha 1A adrenoceptor antagonist for the symptomatic treatment of benign prostatic hyperplasia.

Meyer MD, Altenbach RJ, Basha FZ, Carroll WA, Drizin I, Elmore SW, Ehrlich PP, Lebold SA, Tietje K, Sippy KB, Wendt MD, Plata DJ, Plagge F, Buckner SA, Brune ME, Hancock AA, Kerwin JF Jr.

J Med Chem. 1997 Sep 26;40(20):3141-3. No abstract available.

PMID:
9379432

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