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Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.

Fidanze SD, Liu D, Mantei RA, Hasvold LA, Pratt JK, Sheppard GS, Wang L, Holms JH, Dai Y, Aguirre A, Bogdan A, Dietrich JD, Marjanovic J, Park CH, Hutchins CW, Lin X, Bui MH, Huang X, Wilcox D, Li L, Wang R, Kovar P, Magoc TJ, Rajaraman G, Albert DH, Shen Y, Kati WM, McDaniel KF.

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1804-1810. doi: 10.1016/j.bmcl.2018.04.020. Epub 2018 Apr 11.


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.


Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors.

Lam LT, Lin X, Faivre EJ, Yang Z, Huang X, Wilcox DM, Bellin RJ, Jin S, Tahir SK, Mitten M, Magoc T, Bhathena A, Kati WM, Albert DH, Shen Y, Uziel T.

Mol Cancer Ther. 2017 Aug;16(8):1511-1520. doi: 10.1158/1535-7163.MCT-16-0459. Epub 2017 May 3.


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.


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.


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.


HEXIM1 as a Robust Pharmacodynamic Marker for Monitoring Target Engagement of BET Family Bromodomain Inhibitors in Tumors and Surrogate Tissues.

Lin X, Huang X, Uziel T, Hessler P, Albert DH, Roberts-Rapp LA, McDaniel KF, Kati WM, Shen Y.

Mol Cancer Ther. 2017 Feb;16(2):388-396. doi: 10.1158/1535-7163.MCT-16-0475. Epub 2016 Nov 30.


Exploitation of Castration-Resistant Prostate Cancer Transcription Factor Dependencies by the Novel BET Inhibitor ABBV-075.

Faivre EJ, Wilcox D, Lin X, Hessler P, Torrent M, He W, Uziel T, Albert DH, McDaniel K, Kati W, Shen Y.

Mol Cancer Res. 2017 Jan;15(1):35-44. doi: 10.1158/1541-7786.MCR-16-0221. Epub 2016 Oct 5.


Phase 1 dose escalation trial of ilorasertib, a dual Aurora/VEGF receptor kinase inhibitor, in patients with hematologic malignancies.

Garcia-Manero G, Tibes R, Kadia T, Kantarjian H, Arellano M, Knight EA, Xiong H, Qin Q, Munasinghe W, Roberts-Rapp L, Ansell P, Albert DH, Oliver B, McKee MD, Ricker JL, Khoury HJ.

Invest New Drugs. 2015 Aug;33(4):870-80. doi: 10.1007/s10637-015-0242-6. Epub 2015 May 2.


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.


Monitoring tumor response to linifanib therapy with SPECT/CT using the integrin αvβ3-targeted radiotracer 99mTc-3P-RGD2.

Ji S, Zhou Y, Voorbach MJ, Shao G, Zhang Y, Fox GB, Albert DH, Luo Y, Liu S, Mudd SR.

J Pharmacol Exp Ther. 2013 Aug;346(2):251-8. doi: 10.1124/jpet.112.202622. Epub 2013 Jun 7.


Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families.

Glaser KB, Li J, Marcotte PA, Magoc TJ, Guo J, Reuter DR, Tapang P, Wei RQ, Pease LJ, Bui MH, Chen Z, Frey RR, Johnson EF, Osterling DJ, Olson AM, Bouska JJ, Luo Y, Curtin ML, Donawho CK, Michaelides MR, Tse C, Davidsen SK, Albert DH.

J Pharmacol Exp Ther. 2012 Dec;343(3):617-27. doi: 10.1124/jpet.112.197087. Epub 2012 Aug 30.


Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.

Ji Z, Dai Y, Abad-Zapatero C, Albert DH, Bouska JJ, Glaser KB, Marcotte PA, Soni NB, Magoc TJ, Stewart KD, Wei RQ, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4528-31. doi: 10.1016/j.bmcl.2012.05.125. Epub 2012 Jun 7.


Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.

Curtin ML, Heyman HR, Frey RR, Marcotte PA, Glaser KB, Jankowski JR, Magoc TJ, Albert DH, Olson AM, Reuter DR, Bouska JJ, Montgomery DA, Palma JP, Donawho CK, Stewart KD, Tse C, Michaelides MR.

Bioorg Med Chem Lett. 2012 Jul 15;22(14):4750-5. doi: 10.1016/j.bmcl.2012.05.067. Epub 2012 May 26.


Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.

Curtin ML, Frey RR, Heyman HR, Soni NB, Marcotte PA, Pease LJ, Glaser KB, Magoc TJ, Tapang P, Albert DH, Osterling DJ, Olson AM, Bouska JJ, Guan Z, Preusser LC, Polakowski JS, Stewart KD, Tse C, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2012 May 1;22(9):3208-12. doi: 10.1016/j.bmcl.2012.03.035. Epub 2012 Mar 14.


FDG-PET as a pharmacodynamic biomarker for early assessment of treatment response to linifanib (ABT-869) in a non-small cell lung cancer xenograft model.

Mudd SR, Voorbach MJ, Reuter DR, Tapang P, Hickson JA, Refici-Buhr M, Fox GB, Albert DH, Luo Y, Day M.

Cancer Chemother Pharmacol. 2012 Jun;69(6):1669-72. doi: 10.1007/s00280-012-1840-z. Epub 2012 Feb 12.


Phase 1 trial of linifanib (ABT-869) in patients with refractory or relapsed acute myeloid leukemia.

Wang ES, Yee K, Koh LP, Hogge D, Enschede S, Carlson DM, Dudley M, Glaser K, McKeegan E, Albert DH, Li X, Pradhan R, Stock W.

Leuk Lymphoma. 2012 Aug;53(8):1543-51. doi: 10.3109/10428194.2012.660631. Epub 2012 Mar 1.


A novel multi-targeted tyrosine kinase inhibitor, linifanib (ABT-869), produces functional and structural changes in tumor vasculature in an orthotopic rat glioma model.

Luo Y, Jiang F, Cole TB, Hradil VP, Reuter D, Chakravartty A, Albert DH, Davidsen SK, Cox BF, McKeegan EM, Fox GB.

Cancer Chemother Pharmacol. 2012 Apr;69(4):911-21. doi: 10.1007/s00280-011-1740-7. Epub 2011 Nov 12.


Discovery of potent and selective thienopyrimidine inhibitors of Aurora kinases.

McClellan WJ, Dai Y, Abad-Zapatero C, Albert DH, Bouska JJ, Glaser KB, Magoc TJ, Marcotte PA, Osterling DJ, Stewart KD, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5620-4. doi: 10.1016/j.bmcl.2011.06.041. Epub 2011 Jun 29.


PRL-3, a metastasis associated tyrosine phosphatase, is involved in FLT3-ITD signaling and implicated in anti-AML therapy.

Zhou J, Bi C, Chng WJ, Cheong LL, Liu SC, Mahara S, Tay KG, Zeng Q, Li J, Guo K, Tan CP, Yu H, Albert DH, Chen CS.

PLoS One. 2011 May 12;6(5):e19798. doi: 10.1371/journal.pone.0019798.


ABT-869, a multitargeted receptor tyrosine kinase inhibitor, reduces tumor microvascularity and improves vascular wall integrity in preclinical tumor models.

Jiang F, Albert DH, Luo Y, Tapang P, Zhang K, Davidsen SK, Fox GB, Lesniewski R, McKeegan EM.

J Pharmacol Exp Ther. 2011 Jul;338(1):134-42. doi: 10.1124/jpet.110.178061. Epub 2011 Apr 19.


ABT-869, a promising multi-targeted tyrosine kinase inhibitor: from bench to bedside.

Zhou J, Goh BC, Albert DH, Chen CS.

J Hematol Oncol. 2009 Jul 30;2:33. doi: 10.1186/1756-8722-2-33. Review.


Effect of the multitargeted receptor tyrosine kinase inhibitor, ABT-869 [N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea], on blood pressure in conscious rats and mice: reversal with antihypertensive agents and effect on tumor growth inhibition.

Franklin PH, Banfor PN, Tapang P, Segreti JA, Widomski DL, Larson KJ, Noonan WT, Gintant GA, Davidsen SK, Albert DH, Fryer RM, Cox BF.

J Pharmacol Exp Ther. 2009 Jun;329(3):928-37. doi: 10.1124/jpet.108.144816. Epub 2009 Mar 2.


Identification of genes that confer tumor cell resistance to the aurora B kinase inhibitor, AZD1152.

Guo J, Anderson MG, Tapang P, Palma JP, Rodriguez LE, Niquette A, Li J, Bouska JJ, Wang G, Semizarov D, Albert DH, Donawho CK, Glaser KB, Shah OJ.

Pharmacogenomics J. 2009 Apr;9(2):90-102. doi: 10.1038/tpj.2008.20. Epub 2009 Feb 3.


ETA receptor blockade with atrasentan prevents hypertension with the multitargeted tyrosine kinase inhibitor ABT-869 in telemetry-instrumented rats.

Banfor PN, Franklin PA, Segreti JA, Widomski DL, Davidsen SK, Albert DH, Cox BF, Fryer RM, Gintant GA.

J Cardiovasc Pharmacol. 2009 Feb;53(2):173-8. doi: 10.1097/FJC.0b013e3181993493.


Enhanced activation of STAT pathways and overexpression of survivin confer resistance to FLT3 inhibitors and could be therapeutic targets in AML.

Zhou J, Bi C, Janakakumara JV, Liu SC, Chng WJ, Tay KG, Poon LF, Xie Z, Palaniyandi S, Yu H, Glaser KB, Albert DH, Davidsen SK, Chen CS.

Blood. 2009 Apr 23;113(17):4052-62. doi: 10.1182/blood-2008-05-156422. Epub 2009 Jan 14.


ABT-869, a multi-targeted tyrosine kinase inhibitor, in combination with rapamycin is effective for subcutaneous hepatocellular carcinoma xenograft.

Jasinghe VJ, Xie Z, Zhou J, Khng J, Poon LF, Senthilnathan P, Glaser KB, Albert DH, Davidsen SK, Chen CS.

J Hepatol. 2008 Dec;49(6):985-97. doi: 10.1016/j.jhep.2008.08.010. Epub 2008 Oct 1.


7-Aminopyrazolo[1,5-a]pyrimidines as potent multitargeted receptor tyrosine kinase inhibitors.

Frey RR, Curtin ML, Albert DH, Glaser KB, Pease LJ, Soni NB, Bouska JJ, Reuter D, Stewart KD, Marcotte P, Bukofzer G, Li J, Davidsen SK, Michaelides MR.

J Med Chem. 2008 Jul 10;51(13):3777-87. doi: 10.1021/jm701397k. Epub 2008 Jun 17.


3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases.

Ji Z, Ahmed AA, Albert DH, Bouska JJ, Bousquet PF, Cunha GA, Diaz G, Glaser KB, Guo J, Harris CM, Li J, Marcotte PA, Moskey MD, Oie T, Pease L, Soni NB, Stewart KD, Davidsen SK, Michaelides MR.

J Med Chem. 2008 Mar 13;51(5):1231-41. doi: 10.1021/jm701096v. Epub 2008 Feb 9.


In vivo activity of ABT-869, a multi-target kinase inhibitor, against acute myeloid leukemia with wild-type FLT3 receptor.

Zhou J, Khng J, Jasinghe VJ, Bi C, Neo CH, Pan M, Poon LF, Xie Z, Yu H, Yeoh AE, Lu Y, Glaser KB, Albert DH, Davidsen SK, Chen CS.

Leuk Res. 2008 Jul;32(7):1091-100. Epub 2007 Dec 26.


Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors.

Dai Y, Hartandi K, Soni NB, Pease LJ, Reuter DR, Olson AM, Osterling DJ, Doktor SZ, Albert DH, Bouska JJ, Glaser KB, Marcotte PA, Stewart KD, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):386-90. Epub 2007 Oct 17.


Synergistic antileukemic effects between ABT-869 and chemotherapy involve downregulation of cell cycle-regulated genes and c-Mos-mediated MAPK pathway.

Zhou J, Pan M, Xie Z, Loh SL, Bi C, Tai YC, Lilly M, Lim YP, Han JH, Glaser KB, Albert DH, Davidsen SK, Chen CS.

Leukemia. 2008 Jan;22(1):138-46. Epub 2007 Oct 18.


1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.

Dinges J, Albert DH, Arnold LD, Ashworth KL, Akritopoulou-Zanze I, Bousquet PF, Bouska JJ, Cunha GA, Davidsen SK, Diaz GJ, Djuric SW, Gasiecki AF, Gintant GA, Gracias VJ, Harris CM, Houseman KA, Hutchins CW, Johnson EF, Li H, Marcotte PA, Martin RL, Michaelides MR, Nyein M, Sowin TJ, Su Z, Tapang PH, Xia Z, Zhang HQ.

J Med Chem. 2007 May 3;50(9):2011-29. Epub 2007 Apr 11.


Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors.

Akritopoulou-Zanze I, Albert DH, Bousquet PF, Cunha GA, Harris CM, Moskey M, Dinges J, Stewart KD, Sowin TJ.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3136-40. Epub 2007 Mar 15.


Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.

Dai Y, Hartandi K, Ji Z, Ahmed AA, Albert DH, Bauch JL, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Harris CM, Hickman D, Guo J, Li J, Marcotte PA, Marsh KC, Moskey MD, Martin RL, Olson AM, Osterling DJ, Pease LJ, Soni NB, Stewart KD, Stoll VS, Tapang P, Reuter DR, Davidsen SK, Michaelides MR.

J Med Chem. 2007 Apr 5;50(7):1584-97. Epub 2007 Mar 8.


ABT-869, a multitargeted receptor tyrosine kinase inhibitor: inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia.

Shankar DB, Li J, Tapang P, Owen McCall J, Pease LJ, Dai Y, Wei RQ, Albert DH, Bouska JJ, Osterling DJ, Guo J, Marcotte PA, Johnson EF, Soni N, Hartandi K, Michaelides MR, Davidsen SK, Priceman SJ, Chang JC, Rhodes K, Shah N, Moore TB, Sakamoto KM, Glaser KB.

Blood. 2007 Apr 15;109(8):3400-8. Epub 2007 Jan 5.


Thienopyridine urea inhibitors of KDR kinase.

Heyman HR, Frey RR, Bousquet PF, Cunha GA, Moskey MD, Ahmed AA, Soni NB, Marcotte PA, Pease LJ, Glaser KB, Yates M, Bouska JJ, Albert DH, Black-Schaefer CL, Dandliker PJ, Stewart KD, Rafferty P, Davidsen SK, Michaelides MR, Curtin ML.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1246-9. Epub 2006 Dec 9.


Hypoxia-inducible factor-1 inhibition in combination with temozolomide treatment exhibits robust antitumor efficacy in vivo.

Li L, Lin X, Shoemaker AR, Albert DH, Fesik SW, Shen Y.

Clin Cancer Res. 2006 Aug 1;12(15):4747-54.


Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.

Ji Z, Ahmed AA, Albert DH, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Guo J, Li J, Marcotte PA, Moskey MD, Pease LJ, Stewart KD, Yates M, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2006 Aug 15;16(16):4326-30. Epub 2006 Jun 2.


Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor.

Albert DH, Tapang P, Magoc TJ, Pease LJ, Reuter DR, Wei RQ, Li J, Guo J, Bousquet PF, Ghoreishi-Haack NS, Wang B, Bukofzer GT, Wang YC, Stavropoulos JA, Hartandi K, Niquette AL, Soni N, Johnson EF, McCall JO, Bouska JJ, Luo Y, Donawho CK, Dai Y, Marcotte PA, Glaser KB, Michaelides MR, Davidsen SK.

Mol Cancer Ther. 2006 Apr;5(4):995-1006.


Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.

Dai Y, Guo Y, Frey RR, Ji Z, Curtin ML, Ahmed AA, Albert DH, Arnold L, Arries SS, Barlozzari T, Bauch JL, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Guo J, Li J, Marcotte PA, Marsh KC, Moskey MD, Pease LJ, Stewart KD, Stoll VS, Tapang P, Wishart N, Davidsen SK, Michaelides MR.

J Med Chem. 2005 Sep 22;48(19):6066-83.


Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2.

Wang J, Sheppard GS, Lou P, Kawai M, BaMaung N, Erickson SA, Tucker-Garcia L, Park C, Bouska J, Wang YC, Frost D, Tapang P, Albert DH, Morgan SJ, Morowitz M, Shusterman S, Maris JM, Lesniewski R, Henkin J.

Cancer Res. 2003 Nov 15;63(22):7861-9.


Role of class I and class II histone deacetylases in carcinoma cells using siRNA.

Glaser KB, Li J, Staver MJ, Wei RQ, Albert DH, Davidsen SK.

Biochem Biophys Res Commun. 2003 Oct 17;310(2):529-36.


Alpha-keto amides as inhibitors of histone deacetylase.

Wada CK, Frey RR, Ji Z, Curtin ML, Garland RB, Holms JH, Li J, Pease LJ, Guo J, Glaser KB, Marcotte PA, Richardson PL, Murphy SS, Bouska JJ, Tapang P, Magoc TJ, Albert DH, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3331-5.


Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.

Dai Y, Guo Y, Guo J, Pease LJ, Li J, Marcotte PA, Glaser KB, Tapang P, Albert DH, Richardson PL, Davidsen SK, Michaelides MR.

Bioorg Med Chem Lett. 2003 Jun 2;13(11):1897-901.


NMR-based modification of matrix metalloproteinase inhibitors with improved bioavailability.

Hajduk PJ, Shuker SB, Nettesheim DG, Craig R, Augeri DJ, Betebenner D, Albert DH, Guo Y, Meadows RP, Xu L, Michaelides M, Davidsen SK, Fesik SW.

J Med Chem. 2002 Dec 19;45(26):5628-39.


Phenoxyphenyl sulfone N-formylhydroxylamines (retrohydroxamates) as potent, selective, orally bioavailable matrix metalloproteinase inhibitors.

Wada CK, Holms JH, Curtin ML, Dai Y, Florjancic AS, Garland RB, Guo Y, Heyman HR, Stacey JR, Steinman DH, Albert DH, Bouska JJ, Elmore IN, Goodfellow CL, Marcotte PA, Tapang P, Morgan DW, Michaelides MR, Davidsen SK.

J Med Chem. 2002 Jan 3;45(1):219-32.


Characterization of matrix metalloproteinase inhibitors: angiogenesis and tumor models.

Albert DH, Davidsen SK.

Curr Protoc Pharmacol. 2001 Aug;Chapter 5:Unit5.23. doi: 10.1002/0471141755.ph0523s13.


Discovery and characterization of the potent, selective and orally bioavailable MMP inhibitor ABT-770.

Curtin ML, Florjancic AS, Heyman HR, Michaelides MR, Garland RB, Holms JH, Steinman DH, Dellaria JF, Gong J, Wada CK, Guo Y, Elmore IB, Tapang P, Albert DH, Magoc TJ, Marcotte PA, Bouska JJ, Goodfellow CL, Bauch JL, Marsh KC, Morgan DW, Davidsen SK.

Bioorg Med Chem Lett. 2001 Jun 18;11(12):1557-60.


Biaryl ether retrohydroxamates as potent, long-lived, orally bioavailable MMP inhibitors.

Michaelides MR, Dellaria JF, Gong J, Holms JH, Bouska JJ, Stacey J, Wada CK, Heyman HR, Curtin ML, Guo Y, Goodfellow CL, Elmore IB, Albert DH, Magoc TJ, Marcotte PA, Morgan DW, Davidsen SK.

Bioorg Med Chem Lett. 2001 Jun 18;11(12):1553-6.


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