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Items: 38

1.

Discovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents.

Zhang Y, Zhao Y, Tebben AJ, Sheriff S, Ruzanov M, Fereshteh MP, Fan Y, Lippy J, Swanson J, Ho CP, Wautlet BS, Rose A, Parrish K, Yang Z, Donnell AF, Zhang L, Fink BE, Vite GD, Augustine-Rauch K, Fargnoli J, Borzilleri RM.

ACS Med Chem Lett. 2018 Oct 17;9(11):1117-1122. doi: 10.1021/acsmedchemlett.8b00357. eCollection 2018 Nov 8.

2.

Immune-modulating enzyme indoleamine 2,3-dioxygenase is effectively inhibited by targeting its apo-form.

Nelp MT, Kates PA, Hunt JT, Newitt JA, Balog A, Maley D, Zhu X, Abell L, Allentoff A, Borzilleri R, Lewis HA, Lin Z, Seitz SP, Yan C, Groves JT.

Proc Natl Acad Sci U S A. 2018 Mar 27;115(13):3249-3254. doi: 10.1073/pnas.1719190115. Epub 2018 Mar 12.

3.

Heterobicyclic inhibitors of transforming growth factor beta receptor I (TGFβRI).

Harikrishnan LS, Warrier J, Tebben AJ, Tonukunuru G, Madduri SR, Baligar V, Mannoori R, Seshadri B, Rahaman H, Arunachalam PN, Dikundwar AG, Fink BE, Fargnoli J, Fereshteh M, Fan Y, Lippy J, Ho CP, Wautlet B, Sheriff S, Ruzanov M, Borzilleri RM.

Bioorg Med Chem. 2018 Mar 1;26(5):1026-1034. doi: 10.1016/j.bmc.2018.01.014. Epub 2018 Jan 31.

PMID:
29422332
4.

Macrocyclic pyrrolobenzodiazepine dimers as antibody-drug conjugate payloads.

Donnell AF, Zhang Y, Stang EM, Wei DD, Tebben AJ, Perez HL, Schroeder GM, Pan C, Rao C, Borzilleri RM, Vite GD, Gangwar S.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5267-5271. doi: 10.1016/j.bmcl.2017.10.028. Epub 2017 Oct 16.

PMID:
29102228
5.

Decarboxylative Peptide Macrocyclization through Photoredox Catalysis.

McCarver SJ, Qiao JX, Carpenter J, Borzilleri RM, Poss MA, Eastgate MD, Miller MM, MacMillan DW.

Angew Chem Int Ed Engl. 2017 Jan 16;56(3):728-732. doi: 10.1002/anie.201608207. Epub 2016 Nov 17.

6.

Antroquinonol A: Scalable Synthesis and Preclinical Biology of a Phase 2 Drug Candidate.

Villaume MT, Sella E, Saul G, Borzilleri RM, Fargnoli J, Johnston KA, Zhang H, Fereshteh MP, Dhar TG, Baran PS.

ACS Cent Sci. 2016 Jan 27;2(1):27-31. doi: 10.1021/acscentsci.5b00345. Epub 2015 Dec 23.

7.

Ultrasensitive quantitative LC-MS/MS of an inhibitor of apoptosis protein's antagonist in plasma using protein target affinity extraction.

Discenza LN, Cornelius G, Gan J, Szapiel N, Talbott RL, Chaudhry C, Roy A, Borzilleri RM, Vuppugalla R, Stefanski K, Moore R, D'Arienzo CJ, Olah TV, Mehl JT.

Bioanalysis. 2016 Feb;8(4):265-74. doi: 10.4155/bio.15.246. Epub 2016 Jan 25.

PMID:
26807991
8.

Building homogeneous time-resolved fluorescence resonance energy transfer assays for characterization of bivalent inhibitors of an inhibitor of apoptosis protein target.

Chaudhry C, Davis J, Zhang Y, Posy S, Lei M, Shen H, Yan C, Devaux B, Zhang L, Blat Y, Metzler W, Borzilleri RM, Talbott RL.

Anal Biochem. 2016 Mar 15;497:8-17. doi: 10.1016/j.ab.2015.11.026. Epub 2015 Dec 30.

PMID:
26743718
9.

Pharmacology of smac mimetics; chemotype differentiation based on physical association with caspase regulators and cellular transport.

Talbott RL, Borzilleri RM, Chaudhry C, Fargnoli J, Shen H, Fairchild C, Barnhart B, Ortega M, McDonagh TE, Vuppugalla R, Vite GD, Hunt JT, Gottardis M, Naglich JG.

Exp Cell Res. 2015 Nov 1;338(2):251-60. doi: 10.1016/j.yexcr.2015.08.011. Epub 2015 Aug 21.

PMID:
26302264
10.

Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer.

Zhang Y, Seigal BA, Terrett NK, Talbott RL, Fargnoli J, Naglich JG, Chaudhry C, Posy SL, Vuppugalla R, Cornelius G, Lei M, Wang C, Zhang Y, Schmidt RJ, Wei DD, Miller MM, Allen MP, Li L, Carter PH, Vite GD, Borzilleri RM.

ACS Med Chem Lett. 2015 May 27;6(7):770-5. doi: 10.1021/acsmedchemlett.5b00091. eCollection 2015 Jul 9.

11.

The discovery of macrocyclic XIAP antagonists from a DNA-programmed chemistry library, and their optimization to give lead compounds with in vivo antitumor activity.

Seigal BA, Connors WH, Fraley A, Borzilleri RM, Carter PH, Emanuel SL, Fargnoli J, Kim K, Lei M, Naglich JG, Pokross ME, Posy SL, Shen H, Surti N, Talbott R, Zhang Y, Terrett NK.

J Med Chem. 2015 Mar 26;58(6):2855-61. doi: 10.1021/jm501892g. Epub 2015 Mar 12.

12.

Discovery of potent heterodimeric antagonists of inhibitor of apoptosis proteins (IAPs) with sustained antitumor activity.

Perez HL, Chaudhry C, Emanuel SL, Fanslau C, Fargnoli J, Gan J, Kim KS, Lei M, Naglich JG, Traeger SC, Vuppugalla R, Wei DD, Vite GD, Talbott RL, Borzilleri RM.

J Med Chem. 2015 Feb 12;58(3):1556-62. doi: 10.1021/jm501482t. Epub 2015 Jan 23.

PMID:
25584393
13.

Mcl-1 antagonism is a potential therapeutic strategy in a subset of solid cancers.

Modugno M, Banfi P, Gasparri F, Borzilleri R, Carter P, Cornelius L, Gottardis M, Lee V, Mapelli C, Naglich JG, Tebben A, Vite G, Pastori W, Albanese C, Corti E, Ballinari D, Galvani A.

Exp Cell Res. 2015 Mar 15;332(2):267-77. doi: 10.1016/j.yexcr.2014.11.022. Epub 2014 Dec 5.

PMID:
25486070
14.

Discovery of tetrahydroisoquinoline-based bivalent heterodimeric IAP antagonists.

Kim KS, Zhang L, Williams D, Perez HL, Stang E, Borzilleri RM, Posy S, Lei M, Chaudhry C, Emanuel S, Talbott R.

Bioorg Med Chem Lett. 2014 Nov 1;24(21):5022-9. doi: 10.1016/j.bmcl.2014.09.022. Epub 2014 Sep 16.

PMID:
25278234
15.

Antibody-drug conjugates: current status and future directions.

Perez HL, Cardarelli PM, Deshpande S, Gangwar S, Schroeder GM, Vite GD, Borzilleri RM.

Drug Discov Today. 2014 Jul;19(7):869-81. doi: 10.1016/j.drudis.2013.11.004. Epub 2013 Nov 15. Review.

PMID:
24239727
16.

Identification of a phenylacylsulfonamide series of dual Bcl-2/Bcl-xL antagonists.

Perez HL, Banfi P, Bertrand J, Cai ZW, Grebinski JW, Kim K, Lippy J, Modugno M, Naglich J, Schmidt RJ, Tebben A, Vianello P, Wei DD, Zhang L, Galvani A, Lombardo LJ, Borzilleri RM.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):3946-50. doi: 10.1016/j.bmcl.2012.04.103. Epub 2012 May 2.

PMID:
22608961
17.

Pyrazole and pyrimidine phenylacylsulfonamides as dual Bcl-2/Bcl-xL antagonists.

Schroeder GM, Wei D, Banfi P, Cai ZW, Lippy J, Menichincheri M, Modugno M, Naglich J, Penhallow B, Perez HL, Sack J, Schmidt RJ, Tebben A, Yan C, Zhang L, Galvani A, Lombardo LJ, Borzilleri RM.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):3951-6. doi: 10.1016/j.bmcl.2012.04.106. Epub 2012 Apr 30.

PMID:
22608393
18.

Cytochrome P450 11A1 bioactivation of a kinase inhibitor in rats: use of radioprofiling, modulation of metabolism, and adrenocortical cell lines to evaluate adrenal toxicity.

Zhang D, Flint O, Wang L, Gupta A, Westhouse RA, Zhao W, Raghavan N, Caceres-Cortes J, Marathe P, Shen G, Zhang Y, Allentoff A, Josephs J, Gan J, Borzilleri R, Humphreys WG.

Chem Res Toxicol. 2012 Mar 19;25(3):556-71. doi: 10.1021/tx200524d. Epub 2012 Mar 2.

PMID:
22295996
19.

Design, synthesis and structure-activity relationships of novel biarylamine-based Met kinase inhibitors.

Williams DK, Chen XT, Tarby C, Kaltenbach R, Cai ZW, Tokarski JS, An Y, Sack JS, Wautlet B, Gullo-Brown J, Henley BJ, Jeyaseelan R, Kellar K, Manne V, Trainor GL, Lombardo LJ, Fargnoli J, Borzilleri RM.

Bioorg Med Chem Lett. 2010 May 1;20(9):2998-3002. doi: 10.1016/j.bmcl.2010.01.042. Epub 2010 Jan 20.

PMID:
20382527
20.

Assessing compound binding to the Eg5 motor domain using a thermal shift assay.

McDonnell PA, Yanchunas J, Newitt JA, Tao L, Kiefer SE, Ortega M, Kut S, Burford N, Goldfarb V, Duke GJ, Shen H, Metzler W, Doyle M, Chen Z, Tarby C, Borzilleri R, Vaccaro W, Gottardis M, Lu S, Crews D, Kim K, Lombardo L, Roussell DL.

Anal Biochem. 2009 Sep 1;392(1):59-69. doi: 10.1016/j.ab.2009.05.044. Epub 2009 Jun 2.

PMID:
19497292
21.

Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.

Schroeder GM, An Y, Cai ZW, Chen XT, Clark C, Cornelius LA, Dai J, Gullo-Brown J, Gupta A, Henley B, Hunt JT, Jeyaseelan R, Kamath A, Kim K, Lippy J, Lombardo LJ, Manne V, Oppenheimer S, Sack JS, Schmidt RJ, Shen G, Stefanski K, Tokarski JS, Trainor GL, Wautlet BS, Wei D, Williams DK, Zhang Y, Zhang Y, Fargnoli J, Borzilleri RM.

J Med Chem. 2009 Mar 12;52(5):1251-4. doi: 10.1021/jm801586s.

PMID:
19260711
22.

Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities.

Kim KS, Zhang L, Schmidt R, Cai ZW, Wei D, Williams DK, Lombardo LJ, Trainor GL, Xie D, Zhang Y, An Y, Sack JS, Tokarski JS, Darienzo C, Kamath A, Marathe P, Zhang Y, Lippy J, Jeyaseelan R Sr, Wautlet B, Henley B, Gullo-Brown J, Manne V, Hunt JT, Fargnoli J, Borzilleri RM.

J Med Chem. 2008 Sep 11;51(17):5330-41. doi: 10.1021/jm800476q. Epub 2008 Aug 9.

PMID:
18690676
23.

Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors.

Cai ZW, Wei D, Schroeder GM, Cornelius LA, Kim K, Chen XT, Schmidt RJ, Williams DK, Tokarski JS, An Y, Sack JS, Manne V, Kamath A, Zhang Y, Marathe P, Hunt JT, Lombardo LJ, Fargnoli J, Borzilleri RM.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3224-9. doi: 10.1016/j.bmcl.2008.04.047. Epub 2008 Apr 25.

PMID:
18479916
24.

Preclinical discovery of ixabepilone, a highly active antineoplastic agent.

Lee FY, Borzilleri R, Fairchild CR, Kamath A, Smykla R, Kramer R, Vite G.

Cancer Chemother Pharmacol. 2008 Dec;63(1):157-66. doi: 10.1007/s00280-008-0724-8. Epub 2008 Mar 18. Review.

PMID:
18347795
25.

Identification of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of Met kinase.

Schroeder GM, Chen XT, Williams DK, Nirschl DS, Cai ZW, Wei D, Tokarski JS, An Y, Sack J, Chen Z, Huynh T, Vaccaro W, Poss M, Wautlet B, Gullo-Brown J, Kellar K, Manne V, Hunt JT, Wong TW, Lombardo LJ, Fargnoli J, Borzilleri RM.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1945-51. doi: 10.1016/j.bmcl.2008.01.121. Epub 2008 Feb 7.

PMID:
18289854
26.

Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 kinase inhibitor (BMS-540215).

Cai ZW, Zhang Y, Borzilleri RM, Qian L, Barbosa S, Wei D, Zheng X, Wu L, Fan J, Shi Z, Wautlet BS, Mortillo S, Jeyaseelan R Sr, Kukral DW, Kamath A, Marathe P, D'Arienzo C, Derbin G, Barrish JC, Robl JA, Hunt JT, Lombardo LJ, Fargnoli J, Bhide RS.

J Med Chem. 2008 Mar 27;51(6):1976-80. doi: 10.1021/jm7013309. Epub 2008 Feb 21.

PMID:
18288793
27.

Synthesis, SAR, and Evaluation of 4-[2,4-Difluoro-5-(cyclopropylcarbamoyl)phenylamino]pyrrolo[2,1-f][1,2,4]triazine-based VEGFR-2 kinase inhibitors.

Cai ZW, Wei D, Borzilleri RM, Qian L, Kamath A, Mortillo S, Wautlet B, Henley BJ, Jeyaseelan R Sr, Tokarski J, Hunt JT, Bhide RS, Fargnoli J, Lombardo LJ.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1354-8. doi: 10.1016/j.bmcl.2008.01.012. Epub 2008 Jan 9.

PMID:
18221875
28.

Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2.

Borzilleri RM, Bhide RS, Barrish JC, D'Arienzo CJ, Derbin GM, Fargnoli J, Hunt JT, Jeyaseelan R Sr, Kamath A, Kukral DW, Marathe P, Mortillo S, Qian L, Tokarski JS, Wautlet BS, Zheng X, Lombardo LJ.

J Med Chem. 2006 Jun 29;49(13):3766-9.

PMID:
16789733
29.

Synthesis and SAR of pyrrolotriazine-4-one based Eg5 inhibitors.

Kim KS, Lu S, Cornelius LA, Lombardo LJ, Borzilleri RM, Schroeder GM, Sheng C, Rovnyak G, Crews D, Schmidt RJ, Williams DK, Bhide RS, Traeger SC, McDonnell PA, Mueller L, Sheriff S, Newitt JA, Pudzianowski AT, Yang Z, Wild R, Lee FY, Batorsky R, Ryder JS, Ortega-Nanos M, Shen H, Gottardis M, Roussell DL.

Bioorg Med Chem Lett. 2006 Aug 1;16(15):3937-42. Epub 2006 May 30.

PMID:
16730979
30.

Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.

Bhide RS, Cai ZW, Zhang YZ, Qian L, Wei D, Barbosa S, Lombardo LJ, Borzilleri RM, Zheng X, Wu LI, Barrish JC, Kim SH, Leavitt K, Mathur A, Leith L, Chao S, Wautlet B, Mortillo S, Jeyaseelan R Sr, Kukral D, Hunt JT, Kamath A, Fura A, Vyas V, Marathe P, D'Arienzo C, Derbin G, Fargnoli J.

J Med Chem. 2006 Apr 6;49(7):2143-6.

PMID:
16570908
31.

Inhibitors of human mitotic kinesin Eg5: characterization of the 4-phenyl-tetrahydroisoquinoline lead series.

Tarby CM, Kaltenbach RF 3rd, Huynh T, Pudzianowski A, Shen H, Ortega-Nanos M, Sheriff S, Newitt JA, McDonnell PA, Burford N, Fairchild CR, Vaccaro W, Chen Z, Borzilleri RM, Naglich J, Lombardo LJ, Gottardis M, Trainor GL, Roussell DL.

Bioorg Med Chem Lett. 2006 Apr 15;16(8):2095-100. Epub 2006 Feb 3.

PMID:
16458511
32.

Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.

Borzilleri RM, Zheng X, Qian L, Ellis C, Cai ZW, Wautlet BS, Mortillo S, Jeyaseelan R Sr, Kukral DW, Fura A, Kamath A, Vyas V, Tokarski JS, Barrish JC, Hunt JT, Lombardo LJ, Fargnoli J, Bhide RS.

J Med Chem. 2005 Jun 16;48(12):3991-4008.

PMID:
15943473
33.

Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.

Borzilleri RM, Cai ZW, Ellis C, Fargnoli J, Fura A, Gerhardt T, Goyal B, Hunt JT, Mortillo S, Qian L, Tokarski J, Vyas V, Wautlet B, Zheng X, Bhide RS.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1429-33.

PMID:
15713401
34.

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.

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, Klei H, Marathe P, Pang S, Peterson R, Pitt S, Schieven GL, Schmidt RJ, Tokarski J, Wen ML, Wityak J, Borzilleri RM.

J Med Chem. 2004 Dec 30;47(27):6658-61.

PMID:
15615512
35.

Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template.

Hunt JT, Mitt T, Borzilleri R, Gullo-Brown J, Fargnoli J, Fink B, Han WC, Mortillo S, Vite G, Wautlet B, Wong T, Yu C, Zheng X, Bhide R.

J Med Chem. 2004 Jul 29;47(16):4054-9.

PMID:
15267243
36.

Synthesis and biological activity of novel epothilone aziridines.

Regueiro-Ren A, Borzilleri RM, Zheng X, Kim SH, Johnson JA, Fairchild CR, Lee FY, Long BH, Vite GD.

Org Lett. 2001 Aug 23;3(17):2693-6.

PMID:
11506611
37.

BMS-247550: a novel epothilone analog with a mode of action similar to paclitaxel but possessing superior antitumor efficacy.

Lee FY, Borzilleri R, Fairchild CR, Kim SH, Long BH, Reventos-Suarez C, Vite GD, Rose WC, Kramer RA.

Clin Cancer Res. 2001 May;7(5):1429-37.

38.

Synthesis of (9R,12S)- and (9S,12S)-Cycloisodityrosine and Their N-Methyl Derivatives.

Boger DL, Zhou J, Borzilleri RM, Nukui S, Castle SL.

J Org Chem. 1997 Apr 4;62(7):2054-2069.

PMID:
11671510

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