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Items: 20

1.

Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.

Schnute ME, Wennerstål M, Alley J, Bengtsson M, Blinn JR, Bolten CW, Braden T, Bonn T, Carlsson B, Caspers N, Chen M, Choi C, Collis LP, Crouse K, Färnegårdh M, Fennell KF, Fish S, Flick AC, Goos-Nilsson A, Gullberg H, Harris PK, Heasley SE, Hegen M, Hromockyj AE, Hu X, Husman B, Janosik T, Jones P, Kaila N, Kallin E, Kauppi B, Kiefer JR, Knafels J, Koehler K, Kruger L, Kurumbail RG, Kyne RE Jr, Li W, Löfstedt J, Long SA, Menard CA, Mente S, Messing D, Meyers MJ, Napierata L, Nöteberg D, Nuhant P, Pelc MJ, Prinsen MJ, Rhönnstad P, Backström-Rydin E, Sandberg J, Sandström M, Shah F, Sjöberg M, Sundell A, Taylor AP, Thorarensen A, Trujillo JI, Trzupek JD, Unwalla R, Vajdos FF, Weinberg RA, Wood DC, Xing L, Zamaratski E, Zapf CW, Zhao Y, Wilhelmsson A, Berstein G.

J Med Chem. 2018 Dec 13;61(23):10415-10439. doi: 10.1021/acs.jmedchem.8b00392. Epub 2018 Sep 9.

PMID:
30130103
2.

Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.

Vazquez ML, Kaila N, Strohbach JW, Trzupek JD, Brown MF, Flanagan ME, Mitton-Fry MJ, Johnson TA, TenBrink RE, Arnold EP, Basak A, Heasley SE, Kwon S, Langille J, Parikh MD, Griffin SH, Casavant JM, Duclos BA, Fenwick AE, Harris TM, Han S, Caspers N, Dowty ME, Yang X, Banker ME, Hegen M, Symanowicz PT, Li L, Wang L, Lin TH, Jussif J, Clark JD, Telliez JB, Robinson RP, Unwalla R.

J Med Chem. 2018 Feb 8;61(3):1130-1152. doi: 10.1021/acs.jmedchem.7b01598. Epub 2018 Jan 23.

PMID:
29298069
3.

Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.

Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW.

J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14.

PMID:
28498658
4.

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.

Gerstenberger BS, Trzupek JD, Tallant C, Fedorov O, Filippakopoulos P, Brennan PE, Fedele V, Martin S, Picaud S, Rogers C, Parikh M, Taylor A, Samas B, O'Mahony A, Berg E, Pallares G, Torrey AD, Treiber DK, Samardjiev IJ, Nasipak BT, Padilla-Benavides T, Wu Q, Imbalzano AN, Nickerson JA, Bunnage ME, Müller S, Knapp S, Owen DR.

J Med Chem. 2016 May 26;59(10):4800-11. doi: 10.1021/acs.jmedchem.6b00012. Epub 2016 May 3.

5.

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.

Fedorov O, Castex J, Tallant C, Owen DR, Martin S, Aldeghi M, Monteiro O, Filippakopoulos P, Picaud S, Trzupek JD, Gerstenberger BS, Bountra C, Willmann D, Wells C, Philpott M, Rogers C, Biggin PC, Brennan PE, Bunnage ME, Schüle R, Günther T, Knapp S, Müller S.

Sci Adv. 2015 Nov 13;1(10):e1500723. doi: 10.1126/sciadv.1500723. eCollection 2015 Nov.

6.

Reversal of Diastereoselection in the Conjugate Addition of Cuprates to Unsaturated Lactams.

Wright SW, Choi C, Chung S, Boscoe BP, Drozda SE, Mousseau JJ, Trzupek JD.

Org Lett. 2015 Nov 6;17(21):5204-7. doi: 10.1021/acs.orglett.5b02533. Epub 2015 Oct 20.

PMID:
26485576
7.

Epigenetic drugs that do not target enzyme activity.

Owen DR, Trzupek JD.

Drug Discov Today Technol. 2014 Jun;12:e29-34. doi: 10.1016/j.ddtec.2012.10.008. Review.

PMID:
25027371
8.

Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.

Fish PV, Filippakopoulos P, Bish G, Brennan PE, Bunnage ME, Cook AS, Federov O, Gerstenberger BS, Jones H, Knapp S, Marsden B, Nocka K, Owen DR, Philpott M, Picaud S, Primiano MJ, Ralph MJ, Sciammetta N, Trzupek JD.

J Med Chem. 2012 Nov 26;55(22):9831-7. doi: 10.1021/jm3010515. Epub 2012 Nov 8.

9.

Lessons from the Total Synthesis of (±) Phalarine: Insights Into the Mechanism of the Pictet-Spengler Reaction.

Trzupek JD, Li C, Chan C, Crowley BM, Heimann AC, Danishefsky SJ.

Pure Appl Chem. 2010 Apr 6;82(9):1735-1748.

10.

Total synthesis of enantiopure phalarine via a stereospecific Pictet-Spengler reaction: traceless transfer of chirality from L-tryptophan.

Trzupek JD, Lee D, Crowley BM, Marathias VM, Danishefsky SJ.

J Am Chem Soc. 2010 Jun 23;132(24):8506-12. doi: 10.1021/ja1030968.

11.

Total synthesis of complestatin: development of a Pd(0)-mediated indole annulation for macrocyclization.

Shimamura H, Breazzano SP, Garfunkle J, Kimball FS, Trzupek JD, Boger DL.

J Am Chem Soc. 2010 Jun 9;132(22):7776-83. doi: 10.1021/ja102304p.

12.

Total synthesis of chloropeptin II (complestatin) and chloropeptin I.

Garfunkle J, Kimball FS, Trzupek JD, Takizawa S, Shimamura H, Tomishima M, Boger DL.

J Am Chem Soc. 2009 Nov 11;131(44):16036-8. doi: 10.1021/ja907193b.

13.

Toward homogeneous erythropoietin: chemical synthesis of the Ala1-Gly28 glycopeptide domain by "alanine" ligation.

Kan C, Trzupek JD, Wu B, Wan Q, Chen G, Tan Z, Yuan Y, Danishefsky SJ.

J Am Chem Soc. 2009 Apr 22;131(15):5438-43. doi: 10.1021/ja808707w.

14.

A unique class of duocarmycin and CC-1065 analogues subject to reductive activation.

Jin W, Trzupek JD, Rayl TJ, Broward MA, Vielhauer GA, Weir SJ, Hwang I, Boger DL.

J Am Chem Soc. 2007 Dec 12;129(49):15391-7. Epub 2007 Nov 17.

15.

Systematic exploration of the structural features of yatakemycin impacting DNA alkylation and biological activity.

Tichenor MS, MacMillan KS, Trzupek JD, Rayl TJ, Hwang I, Boger DL.

J Am Chem Soc. 2007 Sep 5;129(35):10858-69. Epub 2007 Aug 11.

16.

Asymmetric total synthesis of (+)- and ent-(-)-yatakemycin and duocarmycin SA: evaluation of yatakemycin key partial structures and its unnatural enantiomer.

Tichenor MS, Trzupek JD, Kastrinsky DB, Shiga F, Hwang I, Boger DL.

J Am Chem Soc. 2006 Dec 13;128(49):15683-96.

17.

A novel achiral seco-amino-cyclopropylindoline (CI) analog of CC-1065 and the duocarmycins: design, synthesis and biological studies.

Toth JL, Trzupek JD, Flores LV, Kiakos K, Hartley JA, Pennington WT, Lee M.

Med Chem. 2005 Jan;1(1):13-9.

PMID:
16789881
18.

Alkylation of duplex DNA in nucleosome core particles by duocarmycin SA and yatakemycin.

Trzupek JD, Gottesfeld JM, Boger DL.

Nat Chem Biol. 2006 Feb;2(2):79-82. Epub 2006 Jan 15.

PMID:
16415862
19.

Photochemical generation of ribose abasic sites in RNA oligonucleotides.

Trzupek JD, Sheppard TL.

Org Lett. 2005 Apr 14;7(8):1493-6.

PMID:
15816735
20.

Synthesis and evaluation of N-aryl and N-alkenyl CBI derivatives.

Parrish JP, Trzupek JD, Hughes TV, Hwang I, Boger DL.

Bioorg Med Chem. 2004 Nov 15;12(22):5845-56.

PMID:
15498660

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