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Items: 11

1.

Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers.

Papillon JPN, Nakajima K, Adair CD, Hempel J, Jouk AO, Karki RG, Mathieu S, Möbitz H, Ntaganda R, Smith T, Visser M, Hill SE, Hurtado FK, Chenail G, Bhang HC, Bric A, Xiang K, Bushold G, Gilbert T, Vattay A, Dooley J, Costa EA, Park I, Li A, Farley D, Lounkine E, Yue QK, Xie X, Zhu X, Kulathila R, King D, Hu T, Vulic K, Cantwell J, Luu C, Jagani Z.

J Med Chem. 2018 Nov 21;61(22):10155-10172. doi: 10.1021/acs.jmedchem.8b01318. Epub 2018 Oct 31.

PMID:
30339381
2.

Discovery of 1-((6-Aminopyridin-3-yl)Methyl)-3-(4-Bromophenyl)Urea as a Potent, Irreversible Myeloperoxidase Inhibitor.

Marro ML, Patterson AW, Lee L, Deng L, Reynolds A, Ren X, Axford L, Patnaik A, Hollis-Symynkywicz M, Casson N, Custeau D, Ames L, Loi S, Zhang L, Honda T, Blank J, Harrison TJ, Papillon JPN, Hamann LG, Marcinkeviciene J, Regard JB.

J Pharmacol Exp Ther. 2018 Oct;367(1):147-154. doi: 10.1124/jpet.118.248435. Epub 2018 Aug 3.

PMID:
30076263
3.

Synthetic phospholipids as specific substrates for plasma endothelial lipase.

Papillon JP, Pan M, Brousseau ME, Gilchrist MA, Lou C, Singh AK, Stawicki T, Thompson JE.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3514-7. doi: 10.1016/j.bmcl.2016.06.032. Epub 2016 Jun 14.

PMID:
27344207
4.

Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects.

Papillon JP, Lou C, Singh AK, Adams CM, Ksander GM, Beil ME, Chen W, Leung-Chu J, Fu F, Gan L, Hu CW, Jeng AY, LaSala D, Liang G, Rigel DF, Russell KS, Vest JA, Watson C.

J Med Chem. 2015 Dec 10;58(23):9382-94. doi: 10.1021/acs.jmedchem.5b01545. Epub 2015 Nov 18.

PMID:
26540564
5.

Structure-Activity Relationships, Pharmacokinetics, and in Vivo Activity of CYP11B2 and CYP11B1 Inhibitors.

Papillon JP, Adams CM, Hu QY, Lou C, Singh AK, Zhang C, Carvalho J, Rajan S, Amaral A, Beil ME, Fu F, Gangl E, Hu CW, Jeng AY, LaSala D, Liang G, Logman M, Maniara WM, Rigel DF, Smith SA, Ksander GM.

J Med Chem. 2015 Jun 11;58(11):4749-70. doi: 10.1021/acs.jmedchem.5b00407. Epub 2015 May 21.

PMID:
25953419
6.

Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.

Meredith EL, Ksander G, Monovich LG, Papillon JP, Liu Q, Miranda K, Morris P, Rao C, Burgis R, Capparelli M, Hu QY, Singh A, Rigel DF, Jeng AY, Beil M, Fu F, Hu CW, LaSala D.

ACS Med Chem Lett. 2013 Oct 17;4(12):1203-7. doi: 10.1021/ml400324c. eCollection 2013 Dec 12.

7.

Ru-catalyzed alkene-alkyne coupling. Total synthesis of amphidinolide P.

Trost BM, Papillon JP, Nussbaumer T.

J Am Chem Soc. 2005 Dec 21;127(50):17921-37.

8.

Dinuclear asymmetric Zn aldol additions: formal asymmetric synthesis of fostriecin.

Trost BM, Frederiksen MU, Papillon JP, Harrington PE, Shin S, Shireman BT.

J Am Chem Soc. 2005 Mar 23;127(11):3666-7.

PMID:
15771479
9.

Alkene-alkyne coupling as a linchpin: an efficient and convergent synthesis of amphidinolide P.

Trost BM, Papillon JP.

J Am Chem Soc. 2004 Oct 27;126(42):13618-9.

PMID:
15493910
11.

The first syntheses of the 1-oxo-2-oxa-5-azaspiro[3.4]octane ring system found in oxazolomycin.

Papillon JP, Taylor RJ.

Org Lett. 2000 Jul 13;2(14):1987-90.

PMID:
10891211

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