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Items: 16

1.

Development of indazole mineralocorticoid receptor antagonists and investigation into their selective late-stage functionalization.

Liu K, Kurukulasuriya R, Dykstra K, DiMichelle L, Liu J, Vachal P, Ogawa A, DeVita RJ, Shen DM, Tan Q, Chen Y, Gauthier D, Verras A, Crespo A, Zamlynny B, Madwed J, Hoek M, Bateman T, Yang YF, Houk KN, Krska S, Cernak T.

Bioorg Med Chem Lett. 2019 Jul 15;29(14):1854-1858. doi: 10.1016/j.bmcl.2019.04.024. Epub 2019 Apr 15.

PMID:
31104995
2.

Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC).

Yu Y, Wu Z, Shi ZC, He S, Lai Z, Cernak TA, Vachal P, Liu M, Liu J, Hong Q, Jian T, Guiadeen D, Krikorian A, Sperbeck DM, Verras A, Sonatore LM, Murphy BA, Wiltsie J, Chung CC, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, De Vita RJ, Pinto S, Nargund RP.

Bioorg Med Chem Lett. 2019 Jun 1;29(11):1380-1385. doi: 10.1016/j.bmcl.2019.03.039. Epub 2019 Mar 27.

PMID:
30952592
3.

Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.

He S, Lai Z, Hong Q, Shang J, Reibarkh M, Kuethe JT, Liu J, Guiadeen D, Krikorian AD, Cernak TA, Dykstra KD, Sperbeck DM, Wu Z, Yu Y, Yang GX, Jian T, Verras A, Sonatore LM, Wiltsie J, Chung CC, Murphy BA, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ.

Bioorg Med Chem Lett. 2019 May 15;29(10):1182-1186. doi: 10.1016/j.bmcl.2019.03.025. Epub 2019 Mar 21.

PMID:
30926247
4.

Pharmaceutical diversification via palladium oxidative addition complexes.

Uehling MR, King RP, Krska SW, Cernak T, Buchwald SL.

Science. 2019 Jan 25;363(6425):405-408. doi: 10.1126/science.aac6153.

PMID:
30679373
5.

Mapping the dark space of chemical reactions with extended nanomole synthesis and MALDI-TOF MS.

Lin S, Dikler S, Blincoe WD, Ferguson RD, Sheridan RP, Peng Z, Conway DV, Zawatzky K, Wang H, Cernak T, Davies IW, DiRocco DA, Sheng H, Welch CJ, Dreher SD.

Science. 2018 Aug 10;361(6402). pii: eaar6236. doi: 10.1126/science.aar6236. Epub 2018 May 24.

PMID:
29794218
6.

Nanoscale synthesis and affinity ranking.

Gesmundo NJ, Sauvagnat B, Curran PJ, Richards MP, Andrews CL, Dandliker PJ, Cernak T.

Nature. 2018 May;557(7704):228-232. doi: 10.1038/s41586-018-0056-8. Epub 2018 Apr 23.

PMID:
29686415
7.

Correction: The medicinal chemist's toolbox for late stage functionalization of drug-like molecules.

Cernak T, Dykstra KD, Tyagarajan S, Vachal P, Krska SW.

Chem Soc Rev. 2017 Mar 21;46(6):1760. doi: 10.1039/c7cs90023f.

PMID:
28280821
8.

Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.

Cernak T, Gesmundo NJ, Dykstra K, Yu Y, Wu Z, Shi ZC, Vachal P, Sperbeck D, He S, Murphy BA, Sonatore L, Williams S, Madeira M, Verras A, Reiter M, Lee CH, Cuff J, Sherer EC, Kuethe J, Goble S, Perrotto N, Pinto S, Shen DM, Nargund R, Balkovec J, DeVita RJ, Dreher SD.

J Med Chem. 2017 May 11;60(9):3594-3605. doi: 10.1021/acs.jmedchem.6b01543. Epub 2017 Mar 2.

PMID:
28252959
9.

Chemistry informer libraries: a chemoinformatics enabled approach to evaluate and advance synthetic methods.

Kutchukian PS, Dropinski JF, Dykstra KD, Li B, DiRocco DA, Streckfuss EC, Campeau LC, Cernak T, Vachal P, Davies IW, Krska SW, Dreher SD.

Chem Sci. 2016 Apr 21;7(4):2604-2613. doi: 10.1039/c5sc04751j. Epub 2016 Jan 26.

10.

The medicinal chemist's toolbox for late stage functionalization of drug-like molecules.

Cernak T, Dykstra KD, Tyagarajan S, Vachal P, Krska SW.

Chem Soc Rev. 2016 Feb 7;45(3):546-76. doi: 10.1039/c5cs00628g. Epub 2015 Oct 28. Erratum in: Chem Soc Rev. 2017 Mar 21;46(6):1760.

PMID:
26507237
11.

Organic chemistry. Nanomole-scale high-throughput chemistry for the synthesis of complex molecules.

Buitrago Santanilla A, Regalado EL, Pereira T, Shevlin M, Bateman K, Campeau LC, Schneeweis J, Berritt S, Shi ZC, Nantermet P, Liu Y, Helmy R, Welch CJ, Vachal P, Davies IW, Cernak T, Dreher SD.

Science. 2015 Jan 2;347(6217):49-53. doi: 10.1126/science.1259203. Epub 2014 Nov 20.

12.

Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.

He S, Hong Q, Lai Z, Yang DX, Ting PC, Kuethe JT, Cernak TA, Dykstra KD, Sperbeck DM, Wu Z, Yu Y, Yang GX, Jian T, Liu J, Guiadeen D, Krikorian AD, Sonatore LM, Wiltsie J, Liu J, Gorski JN, Chung CC, Gibson JT, Lisnock J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ.

ACS Med Chem Lett. 2014 Sep 8;5(10):1082-7. doi: 10.1021/ml5003426. eCollection 2014 Oct 9.

13.

Profound methyl effects in drug discovery and a call for new C-H methylation reactions.

Schönherr H, Cernak T.

Angew Chem Int Ed Engl. 2013 Nov 18;52(47):12256-67. doi: 10.1002/anie.201303207. Epub 2013 Oct 22. Review.

PMID:
24151256
14.
15.

Stable 5-substituted cyclopentadienes for the Diels-Alder cycloaddition and their application to the synthesis of palau'amine.

Hudon J, Cernak TA, Ashenhurst JA, Gleason JL.

Angew Chem Int Ed Engl. 2008;47(46):8885-8. doi: 10.1002/anie.200803344. No abstract available.

PMID:
18855951
16.

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