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Items: 24

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.

Profiling and Application of Photoredox C(sp3)-C(sp2) Cross-Coupling in Medicinal Chemistry.

Zhang R, Li G, Wismer M, Vachal P, Colletti SL, Shi ZC.

ACS Med Chem Lett. 2018 May 7;9(7):773-777. doi: 10.1021/acsmedchemlett.8b00183. eCollection 2018 Jul 12.

4.

Chemoselective Peptide Modification via Photocatalytic Tryptophan β-Position Conjugation.

Yu Y, Zhang LK, Buevich AV, Li G, Tang H, Vachal P, Colletti SL, Shi ZC.

J Am Chem Soc. 2018 Jun 6;140(22):6797-6800. doi: 10.1021/jacs.8b03973. Epub 2018 May 23.

PMID:
29762027
5.

A General Small-Scale Reactor To Enable Standardization and Acceleration of Photocatalytic Reactions.

Le CC, Wismer MK, Shi ZC, Zhang R, Conway DV, Li G, Vachal P, Davies IW, MacMillan DWC.

ACS Cent Sci. 2017 Jun 28;3(6):647-653. doi: 10.1021/acscentsci.7b00159. Epub 2017 May 17.

6.

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
7.

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
8.

Synthesis of Complex Druglike Molecules by the Use of Highly Functionalized Bench-Stable Organozinc Reagents.

Greshock TJ, Moore KP, McClain RT, Bellomo A, Chung CK, Dreher SD, Kutchukian PS, Peng Z, Davies IW, Vachal P, Ellwart M, Manolikakes SM, Knochel P, Nantermet PG.

Angew Chem Int Ed Engl. 2016 Oct 24;55(44):13714-13718. doi: 10.1002/anie.201604652. Epub 2016 Sep 30.

PMID:
27690172
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.

Discovery of Novel Indoline Cholesterol Ester Transfer Protein Inhibitors (CETP) through a Structure-Guided Approach.

Wilson JE, Kurukulasuriya R, Reibarkh M, Reiter M, Zwicker A, Zhao K, Zhang F, Anand R, Colandrea VJ, Cumiskey AM, Crespo A, Duffy RA, Murphy BA, Mitra K, Johns DG, Duffy JL, Vachal P.

ACS Med Chem Lett. 2016 Jan 4;7(3):261-5. doi: 10.1021/acsmedchemlett.5b00404. eCollection 2016 Mar 10.

11.

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
12.

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.

13.

Effects of anacetrapib on plasma lipids, apolipoproteins and PCSK9 in healthy, lean rhesus macaques.

Roddy TP, McLaren DG, Chen Y, Xie D, Dunn K, Kulick A, Szeto D, Forrest G, Albanese K, Donnelly M, Gai C, Gewain A, Lederman H, Jensen KK, Ai X, Vachal P, Akinsanya KO, Cleary MA, Previs SF, Dansky HM, Johns DG.

Eur J Pharmacol. 2014 Oct 5;740:410-6. doi: 10.1016/j.ejphar.2014.04.015. Epub 2014 Apr 21.

PMID:
24769414
14.

Late-stage functionalization of biologically active heterocycles through photoredox catalysis.

Dirocco DA, Dykstra K, Krska S, Vachal P, Conway DV, Tudge M.

Angew Chem Int Ed Engl. 2014 May 5;53(19):4802-6. doi: 10.1002/anie.201402023. Epub 2014 Mar 26.

PMID:
24677697
15.

1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.

Vachal P, Miao S, Pierce JM, Guiadeen D, Colandrea VJ, Wyvratt MJ, Salowe SP, Sonatore LM, Milligan JA, Hajdu R, Gollapudi A, Keohane CA, Lingham RB, Mandala SM, DeMartino JA, Tong X, Wolff M, Steinhuebel D, Kieczykowski GR, Fleitz FJ, Chapman K, Athanasopoulos J, Adam G, Akyuz CD, Jena DK, Lusen JW, Meng J, Stein BD, Xia L, Sherer EC, Hale JJ.

J Med Chem. 2012 Apr 12;55(7):2945-59. doi: 10.1021/jm201542d. Epub 2012 Feb 27.

PMID:
22364528
16.

High-throughput purification platform in support of drug discovery.

Liu M, Chen K, Christian D, Fatima T, Pissarnitski N, Streckfuss E, Zhang C, Xia L, Borges S, Shi Z, Vachal P, Tata J, Athanasopoulos J.

ACS Comb Sci. 2012 Jan 9;14(1):51-9. doi: 10.1021/co200138h. Epub 2011 Nov 2.

PMID:
22032344
17.

Fluorescence properties and dipole moments of novel fused thienobenzofurans. Solvent and structural effects.

Aaron JJ, Párkányi C, Adenier A, Potin C, Zajíčková Z, Martínez OR, Svoboda J, Pihera P, Váchal P.

J Fluoresc. 2011 Nov;21(6):2133-41. doi: 10.1007/s10895-011-0914-3. Epub 2011 Jul 13.

PMID:
21750892
18.

1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity.

Vachal P, Fletcher JM, Fong TM, Huang CC, Lao J, Xiao JC, Shen CP, Strack AM, Shearman L, Stribling S, Chen RZ, Frassetto A, Tong X, Wang J, Ball RG, Tsou NN, Hickey GJ, Thompson DF, Faidley TD, Nicolich S, Achanfuo-Yeboah J, Hora DF, Hale JJ, Hagmann WK.

J Med Chem. 2009 Apr 23;52(8):2550-8. doi: 10.1021/jm900063x.

PMID:
19320488
19.

Synthesis and study of alendronate derivatives as potential prodrugs of alendronate sodium for the treatment of low bone density and osteoporosis.

Vachal P, Hale JJ, Lu Z, Streckfuss EC, Mills SG, MacCoss M, Yin DH, Algayer K, Manser K, Kesisoglou F, Ghosh S, Alani LL.

J Med Chem. 2006 Jun 1;49(11):3060-3.

PMID:
16722624
20.

Highly selective and potent agonists of sphingosine-1-phosphate 1 (S1P1) receptor.

Vachal P, Toth LM, Hale JJ, Yan L, Mills SG, Chrebet GL, Koehane CA, Hajdu R, Milligan JA, Rosenbach MJ, Mandala S.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3684-7. Epub 2006 May 6.

PMID:
16682185
21.

Topological nonconnectivity threshold in long-range spin systems.

Borgonovi F, Celardo GL, Musesti A, Trasarti-Battistoni R, Vachal P.

Phys Rev E Stat Nonlin Soft Matter Phys. 2006 Feb;73(2 Pt 2):026116. Epub 2006 Feb 16. Erratum in: Phys Rev E Stat Nonlin Soft Matter Phys. 2006 Mar;73(3 Pt 2):039903.

PMID:
16605407
22.
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