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Items: 1 to 20 of 149

1.

Syntheses of PDE3A inhibitor ORG9935 and determination of the absolute stereochemistries of its enantiomers by X-ray crystallography.

Jakkaraj S, Young VG Jr, Georg GI.

Tetrahedron. 2018 May 31;74(22):2769-2774. doi: 10.1016/j.tet.2018.04.045. Epub 2018 Apr 18.

PMID:
30416214
2.

Allosteric Modulators of Drug Targets Special Issue.

Haskell-Luevano C, Georg GI, Wang S, Meanwell N.

J Med Chem. 2018 Feb 22;61(4):1381. doi: 10.1021/acs.jmedchem.8b00171. Epub 2018 Feb 7. No abstract available.

PMID:
29412672
3.

Design, Synthesis, and in Vitro and in Vivo Evaluation of Ouabain Analogues as Potent and Selective Na,K-ATPase α4 Isoform Inhibitors for Male Contraception.

Syeda SS, Sánchez G, Hong KH, Hawkinson JE, Georg GI, Blanco G.

J Med Chem. 2018 Mar 8;61(5):1800-1820. doi: 10.1021/acs.jmedchem.7b00925. Epub 2018 Jan 19.

4.

Structural Basis of ALDH1A2 Inhibition by Irreversible and Reversible Small Molecule Inhibitors.

Chen Y, Zhu JY, Hong KH, Mikles DC, Georg GI, Goldstein AS, Amory JK, Schönbrunn E.

ACS Chem Biol. 2018 Mar 16;13(3):582-590. doi: 10.1021/acschembio.7b00685. Epub 2018 Jan 3.

5.

Synthesis and evaluation of C2 functionalized analogs of the α-tubulin-binding natural product pironetin.

Huang DS, Wong HL, Georg GI.

Bioorg Med Chem Lett. 2018 Sep 1;28(16):2789-2793. doi: 10.1016/j.bmcl.2017.10.057. Epub 2017 Nov 11.

PMID:
29138028
6.

Heme Binding Biguanides Target Cytochrome P450-Dependent Cancer Cell Mitochondria.

Guo Z, Sevrioukova IF, Denisov IG, Zhang X, Chiu TL, Thomas DG, Hanse EA, Cuellar RAD, Grinkova YV, Langenfeld VW, Swedien DS, Stamschror JD, Alvarez J, Luna F, Galván A, Bae YK, Wulfkuhle JD, Gallagher RI, Petricoin EF Rd, Norris B, Flory CM, Schumacher RJ, O'Sullivan MG, Cao Q, Chu H, Lipscomb JD, Atkins WM, Gupta K, Kelekar A, Blair IA, Capdevila JH, Falck JR, Sligar SG, Poulos TL, Georg GI, Ambrose E, Potter DA.

Cell Chem Biol. 2017 Oct 19;24(10):1314. doi: 10.1016/j.chembiol.2017.09.012. No abstract available.

7.

Structure-Activity Studies of N-Butyl-1-deoxynojirimycin (NB-DNJ) Analogues: Discovery of Potent and Selective Aminocyclopentitol Inhibitors of GBA1 and GBA2.

Gu X, Gupta V, Yang Y, Zhu JY, Carlson EJ, Kingsley C, Tash JS, Schönbrunn E, Hawkinson J, Georg GI.

ChemMedChem. 2017 Dec 7;12(23):1977-1984. doi: 10.1002/cmdc.201700558. Epub 2017 Nov 24.

8.

Potent Pyrimidine and Pyrrolopyrimidine Inhibitors of Testis-Specific Serine/Threonine Kinase 2 (TSSK2).

Hawkinson JE, Sinville R, Mudaliar D, Shetty J, Ward T, Herr JC, Georg GI.

ChemMedChem. 2017 Nov 22;12(22):1857-1865. doi: 10.1002/cmdc.201700503. Epub 2017 Oct 20.

PMID:
28952188
9.

Heme Binding Biguanides Target Cytochrome P450-Dependent Cancer Cell Mitochondria.

Guo Z, Sevrioukova IF, Denisov IG, Zhang X, Chiu TL, Thomas DG, Hanse EA, Cuellar RAD, Grinkova YV, Langenfeld VW, Swedien DS, Stamschror JD, Alvarez J, Luna F, Galván A, Bae YK, Wulfkuhle JD, Gallagher RI, Petricoin EF Rd, Norris B, Flory CM, Schumacher RJ, O'Sullivan MG, Cao Q, Chu H, Lipscomb JD, Atkins WM, Gupta K, Kelekar A, Blair IA, Capdevila JH, Falck JR, Sligar SG, Poulos TL, Georg GI, Ambrose E, Potter DA.

Cell Chem Biol. 2017 Oct 19;24(10):1259-1275.e6. doi: 10.1016/j.chembiol.2017.08.009. Epub 2017 Sep 14.

10.

Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors.

Zhu JY, Cuellar RA, Berndt N, Lee HE, Olesen SH, Martin MP, Jensen JT, Georg GI, Schönbrunn E.

J Med Chem. 2017 Sep 28;60(18):7863-7875. doi: 10.1021/acs.jmedchem.7b00996. Epub 2017 Sep 14.

11.

Correction to BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.

Ayoub AM, Hawk LML, Herzig RJ, Jiang J, Wisniewski AJ, Gee CT, Zhao P, Zhu JY, Berndt N, Offei-Addo NK, Scott TG, Qi J, Bradner JE, Ward TR, Schönbrunn E, Georg GI, Pomerantz WCK.

J Med Chem. 2017 Jul 27;60(14):6458. doi: 10.1021/acs.jmedchem.7b00943. Epub 2017 Jul 11. No abstract available.

PMID:
28696689
12.

BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.

Ayoub AM, Hawk LML, Herzig RJ, Jiang J, Wisniewski AJ, Gee CT, Zhao P, Zhu JY, Berndt N, Offei-Addo NK, Scott TG, Qi J, Bradner JE, Ward TR, Schönbrunn E, Georg GI, Pomerantz WCK.

J Med Chem. 2017 Jun 22;60(12):4805-4817. doi: 10.1021/acs.jmedchem.6b01336. Epub 2017 Jun 7.

13.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

ACS Med Chem Lett. 2017 Feb 28;8(4):379-382. doi: 10.1021/acsmedchemlett.7b00056. eCollection 2017 Apr 13. No abstract available.

14.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

ACS Cent Sci. 2017 Mar 22;3(3):143-147. doi: 10.1021/acscentsci.7b00069. Epub 2017 Feb 28. No abstract available.

15.

Current Medicinal Chemistry Research in India: Progress and Opportunities.

Georg GI, Wang S.

J Med Chem. 2017 Mar 9;60(5):1619. doi: 10.1021/acs.jmedchem.7b00317. No abstract available.

PMID:
28274124
16.

Synthesis and Cytotoxicity Evaluation of C4- and C5-Modified Analogues of the α,β-Unsaturated Lactone of Pironetin.

Huang DS, Wong HL, Georg GI.

ChemMedChem. 2017 Apr 6;12(7):520-528. doi: 10.1002/cmdc.201700084. Epub 2017 Mar 22.

17.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

J Med Chem. 2017 Mar 23;60(6):2165-2168. doi: 10.1021/acs.jmedchem.7b00229. Epub 2017 Feb 28. No abstract available.

PMID:
28244745
18.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

J Chem Inf Model. 2017 Mar 27;57(3):387-390. doi: 10.1021/acs.jcim.7b00105. Epub 2017 Feb 28. No abstract available.

PMID:
28244743
19.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

Biochemistry. 2017 Mar 14;56(10):1363-1366. doi: 10.1021/acs.biochem.7b00110. Epub 2017 Feb 28. No abstract available.

PMID:
28244742
20.

The Ecstasy and Agony of Assay Interference Compounds.

Aldrich C, Bertozzi C, Georg GI, Kiessling L, Lindsley C, Liotta D, Merz KM Jr, Schepartz A, Wang S.

ACS Chem Neurosci. 2017 Mar 15;8(3):420-423. doi: 10.1021/acschemneuro.7b00064. Epub 2017 Feb 28. No abstract available.

PMID:
28244737

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