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Anthony J. Roecker, Ph.D. - Publications

Affiliations: 
Scripps Research Institute, La Jolla, La Jolla, CA, United States 
Area:
chemistry, biology, and medicine of natural and designed molecules
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32 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2020 VanHeyst MD, Qi J, Roecker AJ, Hughes JME, Cheng L, Zhao Z, Yin J. Continuous Flow-Enabled Synthesis of Bench-Stable Bicyclo[1.1.1]pentane Trifluoroborate Salts and Their Utilization in Metallaphotoredox Cross-Couplings. Organic Letters. PMID 31990565 DOI: 10.1021/Acs.Orglett.0C00242  0.342
2017 Skudlarek JW, DiMarco CN, Babaoglu K, Roecker AJ, Bruno JG, Pausch MA, O'Brien JA, Cabalu TD, Stevens J, Brunner J, Tannenbaum PL, Wuelfing WP, Garson SL, Fox SV, Savitz AT, et al. Investigation of orexin-2 selective receptor antagonists: Structural modifications resulting in dual orexin receptor antagonists. Bioorganic & Medicinal Chemistry Letters. PMID 28216403 DOI: 10.1016/J.Bmcl.2017.02.012  0.344
2016 Yin J, Babaoglu K, Brautigam CA, Clark L, Shao Z, Scheuermann TH, Harrell CM, Gotter AL, Roecker AJ, Winrow CJ, Renger JJ, Coleman PJ, Rosenbaum DM. Structure and ligand-binding mechanism of the human OX1 and OX2 orexin receptors. Nature Structural & Molecular Biology. PMID 26950369 DOI: 10.1038/Nsmb.3183  0.321
2015 Roecker AJ, Cox CD, Coleman PJ. Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia. Journal of Medicinal Chemistry. PMID 26317591 DOI: 10.1021/Acs.Jmedchem.5B00832  0.316
2015 Roecker AJ, Mercer SP, Bergman JM, Gilbert KF, Kuduk SD, Harrell CM, Garson SL, Fox SV, Gotter AL, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Lemaire W, Winrow CJ, et al. Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements. Bioorganic & Medicinal Chemistry Letters. PMID 25613676 DOI: 10.1016/J.Bmcl.2014.12.081  0.361
2014 Roecker AJ, Reger TS, Mattern MC, Mercer SP, Bergman JM, Schreier JD, Cube RV, Cox CD, Li D, Lemaire W, Bruno JG, Harrell CM, Garson SL, Gotter AL, Fox SV, et al. Discovery of MK-3697: a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia. Bioorganic & Medicinal Chemistry Letters. 24: 4884-90. PMID 25248679 DOI: 10.1016/J.Bmcl.2014.08.041  0.355
2014 Roecker AJ, Mercer SP, Harrell CM, Garson SL, Fox SV, Gotter AL, Prueksaritanont T, Cabalu TD, Cui D, Lemaire W, Winrow CJ, Renger JJ, Coleman PJ. Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis. Bioorganic & Medicinal Chemistry Letters. 24: 2079-85. PMID 24704030 DOI: 10.1016/J.Bmcl.2014.03.052  0.358
2014 Roecker AJ, Mercer SP, Schreier JD, Cox CD, Fraley ME, Steen JT, Lemaire W, Bruno JG, Harrell CM, Garson SL, Gotter AL, Fox SV, Stevens J, Tannenbaum PL, Prueksaritanont T, et al. Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia. Chemmedchem. 9: 311-22. PMID 24376006 DOI: 10.1002/Cmdc.201300447  0.358
2014 Roecker AJ, Mercer SP, Schreier JD, Cox CD, Fraley ME, Steen JT, Lemaire W, Bruno JG, Harrell CM, Garson SL, Gotter AL, Fox SV, Stevens J, Tannenbaum PL, Prueksaritanont T, et al. Cover Picture: Discovery of 5′′-Chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2′:5′,3′′-terpyridine-3′-carboxamide (MK-1064): A Selective Orexin 2 Receptor Antagonist (2-SORA) for the Treatment of Insomnia (ChemMedChem 2/2014) Chemmedchem. 9: 241-241. DOI: 10.1002/Cmdc.201490000  0.301
2013 Mercer SP, Roecker AJ, Garson S, Reiss DR, Meacham Harrell C, Murphy KL, Bruno JG, Bednar RA, Lemaire W, Cui D, Cabalu TD, Tang C, Prueksaritanont T, Hartman GD, Young SD, et al. Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs). Bioorganic & Medicinal Chemistry Letters. 23: 6620-4. PMID 24215892 DOI: 10.1016/J.Bmcl.2013.10.045  0.36
2012 Gotter AL, Roecker AJ, Hargreaves R, Coleman PJ, Winrow CJ, Renger JJ. Orexin receptors as therapeutic drug targets. Progress in Brain Research. 198: 163-88. PMID 22813974 DOI: 10.1016/B978-0-444-59489-1.00010-0  0.351
2011 Coleman PJ, Cox CD, Roecker AJ. Discovery of dual orexin receptor antagonists (DORAs) for the treatment of insomnia. Current Topics in Medicinal Chemistry. 11: 696-725. PMID 21261591 DOI: 10.2174/1568026611109060696  0.329
2010 Cox CD, Breslin MJ, Whitman DB, Schreier JD, McGaughey GB, Bogusky MJ, Roecker AJ, Mercer SP, Bednar RA, Lemaire W, Bruno JG, Reiss DR, Harrell CM, Murphy KL, Garson SL, et al. Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia. Journal of Medicinal Chemistry. 53: 5320-32. PMID 20565075 DOI: 10.1021/Jm100541C  0.37
2008 Roecker AJ, Coleman PJ. Orexin receptor antagonists: medicinal chemistry and therapeutic potential. Current Topics in Medicinal Chemistry. 8: 977-87. PMID 18673167 DOI: 10.2174/156802608784936746  0.302
2008 Bergman JM, Roecker AJ, Mercer SP, Bednar RA, Reiss DR, Ransom RW, Meacham Harrell C, Pettibone DJ, Lemaire W, Murphy KL, Li C, Prueksaritanont T, Winrow CJ, Renger JJ, Koblan KS, et al. Proline bis-amides as potent dual orexin receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 18: 1425-30. PMID 18207395 DOI: 10.1016/J.Bmcl.2008.01.001  0.387
2007 Roecker AJ, Coleman PJ, Mercer SP, Schreier JD, Buser CA, Walsh ES, Hamilton K, Lobell RB, Tao W, Diehl RE, South VJ, Davide JP, Kohl NE, Yan Y, Kuo LC, et al. Kinesin spindle protein (KSP) inhibitors. Part 8: Design and synthesis of 1,4-diaryl-4,5-dihydropyrazoles as potent inhibitors of the mitotic kinesin KSP. Bioorganic & Medicinal Chemistry Letters. 17: 5677-82. PMID 17766111 DOI: 10.1016/J.Bmcl.2007.07.074  0.351
2005 Nicolaou KC, Sasmal PK, Koftis TV, Converso A, Loizidou E, Kaiser F, Roecker AJ, Dellios CC, Sun XW, Petrovic G. Studies toward the synthesis of azadirachtin, part 2: construction of fully functionalized ABCD ring frameworks and unusual intramolecular reactions induced by close-proximity effects. Angewandte Chemie (International Ed. in English). 44: 3447-52. PMID 15849805 DOI: 10.1002/Anie.200500217  0.73
2005 Nicolaou KC, Sasmal PK, Roecker AJ, Sun XW, Mandal S, Converso A. Studies toward the synthesis of azadirachtin, part 1: total synthesis of a fully functionalized ABC ring framework and coupling with a norbornene domain. Angewandte Chemie (International Ed. in English). 44: 3443-7. PMID 15846829 DOI: 10.1002/Anie.200500216  0.728
2005 Tan C, de Noronha RG, Roecker AJ, Pyrzynska B, Khwaja F, Zhang Z, Zhang H, Teng Q, Nicholson AC, Giannakakou P, Zhou W, Olson JJ, Pereira MM, Nicolaou KC, Van Meir EG. Identification of a novel small-molecule inhibitor of the hypoxia-inducible factor 1 pathway. Cancer Research. 65: 605-12. PMID 15695405  0.341
2003 Nicolaou KC, Evans RM, Roecker AJ, Hughes R, Downes M, Pfefferkorn JA. Discovery and optimization of non-steroidal FXR agonists from natural product-like libraries. Organic & Biomolecular Chemistry. 1: 908-20. PMID 12929628 DOI: 10.1039/B300525A  0.747
2003 Nicolaou KC, Roecker AJ, Monenschein H, Guntupalli P, Follmann M. Studies towards the synthesis of azadirachtin: enantioselective entry into the azadirachtin framework through cascade reactions. Angewandte Chemie (International Ed. in English). 42: 3637-42. PMID 12916035 DOI: 10.1002/Anie.200351744  0.485
2003 Downes M, Verdecia MA, Roecker AJ, Hughes R, Hogenesch JB, Kast-Woelbern HR, Bowman ME, Ferrer JL, Anisfeld AM, Edwards PA, Rosenfeld JM, Alvarez JG, Noel JP, Nicolaou KC, Evans RM. A chemical, genetic, and structural analysis of the nuclear bile acid receptor FXR. Molecular Cell. 11: 1079-92. PMID 12718892 DOI: 10.1016/S1097-2765(03)00104-7  0.613
2003 Nicolaou KC, Roecker AJ, Hughes R, van Summeren R, Pfefferkorn JA, Winssinger N. Novel strategies for the solid phase synthesis of substituted indolines and indoles. Bioorganic & Medicinal Chemistry. 11: 465-76. PMID 12517442 DOI: 10.1016/S0968-0896(02)00386-3  0.757
2002 Nicolaou KC, Roecker AJ, Follmann M, Baati R. Model studies towards azadirachtin: part 2. Construction of the crowded C8-C14 bond by transition metal chemistry. Angewandte Chemie (International Ed. in English). 41: 2107-10. PMID 19746611 DOI: 10.1002/1521-3773(20020617)41:12<2107::Aid-Anie2107>3.0.Co;2-4  0.358
2002 Nicolaou KC, Follmann M, Roecker AJ, Hunt KW. Model studies towards azadirachtin: part 1. Construction of the crowded C8-C14 bond by radical chemistry. Angewandte Chemie (International Ed. in English). 41: 2103-6. PMID 19746610 DOI: 10.1002/1521-3773(20020617)41:12<2103::Aid-Anie2103>3.0.Co;2-S  0.39
2001 Nicolaou KC, Roecker AJ, Barluenga S, Pfefferkorn JA, Cao GQ. Discovery of novel antibacterial agents active against methicillin-resistant Staphylococcus aureus from combinatorial benzopyran libraries. Chembiochem : a European Journal of Chemical Biology. 2: 460-5. PMID 11828478 DOI: 10.1002/1439-7633(20010601)2:6<460::Aid-Cbic460>3.0.Co;2-2  0.715
2001 Nicolaou KC, Hughes R, Pfefferkorn JA, Barluenga S, Roecker AJ. Combinatorial synthesis through disulfide exchange: discovery of potent psammaplin A type antibacterial agents active against methicillin-resistant Staphylococcus aureus (MRSA). Chemistry (Weinheim An Der Bergstrasse, Germany). 7: 4280-95. PMID 11686609 DOI: 10.1002/1521-3765(20011001)7:19<4280::Aid-Chem4280>3.0.Co;2-3  0.753
2000 Nicolaou KC, Pfefferkorn JA, Schuler F, Roecker AJ, Cao GQ, Casida JE. Combinatorial synthesis of novel and potent inhibitors of NADH:ubiquinone oxidoreductase Chemistry and Biology. 7: 979-992. PMID 11137820 DOI: 10.1016/S1074-5521(00)00047-8  0.654
2000 Nicolaou KC, Roecker AJ, Pfefferkorn JA, Cao GQ. A novel strategy for the solid-phase synthesis of substituted indolines [12] Journal of the American Chemical Society. 122: 2966-2967. DOI: 10.1021/Ja994373F  0.691
2000 Nicolaou KC, Pfefferkorn JA, Barluenga S, Mitchell HJ, Roecker AJ, Cao GQ. Natural product-like combinatorial libraries based on privileged structures. 3. The 'libraries from libraries' principle for diversity enhancement of benzopyran libraries Journal of the American Chemical Society. 122: 9968-9976. DOI: 10.1021/Ja0020355  0.759
2000 Nicolaou KC, Pfefferkorn JA, Mitchell HJ, Roecker AJ, Barluenga S, Cao GQ, Affleck RL, Lillig JE. Natural product-like combinatorial libraries based on privileged structures. 2. Construction of a 10 000-membered benzopyran library by directed split-and-pool chemistry using NanoKans and optical encoding Journal of the American Chemical Society. 122: 9954-9967. DOI: 10.1021/Ja002034C  0.763
2000 Nicolaou KC, Pfefferkorn JA, Roecker AJ, Cao GQ, Barluenga S, Mitchell HJ. Natural product-like combinatorial libraries based on privileged structures. 1. General principles and solid-phase synthesis of benzopyrans Journal of the American Chemical Society. 122: 9939-9953. DOI: 10.1021/Ja002033K  0.758
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