Search Results - "Shaghafi, Michael"

Oxazolidine Synthesis by Complementary Stereospecific and Stereoconvergent Methods by Shaghafi, Michael B, Grote, Robin E, Jarvo, Elizabeth R

“…Complementary stereospecific and stereoconvergent reactions for enantioselective synthesis of 1,3-oxazolidines are reported. In the presence of a rhodium…”
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Structure-based Design of Pyridone–Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition by Reich, Siegfried H, Sprengeler, Paul A, Chiang, Gary G, Appleman, James R, Chen, Joan, Clarine, Jeff, Eam, Boreth, Ernst, Justin T, Han, Qing, Goel, Vikas K, Han, Edward Z. R, Huang, Vera, Hung, Ivy N. J, Jemison, Adrianna, Jessen, Katti A, Molter, Jolene, Murphy, Douglas, Neal, Melissa, Parker, Gregory S, Shaghafi, Michael, Sperry, Samuel, Staunton, Jocelyn, Stumpf, Craig R, Thompson, Peggy A, Tran, Chinh, Webber, Stephen E, Wegerski, Christopher J, Zheng, Hong, Webster, Kevin R

“…Dysregulated translation of mRNA plays a major role in tumorigenesis. Mitogen-activated protein kinase interacting kinases (MNK)­1/2 are key regulators of mRNA…”
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Constructing Saturated Guanidinum Heterocycles by Cycloaddition of N‑Amidinyliminium Ions with Indoles by Allred, Tyler K, Shaghafi, Michael B, Chen, Pan-Pan, Tran, Quan, Houk, K. N, Overman, Larry E

“…We report that structurally complex guanidinium heterocycles can be prepared in one step by regio- and stereoselective [4 + 2]-cycloadditions of…”
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The insulin secretory action of novel polycyclic guanidines: discovery through open innovation phenotypic screening, and exploration of structure-activity relationships by Shaghafi, Michael B, Barrett, David G, Willard, Francis S, Overman, Larry E

“…We report the discovery of the glucose-dependent insulin secretogogue activity of a novel class of polycyclic guanidines through phenotypic screening as part…”
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Palladium-Catalyzed Conjugate Allylation Reactions of α,β-Unsaturated N-Acylpyrroles by Shaghafi, Michael B, Kohn, Benjamin L, Jarvo, Elizabeth R

“…Conjugate allylation reactions of α,β-unsaturated N-acylpyrroles using allylboronic ester are catalyzed by a palladium complex that is ligated by a bidentate…”
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Quinolones as HCV NS5B polymerase inhibitors by Kumar, Dange V., Rai, Roopa, Brameld, Ken A., Somoza, John R., Rajagopalan, Ravi, Janc, James W., Xia, Yu M., Ton, Tony L., Shaghafi, Michael B., Hu, Huiyong, Lehoux, Isabelle, To, Nhat, Young, Wendy B., Green, Michael J.

“…Hepatitis C virus (HCV) infection is treated with a combination of peginterferon alfa-2a/b and ribavirin. To address the limitations of this therapy, numerous…”
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Abstract 5333: Combining chemoproteomics with machine learning identifies functionally active covalent fragments for hard-to-drug cancer drivers by Hermann, Johannes C., Everley, Robert, Marholz, Laura, Berberich, Matthew, Yang, Tzu-Yi, Chao, Yu-Hsin, Awol, Abduselam K., Shaghafi, Michael, Yoon, Han, Varma, Rohan, Stein, Reed, Krug, Karsten, Lachtara, Emily, Erlanson, Daniel, Varma, Chris, Webster, Kevin R.

“…Abstract a) Many cancer drivers are considered “undruggable” and without targeted treatments because they lack binding sites for conventional small molecules…”
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Palladium and Nickel-Catalyzed Transformations Accessing Electron-Rich Allylmetal Intermediates by Shaghafi, Michael B

“…The investigation of pre-formed NHC-ligated allylpalladium complexes and their use as efficient catalysts in the context of a conjugate allylation of…”
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Discovery of novel hydroxy pyrazole based factor IXa inhibitor by Vijaykumar, Dange, Sprengeler, Paul A., Shaghafi, Michael, Spencer, Jeffrey R., Katz, Brad A., Yu, Christine, Rai, Roopa, Young, Wendy B., Schultz, Brian, Janc, James

“…Replacement of central phenol in 1 with hydroxy pyrazole resulted in compound 2 which selectively inhibits factor IXa. It is also selective against…”
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Efforts toward oral bioavailability in factor VIIa inhibitors by Vijaykumar, Dange, Rai, Roopa, Shaghafi, Michael, Ton, Tony, Torkelson, Steve, Leahy, Ellen M., Riggs, Jennifer R., Hu, Huiyong, Sprengeler, Paul A., Shrader, William D., O’Bryan, Colin, Cabuslay, Ronnell, Sanford, Ellen, Gjerstadt, Erik, Liu, Liang, Sukbuntherng, Juthamas, Young, Wendy B.

“…Efforts toward developing orally bioavailable factor VIIa inhibitors starting from parenteral lead compound 1 are described. SAR resulted in compound 11 with…”
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Palladium and Nickel-Catalyzed Transformations Accessing Electron-Rich Allylmetal Intermediates by Shaghafi, Michael B

“…The investigation of pre-formed NHC-ligated allylpalladium complexes and their use as efficient catalysts in the context of a conjugate allylation of…”
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