Search Results - "SHOWALTER, H. D. H"

Progress in the Synthesis of Canthine Alkaloids and Ring-Truncated Congeners by Showalter, H. D. Hollis

“…The canthines represent a fairly large subclass of β-carboline alkaloids, with the first members described 75 years ago. Over the last 60 years, many members…”
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Quaternary Diamines as Mass Spectrometry Cleavable Crosslinkers for Protein Interactions by Clifford-Nunn, Billy, Showalter, H. D. Hollis, Andrews, Philip C.

“…Mapping protein interactions and their dynamics is crucial to defining physiologic states, building effective models for understanding cell function, and to…”
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Rifamycins – Obstacles and opportunities by Aristoff, Paul A, Garcia, George A, Kirchhoff, Paul D, Hollis Showalter, H.D

“…Summary With nearly one-third of the global population infected by Mycobacterium tuberculosis , TB remains a major cause of death (1.7 million in 2006). TB is…”
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X‑ray Crystal Structures of the Escherichia coli RNA Polymerase in Complex with Benzoxazinorifamycins by Molodtsov, Vadim, Nawarathne, Irosha N, Scharf, Nathan T, Kirchhoff, Paul D, Showalter, H. D. Hollis, Garcia, George A, Murakami, Katsuhiko S

“…Rifampin, a semisynthetic rifamycin, is the cornerstone of current tuberculosis treatment. Among many semisynthetic rifamycins, benzoxazinorifamycins have…”
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Design, synthesis and prostate cancer cell-based studies of analogs of the Rho/MKL1 transcriptional pathway inhibitor, CCG-1423 by Evelyn, Chris R., Bell, Jessica L., Ryu, Jenny G., Wade, Susan M., Kocab, Andrew, Harzdorf, Nicole L., Hollis Showalter, H.D., Neubig, Richard R., Larsen, Scott D.

“…Conformational restriction and bioisosteric amide replacement were used to generate novel analogs of the Rho-transcriptional pathway inhibitor CCG-1423. Two…”
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Protein cross-linking as a novel mechanism of action of a ubiquitin-activating enzyme inhibitor with anti-tumor activity by Kapuria, Vaibhav, Peterson, Luke F., Showalter, H.D. Hollis, Kirchhoff, Paul D., Talpaz, Moshe, Donato, Nicholas J.

“…Ubiquitin-activating enzyme 1 (UBE1) is a critical regulator of the ubiquitination cycle and its targeted inhibition may be an appropriate therapeutic strategy…”
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Stereoselective Synthesis of (S)-3-(Methylamino)-3-((R)-pyrrolidin-3-yl)propanenitrile by Lall, Manjinder S, Hoge, Garrett, Tran, Tuan P, Kissel, William, Murphy, Sean T, Taylor, Clarke, Hutchings, Kim, Samas, Brian, Ellsworth, Edmund L, Curran, Timothy, Showalter, H. D. Hollis

“…(S)-3-(Methylamino)-3-((R)-pyrrolidin-3-yl)­propanenitrile (1) is a key intermediate in the preparation of PF-00951966, a fluoroquinolone antibiotic for use…”
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Investigation of 3-aryl-pyrimido[5,4-e][1,2,4]triazine-5,7-diones as small molecule antagonists of β-catenin/TCF transcription by Zeller, Jörg, Turbiak, Anjanette J., Powelson, Ian A., Lee, Surin, Sun, Duxin, Showalter, H.D. Hollis, Fearon, Eric R.

“…Nearly all colorectal cancers (CRCs) and varied subsets of other cancers have somatic mutations leading to β-catenin stabilization and increased β-catenin/TCF…”
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Synthesis and structure–activity relationships of 2-amino-3-carboxy-4-phenylthiophenes as novel atypical protein kinase C inhibitors by Titchenell, Paul M., Hollis Showalter, H.D., Pons, Jean-François, Barber, Alistair J., Jin, Yafei, Antonetti, David A.

“…Recent evidence suggests atypical protein kinase C (aPKC) isoforms are required for both TNF- and VEGF-induced breakdown of the blood–retinal barrier (BRB) and…”
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Enediol mimics as inhibitors of the d-arabinose 5-phosphate isomerase (KdsD) from Francisella tularensis by Yep, Alejandra, Sorenson, Roderick J., Wilson, Michael R., Hollis Showalter, H.D., Larsen, Scott D., Keller, Paul R., Woodard, Ronald W.

“…We explored the d-arabinose 5-phosphate isomerase (KdsD, E.C. 5.3.1.13) from Francisella tularensis, a highly infectious Gram-negative pathogen that has raised…”
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3-Aminoquinazolinediones as a New Class of Antibacterial Agents Demonstrating Excellent Antibacterial Activity Against Wild-Type and Multidrug Resistant Organisms by Ellsworth, Edmund L, Tran, Tuan P, Hollis Showalter, H. D, Sanchez, Joseph P, Watson, Brian M, Stier, Michael A, Domagala, John M, Gracheck, Stephen J, Joannides, E. Themis, Shapiro, Martin A, Dunham, Steve A, Hanna, Debra L, Huband, Michael D, Gage, Jeffrey W, Bronstein, Joel C, Liu, Jia Yeu, Nguyen, Dai Q, Singh, Rajeshwar

“…The 3-aminoquinzolinediones represent a new series of antibacterial agents structurally related to the fluoroquinolones. They are inhibitors of bacterial…”
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A novel synthesis of 3-(substituted)pyrimido[4,5- c]pyridazine-5,7(1 H,6 H)-diones by Turbiak, Anjanette J., Kampf, Jeff W., Hollis Showalter, H.D.

“…An improved synthesis of 3-(substituted)pyrimido[4,5- c]pyridazine-5,7(1 H,6 H)-diones, a known subclass of 4-deazatoxoflavins, is reported. The approach…”
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Tyrosine Kinase Inhibitors. 17. Irreversible Inhibitors of the Epidermal Growth Factor Receptor:  4-(Phenylamino)quinazoline- and 4-(Phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides Bearing Additional Solubilizing Functions by Smaill, Jeff B, Rewcastle, Gordon W, Loo, Joseph A, Greis, Kenneth D, Chan, O. Helen, Reyner, Eric L, Lipka, Elke, Showalter, H. D. Hollis, Vincent, Patrick W, Elliott, William L, Denny, William A

“…4-Anilinoquinazoline- and 4-anilinopyrido[3,2-d]pyrimidine-6-acrylamides substituted with solubilizing 7-alkylamine or 7-alkoxyamine side chains were prepared…”
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Property-based design of a glucosylceramide synthase inhibitor that reduces glucosylceramide in the brain by Larsen, Scott D., Wilson, Michael W., Abe, Akira, Shu, Liming, George, Christopher H., Kirchhoff, Paul, Showalter, H. D. Hollis, Xiang, Jianming, Keep, Richard F., Shayman, James A.

“…Synthesis inhibition is the basis for the treatment of type 1 Gaucher disease by the glucosylceramide synthase (GCS) inhibitor eliglustat tartrate. However,…”
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Synthesis and structure–activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin by Jin, Yafei, Gill, Sumandeep K., Kirchhoff, Paul D., Wan, Baojie, Franzblau, Scott G., Garcia, George A., Showalter, H.D. Hollis

“…A series of rifamycin S and rifampin analogues incorporating substituted 8-amino, 8-thio, and 1,8-pyrazole substituents has been synthesized. The compounds…”
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Synthesis and Structure−Activity Relationships of Soluble 7-Substituted 3-(3,5-Dimethoxyphenyl)-1,6-naphthyridin-2-amines and Related Ureas as Dual Inhibitors of the Fibroblast Growth Factor Receptor-1 and Vascular Endothelial Growth Factor Receptor-2 Tyrosine Kinases by Thompson, Andrew M, Delaney, Amy M, Hamby, James M, Schroeder, Mel C, Spoon, Teresa A, Crean, Sheila M, Showalter, H. D. Hollis, Denny, William A

“…7-Substituted 3-aryl-1,6-naphthyridine-2,7-diamines and related 2-ureas are inhibitors of fibroblast growth factor receptor-1 (FGFR-1) and vascular endothelial…”
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Tyrosine Kinase Inhibitors. 18. 6-Substituted 4-Anilinoquinazolines and 4-Anilinopyrido[3,4-d]pyrimidines as Soluble, Irreversible Inhibitors of the Epidermal Growth Factor Receptor by Smaill, Jeff B, Showalter, H. D. Hollis, Zhou, Hairong, Bridges, Alexander J, McNamara, Dennis J, Fry, David W, Nelson, James M, Sherwood, Veronika, Vincent, Patrick W, Roberts, Bill J, Elliott, William L, Denny, William A

“…4-Anilinoquinazoline- and 4-anilinopyrido[3,4-d]pyrimidine-6-acrylamides are potent pan-erbB tyrosine kinase inactivators, and one example (CI-1033) is in…”
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Synthesis and antibacterial activity of the C-7 side chain of 3-aminoquinazolinediones by Hutchings, Kim M., Tran, Tuan P., Ellsworth, Edmund L., Watson, Brian M., Sanchez, Joseph P., Hollis Showalter, H.D., Stier, Michael A., Shapiro, Martin, Themis Joannides, E., Huband, Michael, Nguyen, Dai Q., Maiti, Samarendra, Li, Tingsheng, Tailor, Jyoti, Thomas, George, Ha, Chan, Singh, Rajeshwar

“…The synthesis and structure–activity relationship of a novel series of bacterial topoisomerase (3-aminoquinazolinediones) inhibitors is described. A novel…”
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Synthesis and structural–activity relationships of 3-hydroxyquinazoline-2,4-dione antibacterial agents by Tran, Tuan P., Ellsworth, Edmund L., Stier, Michael A., Domagala, John M., Hollis Showalter, H.D., Gracheck, Stephen J., Shapiro, Martin A., Joannides, Themis E., Singh, Rajeshwar

“…The synthesis and SAR of the 3-hydroxyquinazoline diones, a novel class of bacterial topoisomerase inhibitors, is reported. A series of…”
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3‑Substituted‑N‑(4-Hydroxynaphthalen-1-yl)arylsulfonamides as a Novel Class of Selective Mcl‑1 Inhibitors: Structure-Based Design, Synthesis, SAR, and Biological Evaluation by Abulwerdi, Fardokht A, Liao, Chenzhong, Mady, Ahmed S, Gavin, Jordan, Shen, Chenxi, Cierpicki, Tomasz, Stuckey, Jeanne A, Showalter, H. D. Hollis, Nikolovska-Coleska, Zaneta

“…Mcl-1, an antiapoptotic member of the Bcl-2 family of proteins, is a validated and attractive target for cancer therapy. Overexpression of Mcl-1 in many…”
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