Search Results - "Gupton, John T"

The application of formyl group activation of bromopyrrole esters to formal syntheses of lycogarubin C, permethyl storniamide A and lamellarin G trimethyl ether by Gupton, John T., Telang, Nakul, Patteson, Jon, Lescalleet, Kristin, Yeudall, Scott, Sobieski, John, Harrison, Andrew, Curry, Will

“…Lycogarubin C, permethyl storniamide A, and lamellarin G trimethyl ether are pyrrole containing, natural products, which exhibit interesting biological…”
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The application of vinylogous iminium salt derivatives to efficient formal syntheses of the marine alkaloids lamellarin G trimethyl ether and ningalin B by Gupton, John T., Giglio, Benjamin C., Eaton, James E., Rieck, Elizabeth A., Smith, Kristin L., Keough, Matthew J., Barelli, Peter J., Firich, Lauren T., Hempel, Jonathan E., Smith, Timothy M., Kanters, Rene P.F.

“…Studies directed at the synthesis of lamellarin G trimethyl ether and ningalin B via vinylogous iminium salt derivatives are described. The successful strategy…”
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Preparation of indole containing building blocks for the regiospecific construction of indole appended pyrazoles and pyrroles by Gupton, John T., Telang, Nakul, Gazzo, Dominic F., Barelli, Peter J., Lescalleet, Kristin E., Fagan, Jonathan W., Mills, Brandon J., Finzel, Kara L., Kanters, Rene P.F., Crocker, Kyle R., Dudek, Sean T., Lariviere, Corinne M., Smith, Stanton Q., Keertikar, Kartik M.

“…The preparation of an indole appended vinamidinium salt, an indole appended vinylogous amide and an indole appended chloroenal are described. The subsequent…”
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Identification and characterization of a new tubulin-binding tetrasubstituted brominated pyrrole by Mooberry, Susan L, Weiderhold, Kimberly N, Dakshanamurthy, Sivanesan, Hamel, Ernest, Banner, Edith J, Kharlamova, Anastasia, Hempel, Jonathan, Gupton, John T, Brown, Milton L

“…We studied the mechanism of action of 3,5-dibromo-4-(3,4-dimethoxyphenyl)-1H-pyrrole-2-carboxylic acid ethyl ester (JG-03-14) and found that it is a potent…”
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The application of ( Z)-3-aryl-3-haloenoic acids to the synthesis of ( Z)-5-benzylidene-4-arylpyrrol-2(5 H)-ones by Gupton, John T., Telang, Nakul, Banner, Edith J., Kluball, Emily J., Hall, Kayleigh E., Finzel, Kara L., Jia, Xin, Bates, Spencer R., Welden, R. Scott, Giglio, Benjamin C., Eaton, James E., Barelli, Peter J., Firich, Lauren T., Stafford, John A., Coppock, Matthew B., Worrall, Eric F., Kanters, Rene P.F., Keertikar, Kerry, Osterman, Rebecca

“…Studies directed at the synthesis of ( Z)-5-benzylidene-4-arylpyrrol-2(5 H)-ones from ( Z)-3-aryl-3-haloenoic acids are described. The successful strategy…”
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Effects of Poly‐Substituted Pyrroles on Pro‐Inflammatory Signaling in RAW264.7 Macrophages by Offenback, Gabriel H., Fishberg, Cole L., Wang, Annie L., Brown, Madeline M., Gupton, John T., Fischer‐Stenger, Krista

“…Inflammation is the body’s natural means of protection against infection and the restoration to homeostasis after cellular and tissue damage from injury or…”
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How to Deal with Low-Resolution Target Structures: Using SAR, Ensemble Docking, Hydropathic Analysis, and 3D-QSAR to Definitively Map the αβ-Tubulin Colchicine Site by Da, Chenxiao, Mooberry, Susan L, Gupton, John T, Kellogg, Glen E

“…αβ-Tubulin colchicine site inhibitors (CSIs) from four scaffolds that we previously tested for antiproliferative activity were modeled to better understand…”
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Application of vinylogous carbamates and vinylogous aminonitriles to the regiospecific synthesis of uniquely functionalized pyrroles and quinolones by Gupton, John T., Crawford, Evan, Mahoney, Matt, Clark, Evan, Curry, Will, Lane, Annie, Shimozono, Alex, Moore-Stoll, Veronica, Elofson, Kristen, Juekun, Wen, Newton, Micah, Yeudall, Scott, Jaekle, Elizabeth, Kanters, Rene, Sikorski, James A.

“…Pyrroles and quinolones represent core structures, which are routinely found in both natural and synthetic bioactive substances. Consequently, the development…”
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Further studies on the application of vinylogous amides and β-halovinylaldehydes to the regiospecific synthesis of unsymmetrical, polyfunctionalized 2,3,4- and 1,2,3,4- substituted pyrroles by Gupton, John T., Shimozono, Alex, Crawford, Evan, Ortolani, Joe, Clark, Evan, Mahoney, Matt, Heese, Campbell, Noble, Jeffrey, Mandry, Carlos Perez, Kanters, Rene, Dominey, Raymond N., Goldman, Emma W., Sikorski, James A., Fisher, Daniel C.

“…Highly functionalized pyrroles with appropriate regiochemical functionality represent an important class of marine natural products and potential drug…”
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The application of vinylogous iminium salt derivatives to the synthesis of Ningalin B hexamethyl ether by Gupton, John T, Clough, Stuart C, Miller, Robert B, Lukens, John R, Henry, Charlotte A, Kanters, René P.F, Sikorski, James A

“…A vinylogous iminium salt derivative has been used to prepare a 2,3,4-trisubstituted pyrrole synthon in a regioselective, efficient and convenient manner. This…”
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Effects of a pyrrole-based, microtubule-depolymerizing compound on RAW 264.7 macrophages by Ciemniecki, John A., Lewis, Clarke P., Gupton, John T., Fischer-Stenger, Krista

“…RAW 264.7 murine macrophages were exposed to the pyrrole-based compound 3,5-Dibromo-4-(3,4-dimethoxyphenyl)-1H-pyrrole-2-carboxylic acid ethyl ester…”
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Effects of a novel microtubule-depolymerizer on pro-inflammatory signaling in RAW264.7 macrophages by Gilmore, Samuel P., Gonye, Anna L.K., Li, Elizabeth C., Espinosa de los Reyes, Santiago, Gupton, John T., Quintero, Omar A., Fischer-Stenger, Krista

“…The Nuclear Factor-kappa B (NF-κB) pathway is vital for immune system regulation and pro-inflammatory signaling. Many inflammatory disorders and diseases,…”
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Biological Characterization of an Improved Pyrrole-Based Colchicine Site Agent Identified through Structure-Based Design by Rohena, Cristina C, Telang, Nakul S, Da, Chenxiao, Risinger, April L, Sikorski, James A, Kellogg, Glen E, Gupton, John T, Mooberry, Susan L

“…A refined model of the colchicine site on tubulin was used to design an improved analog of the pyrrole parent compound, JG-03-14. The optimized compound,…”
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Ortho group activation of a bromopyrrole ester in Suzuki-Miyaura cross-coupling reactions: Application to the synthesis of new microtubule depolymerizing agents with potent cytotoxic activities by Gupton, John T., Yeudall, Scott, Telang, Nakul, Hoerrner, Megan, Huff, Ellis, Crawford, Evan, Lounsbury, Katie, Kimmel, Michael, Curry, William, Harrison, Andrew, Juekun, Wen, Shimozono, Alex, Ortolani, Joe, Lescalleet, Kristin, Patteson, Jon, Moore-Stoll, Veronica, Rohena, Cristina C., Mooberry, Susan L., Obaidullah, Ahmad J., Kellogg, Glen E., Sikorski, James A.

“…[Display omitted] New microtubule depolymerizing agents with potent cytotoxic activities have been prepared with a 5-cyano or 5-oximino group attached to a…”
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Formyl group activation of a bromopyrrole ester in Suzuki cross-coupling reactions: application to a formal synthesis of Polycitone A and B and Polycitrin A by Gupton, John T., Telang, Nakul, Wormald, Michael, Lescalleet, Kristin, Patteson, Jon, Curry, Will, Harrison, Andrew, Hoerrner, Megan, Sobieski, John, Kimmel, Michael, Kluball, Emily, Perry, Thomas

“…A new pyrrole building block is described, which allows for the regiospecific synthesis of 2,3,5-trisubstituted pyrroles and 2,3,4,5-tetrasubstituted pyrroles…”
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Lipid-lowering effects of ethyl 2-phenacyl-3-aryl-1H-pyrrole- 4-carboxylates in rodents by Holub, Justin M, O'Toole-Colin, Kathy, Getzel, Adam, Argenti, Anthony, Evans, Michael A, Smith, Daniel C, Dalglish, Gerard A, Rifat, Shahzad, Wilson, Donna L, Taylor, Brett M, Miott, Ulander, Glersaye, Josephine, Lam, Kam Suet, McCranor, Bryan J, Berkowitz, Joshua D, Miller, Robert B, Lukens, John R, Krumpe, Keith, Gupton, John T, Burnham, Bruce S

“…A series of substituted 2-phenacyl-3-phenyl-1H-pyrrole-4-carboxylates were prepared from substituted acetophenones in 6 steps. The final condensations between…”
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Autophagy, cell death and sustained senescence arrest in B16/F10 melanoma cells and HCT-116 colon carcinoma cells in response to the novel microtubule poison, JG-03-14 by Biggers, Jonathan W., Nguyen, Tuyen, Di, Xu, Gupton, John T., Henderson, Scott C., Emery, Sean M., Alotaibi, Moureq, White, Kimber L., Brown, Ronetta, Almenara, Jorge, Gewirtz, David A.

“…Purpose Previous studies have shown that the novel microtubule poison, JG-03-14, which binds to the colchicine binding site of tubulin, has the capacity to…”
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Autophagic cell death, polyploidy and senescence induced in breast tumor cells by the substituted pyrrole JG-03-14, a novel microtubule poison by Arthur, Christopher R., Gupton, John T., Kellogg, Glen E., Yeudall, W. Andrew, Cabot, Myles C., Newsham, Irene F., Gewirtz, David A.

“…JG-03-14, a substituted pyrrole that inhibits microtubule polymerization, was screened against MCF-7 (p53 wild type), MDA-MB231 (p53 mutant), MCF-7/caspase 3…”
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Interference with endothelial cell function by JG-03-14, an agent that binds to the colchicine site on microtubules by Dalyot-Herman, Nava, Delgado-Lopez, Fernando, Gewirtz, David A., Gupton, John T., Schwartz, Edward L.

“…The microtubule-binding agent JG-03-14 (left) disrupted the structure of adherens junctions (middle) and caused membrane blebbing (right) in endothelial cells,…”
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Docking and hydropathic scoring of polysubstituted pyrrole compounds with antitubulin activity by Tripathi, Ashutosh, Fornabaio, Micaela, Kellogg, Glen E., Gupton, John T., Gewirtz, David A., Yeudall, W. Andrew, Vega, Nina E., Mooberry, Susan L.

“…HINT Interaction maps of JG-03-14 bound at the colchicine site of tubulin. Blue contours: favorable polar (H-bond); red: unfavorable polar; green: hydrophobic…”
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