Search Results - "Duncton, Matthew"

Orally Absorbed Derivatives of the β‑Lactamase Inhibitor Avibactam. Design of Novel Prodrugs of Sulfate Containing Drugs by Gordon, Eric M, Duncton, Matthew A. J, Gallop, Mark A

“…Only one FDA-approved β-lactamase inhibitor has ever been orally available: clavulanic acid, approved in 1984. Avibactam, approved by FDA in 2015, is the first…”
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TRPV4 agonists and antagonists by Vincent, Fabien, Duncton, Matthew A J

“…TRPV4 belongs to the TRPV subfamily of Transient Receptor Potential (TRP) ion channels. This year marks the 10 year anniversary of the discovery of this…”
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Synthesis of trans-2-(Trifluoromethyl)cyclopropanes via Suzuki Reactions with an N‑Methyliminodiacetic Acid Boronate by Duncton, Matthew A. J, Singh, Rajinder

“…trans-2-(Trifluoromethyl)cyclopropylboronic acid N-methyliminodiacetic acid (MIDA) ester 5 was synthesized as a pure diastereomer from vinylboronic acid MIDA…”
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A Single-Step Synthesis of Azetidine-3-amines by Wang, Brian J, Duncton, Matthew A J

“…The azetidine group is frequently encountered within contemporary medicinal chemistry. However, the introduction of an azetidine can be synthetically…”
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A New Drug Discovery Platform: Application to DNA Polymerase Eta and Apurinic/Apyrimidinic Endonuclease 1 by Das, Debanu, Duncton, Matthew A J, Georgiadis, Taxiarchis M, Pellicena, Patricia, Clark, Jennifer, Sobol, Robert W, Georgiadis, Millie M, King-Underwood, John, Jobes, David V, Chang, Caleb, Gao, Yang, Deacon, Ashley M, Wilson, 3rd, David M

“…The ability to quickly discover reliable hits from screening and rapidly convert them into lead compounds, which can be verified in functional assays, is…”
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Development of a MEK inhibitor, NFX-179, as a chemoprevention agent for squamous cell carcinoma by Sarin, Kavita Y, Kincaid, John, Sell, Brittney, Shahryari, Jahanbanoo, Duncton, Matthew A J, Morefield, Elaine, Sun, Wenchao, Prieto, Karol, Chavez-Chiang, Omar, de Moran Segura, Carlos, Nguyen, Jonathan, Bronson, Roderick T, Plotkin, Scott R, Kochendoerfer, Gerd G, Fenn, Peter, Wootton, Michael A, Powala, Christopher, de Souza, Mark P, Tsai, Kenneth Y

“…Cutaneous squamous cell carcinoma (cSCC) is the second most common skin cancer. Although cSCC contributes to substantial morbidity and mortality in high-risk…”
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Identification and characterization of novel TRPV4 modulators by Vincent, Fabien, Acevedo, Alejandra, Nguyen, Margaret T., Dourado, Michelle, DeFalco, Jeff, Gustafson, Amy, Spiro, Peter, Emerling, Daniel E., Kelly, Michael G., Duncton, Matthew A.J.

“…TRPV4, a close relative of the vanilloid receptor TRPV1, is activated by diverse modalities such as endogenous lipid ligands, hypotonicity, protein kinases…”
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Tetrazolone as an acid bioisostere: application to marketed drugs containing a carboxylic acid by Duncton, Matthew A J, Murray, Ryan B, Park, Gary, Singh, Rajinder

“…Matched molecular pair analysis was used to evaluate the ability of a tetrazolone group to act as a bioisostere of a carboxylic acid. Compound 7, a tetrazolone…”
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Fragment- and structure-based drug discovery for developing therapeutic agents targeting the DNA Damage Response by Wilson, David M., Deacon, Ashley M., Duncton, Matthew A.J., Pellicena, Patricia, Georgiadis, Millie M., Yeh, Andrew P., Arvai, Andrew S., Moiani, Davide, Tainer, John A., Das, Debanu

“…Cancer will directly affect the lives of over one-third of the population. The DNA Damage Response (DDR) is an intricate system involving damage recognition,…”
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A one-pot synthesis of tetrazolones from acid chlorides: understanding functional group compatibility, and application to the late-stage functionalization of marketed drugs by Duncton, Matthew A J, Singh, Rajinder

“…A one-pot and scalable synthesis of tetrazolones (tetrazol-5-ones) from acid chlorides using azidotrimethylsilane is presented. The reaction tolerates many…”
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Preparation of Heteroaryloxetanes and Heteroarylazetidines by Use of a Minisci Reaction by Duncton, Matthew A. J, Estiarte, M. Angels, Johnson, Russell J, Cox, Matthew, O’Mahony, Donogh J. R, Edwards, William T, Kelly, Michael G

“…Introduction of oxetan-3-yl and azetidin-3-yl groups into heteroaromatic bases was achieved by using a radical addition method (Minisci reaction). To…”
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Early Drug Discovery and Development of Novel Cancer Therapeutics Targeting DNA Polymerase Eta (POLH) by Wilson, David M, Duncton, Matthew A J, Chang, Caleb, Lee Luo, Christie, Georgiadis, Taxiarchis M, Pellicena, Patricia, Deacon, Ashley M, Gao, Yang, Das, Debanu

“…Polymerase eta (or Pol η or POLH) is a specialized DNA polymerase that is able to bypass certain blocking lesions, such as those generated by ultraviolet…”
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Synthesis of 9-nitro-5H-spiro[benzo[b]tetrazolo[1,5-d][1,4]oxazepine-4,2′-oxirane] via an unusual ring-expansion by Kolluri, Rao, Zhang, Jing, Singh, Rajinder, Duncton, Matthew A.J.

“…[Display omitted] •An unusual ring-expansion to prepare 9-nitro-5H-spiro[benzo[b]tetrazolo[1,5-d][1,4]oxazepine-4,2′-oxirane].•A medium-ring and spirocyclic…”
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Enantioselective synthesis of an octahydroindolizine (indolizidine) alcohol using an enzymatic resolution by Zhang, Jing, Kolluri, Rao, Alvarez, Salvador G, Irving, Mark M, Singh, Rajinder, Duncton, Matthew A J

“…A homo-chiral synthesis of (7R,8aS)-octahydro-5,5-dimethylindolizin-7-amine 8 and (7S, 8aS)-octahydro-5,5-dimethylindolizin-7-ol 9, amine building blocks which…”
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5-Benzyloxytryptamine as an antagonist of TRPM8 by DeFalco, Jeff, Steiger, Daniel, Dourado, Michelle, Emerling, Daniel, Duncton, Matthew A.J.

“…5-Benzyloxytryptamine 19 was found to be an antagonist of TRPM8. Related tryptamine derivatives showed diminished, or no activity at TRPM8…”
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Tuning the Reactivity of Nuclear Factor Erythroid 2‑Related Factor 2 (Nrf2) Activators for Optimal in Vivo Efficacy by Markovtsov, Vadim, Duncton, Matthew A. J., Bagos, Art, Yi, Sothy, Braselmann, Sylvia, Bhamidipati, Somasekhar, Darwish, Ihab S., Yu, Jiaxin, Owyang, Alexander M., Fernandez, Beth, Samant, Bhushan, Park, Gary, Masuda, Esteban S., Shaw, Simon J.

“…Dimethyl fumarate 1 is approved for the treatment of multiple sclerosis but is also associated with off-target activation of the niacin receptor. By using a…”
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Toward Orally Absorbed Prodrugs of the Antibiotic Aztreonam. Design of Novel Prodrugs of Sulfate Containing Drugs. Part 2 by Gordon, Eric M, Duncton, Matthew A. J, Wang, Brian J, Qi, Longwu, Fan, Dazhong, Li, Xianfeng, Ni, Zhi-Jie, Ding, Pingyu, Grygorash, Ruslan, Low, Eddy, Yu, Guijun, Sun, Jiawei

“…Aztreonam, first discovered in 1980, is an FDA approved, intravenous, monocyclic beta-lactam antibiotic. Aztreonam is active against Gram-negative bacteria and…”
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TRPM8 biology and medicinal chemistry by DeFalco, Jeff, Duncton, Matthew A J, Emerling, Daniel

“…TRPM8 belongs to the TRPM Melastatin subfamily of Transient Receptor Potential (TRP) ion channels. Activated by cool temperatures and mimetic ligands, such as…”
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Identification of orally-bioavailable antagonists of the TRPV4 ion-channel by Wei, Zhi-Liang, Nguyen, Margaret T., O’Mahony, Donogh J.R., Acevedo, Alejandra, Zipfel, Sheila, Zhang, Qingling, Liu, Luna, Dourado, Michelle, Chi, Candace, Yip, Victor, DeFalco, Jeff, Gustafson, Amy, Emerling, Daniel E., Kelly, Michael G., Kincaid, John, Vincent, Fabien, Duncton, Matthew A.J.

“…[Display omitted] Antagonists of the TRPV4 receptor were identified using a focused screen, followed by a limited optimization program. The leading compounds…”
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A practical asymmetric synthesis of ortho-substituted 4-pyrazolyl-2-ethylamines by O'Mahony, Donogh J.R., Johnson, Russell J., Estiarte, M. Angels, Edwards, William T., Duncton, Matthew A.J.

“…[Display omitted] •An asymmetric synthesis of ortho-substituted 4-pyrazolyl-2-ethylamines.•The synthesis employs Ellman’s tert-butanesulfinamine chiral…”
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