Search Results - "Duncton, Matthew A. J."

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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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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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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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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Preparation of Aryloxetanes and Arylazetidines by Use of an Alkyl−Aryl Suzuki Coupling by Duncton, Matthew A. J, Estiarte, M. Angels, Tan, Darlene, Kaub, Carl, O’Mahony, Donogh J. R, Johnson, Russell J, Cox, Matthew, Edwards, William T, Wan, Min, Kincaid, John, Kelly, Michael G

“…The oxetan-3-yl and azetidin-3-yl substituents have previously been identified as privileged motifs within medicinal chemistry. An efficient approach to…”
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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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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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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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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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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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Oxime derivatives related to AP18: Agonists and antagonists of the TRPA1 receptor by DeFalco, Jeff, Steiger, Daniel, Gustafson, Amy, Emerling, Daniel E., Kelly, Michael G., Duncton, Matthew A.J.

“…AP18 1 was recently disclosed as an antagonist of the TRPA1 receptor by the research group of Patapoutian. However, no detailed structure–activity…”
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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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Novel tricyclic azepine derivatives: Biological evaluation of pyrimido[4,5- b]-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase by Smith, Leon, Wong, Wai C., Kiselyov, Alexander S., Burdzovic-Wizemann, Sabina, Mao, Yunyu, Xu, Yongjiang, Duncton, Matthew A.J., Kim, Ki, Piatnitski, Evgueni L., Doody, Jacqueline F., Wang, Ying, Rosler, Robin L., Milligan, Daniel, Columbus, John, Balagtas, Chris, Lee, Sui Ping, Konovalov, Andrey, Hadari, Yaron R.

“…The synthesis and SAR studies of oxazepines, thiazepines, and diazepines as novel EGFR inhibitor classes are reported. Novel tricyclic derivatives containing…”
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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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A concise one-pot synthesis of trifluoromethyl-containing 2,6-disubstituted 5,6,7,8-tetrahydroquinolines and 5,6,7,8-tetrahydronaphthyridines by Johnson, Russell J, O'Mahony, Donogh J R, Edwards, William T, Duncton, Matthew A J

“…5,6,7,8-Tetrahydroquinolines and 5,6,7,8-tetrahydronaphthyridines with appended trifluoromethyl groups are valuable chemotypes in medicinal chemistry due to…”
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Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2 by Duncton, Matthew A.J., Piatnitski Chekler, Eugene L., Katoch-Rouse, Reeti, Sherman, Dan, Wong, Wai C., Smith, Leon M., Kawakami, Joel K., Kiselyov, Alexander S., Milligan, Daniel L., Balagtas, Chris, Hadari, Yaron R., Wang, Ying, Patel, Sheetal N., Rolster, Robin L., Tonra, James R., Surguladze, David, Mitelman, Stan, Kussie, Paul, Bohlen, Peter, Doody, Jacqueline F.

“…A series of arylphthalazine derivatives were synthesized and evaluated as antagonists of VEGF receptor II (VEGFR-2). IM-094482 57, which was prepared in two…”
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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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Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): Identification of phenmedipham and amperozide as FAAH inhibitors by Vincent, Fabien, Nguyen, Margaret T., Emerling, Daniel E., Kelly, Michael G., Duncton, Matthew A.J.

“…The screening of known medicinal agents against new biological targets has been shown to be a valuable approach for revealing new pharmacology of marketed…”
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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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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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