Search Results - "Mayes, Benjamin"

Pharmacological Characterization of SDX-7320/Evexomostat: A Novel Methionine Aminopeptidase Type 2 Inhibitor with Anti-tumor and Anti-metastatic Activity by Cornelius, Peter, Mayes, Benjamin A, Petersen, John S, Turnquist, David J, Dufour, Pierre J, Dannenberg, Andrew J, Shanahan, James M, Carver, Bradley J

“…Methionine aminopeptidase type 2 (METAP2) is a ubiquitous, evolutionarily conserved metalloprotease fundamental to protein biosynthesis which catalyzes removal…”
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Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor by Dousson, Cyril, Alexandre, François-René, Amador, Agnès, Bonaric, Séverine, Bot, Stéphanie, Caillet, Catherine, Convard, Thierry, da Costa, Daniel, Lioure, Marie-Pierre, Roland, Arlène, Rosinovsky, Elodie, Maldonado, Sébastien, Parsy, Christophe, Trochet, Christophe, Storer, Richard, Stewart, Alistair, Wang, Jingyang, Mayes, Benjamin A, Musiu, Chiara, Poddesu, Barbara, Vargiu, Luana, Liuzzi, Michel, Moussa, Adel, Jakubik, Jocelyn, Hubbard, Luke, Seifer, Maria, Standring, David

“…Here, we describe the design, synthesis, biological evaluation, and identification of a clinical candidate non-nucleoside reverse transcriptase inhibitors…”
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Development of an Efficient Manufacturing Process to GSK2248761A API by Bret, Celine, Smith, Elaine, Vit, Erica, Hayes, Jerome F, Hayler, John D, Ironmonger, Alan, Pascoe, David, Hodnett, Neil, Stanway, Jonathan, Etridge, Stephen, Stewart, Alistair, Wang, Jingyang, Mayes, Benjamin A, Moussa, Adel

“…Amidation of indole 2-carboxylate 1 with ammonia gas via the imidazolide 2 gave GSK2248761A API 3, which was in development for the treatment of HIV. Three…”
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Synthesis of 2,3-Dideoxy-2-fluoro-2,3-endo-methylene- and 2,3-Dideoxy-2-fluoro-3‑C‑hydroxymethyl-2,3-endo-methylene-pentofuranoses and Their Use in the Preparation of Conformationally Locked Bicyclic Nucleosides by Clarkson, Rob, Komsta, Zofia, Mayes, Benjamin A, Moussa, Adel, Shelbourne, Montserrat, Stewart, Alistair, Tyrrell, Andrew J, Wallis, Laura L, Weymouth-Wilson, Alexander C

“…Construction of protected 2,3-dideoxy-2-fluoro-2,3-endo-methylene-pento­furanoses from d-glyceraldehyde and…”
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Stereoselective Cyclopropanation in the Synthesis of 3′-Deoxy-3′‑C‑hydroxymethyl-2′,3′-methylene-uridine by Komsta, Zofia, Mayes, Benjamin A, Moussa, Adel, Shelbourne, Montserrat, Stewart, Alistair, Tyrrell, Andrew J, Wallis, Laura L, Weymouth-Wilson, Alexander C, Yurek-George, Alexander

“…The synthesis of the novel 2′,3′-cyclopropane nucleoside 3′-deoxy-3′-C-hydroxymethyl-2′,3′-methylene-uridine is described. Stereoselective construction of the…”
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Synthesis of 2′-O,4′-C-alkylene-bridged ribonucleosides and their evaluation as inhibitors of HCV NS5B polymerase by Chapron, Christopher, Glen, Rebecca, La Colla, Massimiliano, Mayes, Benjamin A., McCarville, Joseph F., Moore, Stephen, Moussa, Adel, Sarkar, Ruhul, Seifer, Maria, Serra, Ilaria, Stewart, Alistair

“…The synthesis of 2′-O,4′-C-methylene-bridged bicyclic guanine ribonucleosides bearing 2′-C-methyl or 5′-C-methyl modifications is described. Key to the…”
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Synthesis of a Nucleoside Phosphoramidate Prodrug Inhibitor of HCV NS5B Polymerase: Phenylboronate as a Transient Protecting Group by Mayes, Benjamin A, Arumugasamy, Jeevanandam, Baloglu, Erkan, Bauer, David, Becker, Alan, Chaudhuri, Narayan, Latham, G. Mark, Li, Jie, Mathieu, Steve, McGarry, F. Patrick, Rosinovsky, Elodie, Stewart, Alistair, Trochet, Christophe, Wang, Jingyang, Moussa, Adel

“…A synthetic process for 2′-C-methyl­cytidine-5′-[2-[(3-hydroxy-2,2-di­methyl-1-oxo­propyl)thio]ethyl-N-benzyl­phosphor­amidate], a nucleotide prodrug inhibitor…”
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Development of Related HCV Protease Inhibitors: Macrocyclization of Two Highly Functionalized Dienyl-ureas via Ring-Closing Metathesis by Arumugasamy, Jeevanandam, Arunachalam, Kannan, Bauer, David, Becker, Alan, Caillet, Catherine A, Glynn, Roberta, Latham, G. Mark, Lim, Jinsoo, Liu, Jia, Mayes, Benjamin A, Moussa, Adel, Rosinovsky, Elodie, Salanson, Aurelien E, Soret, Adrien F, Stewart, Alistair, Wang, Jingyang, Wu, Xinghua

“…A novel assembly of two structurally related 14-membered ring macrocyclic hepatitis C virus protease inhibitors is presented. Key to their successful…”
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Scalable Synthesis of a Nucleoside Phosphoramidate Prodrug Inhibitor of HCV NS5B RdRp: Challenges in the Production of a Diastereomeric Mixture by Mayes, Benjamin A, Wang, Jingyang, Arumugasamy, Jeevanandam, Arunachalam, Kannan, Baloglu, Erkan, Bauer, David, Becker, Alan, Chaudhuri, Narayan, Glynn, Roberta, Latham, G. Mark, Li, Jie, Lim, Jinsoo, Liu, Jia, Mathieu, Steve, McGarry, F. Patrick, Rosinovsky, Elodie, Soret, Adrien F, Stewart, Alistair, Moussa, Adel

“…A scalable process is described for the synthesis of 2′-C-methyl­guanosine-5′-[2-[(3-hydroxy-2,2-dimethyl-1-oxopropyl)­thio]­ethyl-N-benzyl­phosphor­amidate],…”
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Pharmacokinetics of IDX184, a liver-targeted oral prodrug of 2′-methylguanosine-5′-monophosphate, in the monkey and formulation optimization for human exposure by Pan-Zhou, Xin-Ru, Mayes, Benjamin A., Rashidzadeh, Hassan, Gasparac, Rahela, Smith, Steven, Bhadresa, Sanjeev, Gupta, Kusum, Cohen, Marita Larsson, Bu, Charlie, Good, Steven S., Moussa, Adel, Rush, Roger

“…IDX184 is a phosphoramidate prodrug of 2′-methylguanosine-5′-monophosphate, developed to treat patients infected with hepatitis C virus. A mass balance study…”
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Robust Synthesis of Methyl 5-Chloro-4-fluoro-1H-indole-2-carboxylate: A Key Intermediate in the Preparation of an HIV NNRTI Candidate by Mayes, Benjamin A, Chaudhuri, Narayan C, Hencken, Christopher P, Jeannot, Frederic, Latham, G. Mark, Mathieu, Steven, McGarry, F. Patrick, Stewart, Alistair J, Wang, Jingyang, Moussa, Adel

“…A synthetic preparation of methyl 5-chloro-4-fluoro-1H-indole-2-carboxylate, a key intermediate towards phosphoindole inhibitors of HIV non-nucleoside reverse…”
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Huge (14-, 21-, 28-, 35-, 56- and 70-membered ring) macrocyclic lactams––a novel family of carbopeptoid-cyclodextrins by Mayes, Benjamin A, Simon, Lieven, Watkin, David J, Ansell, Christopher W.G, Fleet, George W.J

“…Graphic Hydrogenation of linear ω-azido-pentafluorophenyl esters gives cyclic peptides containing 14-, 21-, 28-, 35-, 56- and 70-membered ring lactams from…”
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Abstract P5-05-04: Inhibition of HER2+ tumor growth with SDX-7320, a novel MetAP2 inhibitor, alone and in combination with capivasertib/AZD-5363: Reduced expression of hypoxia-inducible and innate-immune system genes by Cornelius, Peter, Mayes, Benjamin, Dufour, Pierre, Kalinich, Mark, Wang, Jonathan, Little, Sara, Carver, Bradley, Shanahan, James

“…MetAP2 inhibitors have shown clinical anti-tumor activity, but CNS side effects and poor drug-like properties have generally limited their development…”
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The Amelia-1 study: A phase 1b/2 trial of evexomostat (SDX-7320) plus fulvestrant and alpelisib in patients with advanced breast cancer at risk for alpelisib-induced hyperglycemia by Cornelius, Peter, Salomon, Neal, Browning, David, Mayes, Benjamin, Dufour, Pierre, Fletcher, Margaret S., Shanahan, James, Carver, Bradley, Rugo, Hope S.

“…TPS1129 Background: Alpelisib, a selective PI3K p110a inhibitor, was approved for breast cancer patients with PIK3CA mutations. An on-target toxicity of…”
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Abstract 1068: SDX-7320, a novel inhibitor of methionine aminopeptidase 2 (MetAP2), inhibits MCF-7 tumor growth in combination with palbociclib (Ibrance®) by Cornelius, Peter, Mayes, Benjamin, Dufour, Pierre, Little, Sara, Slee, Andrew, Nir, Raphael, Nir, Adam, Carver, Bradley J., Shanahan, James

“…Small molecule MetAP2 inhibitor TNP-470 previously showed clinical anti-tumor activity, however CNS side effects and poor drug-like properties limited its…”
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Abstract P3-11-13: Synergistic inhibition of MCF-7 mammary gland tumor growth with Piqray® (alpelisib) plus SDX-7320, a novel polymer-conjugated methionine aminopeptidase 2 (MetAP2) inhibitor by Cornelius, Peter, Mayes, Benjamin, Little, Sara, Slee, Andrew, Nir, Adam, Nir, Raphael, Carver, Bradley, Shanahan, James

“…Mutations in the PI3K pathway have been observed in about 40% of ER+/Her2- breast cancer patients. Amplification as well as mutation of the catalytic p110α…”
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Abstract 1226: A novel polymer-conjugated methionine aminopeptidase 2 (MetAP2) inhibitor SDX-7320 inhibits the growth of EO771 mammary gland tumors and ameliorates the immunosuppressive tumor immune micro-environment (TIME) by Cornelius, Peter, Mayes, Benjamin, Little, Sara, Slee, Andrew, Turnquist, David, Shanahan, James, Carver, Bradley

“…Obese patients with certain cancers face a greater risk of dying from their cancer compared to non-obese patients. Obesity may contribute to cancer progression…”
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Abstract 1656: Evexomostat: A novel therapeutic in development for the treatment of prostate cancer by Cornelius, Peter, Mayes, Benjamin, Carver, Bradley J., Shanahan, James, Gunter, Jennifer, Nelson, Colleen

“…Background: Prostate cancer (PCa) is the second-most diagnosed malignancy among men and is a leading cause of cancer death worldwide (WHO, 2020). Elevated…”
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Abstract CT153: SDX-7320 elicits improvements in tumor-related and metabolic biomarkers: Results of a phase 1 dose-escalation study in patients with advanced refractory or late-stage solid tumors by Mita, Monica M., Bendell, Johanna, Mita, Alain C., Gordon, Michael, Sachdev, Jasgit, Carver, Bradley J., Shanahan, James, Mayes, Benjamin, Awerkamp, Kris, Browning, David, Salomon, Neal, Sullivan, Kimberly, Anderson-Villaluz, Alfred, Johnson, Joe, Petersen, John S., Turnquist, David J., Cornelius, Peter

“…Background and Rationale: Metabo-oncology is the study of specific tumor types whose growth and/or metastasis is accelerated by metabolic dysfunction, often…”
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Abstract 4919: Preclinical activity of SDX-7320 in mouse models of obesity and obesity-driven cancer by Cornelius, Peter, Petersen, John S., Mayes, Benjamin, Turnquist, David, Sullivan, Kimberly, Anderson-Villaluz, Alfred, Lutz, Robert, Little, Sara, Slee, Andrew, Carver, Bradley J., Shanahan, James

“…Cancer patients who are obese face a greater risk of dying from cancer compared to nonobese patients (Calle, 2003). Obesity is believed to contribute to…”
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