Search Results - "Mesaros, Eugen F"

Discovery of Clinical Candidate CEP-37440, a Selective Inhibitor of Focal Adhesion Kinase (FAK) and Anaplastic Lymphoma Kinase (ALK) by Ott, Gregory R, Cheng, Mangeng, Learn, Keith S, Wagner, Jason, Gingrich, Diane E, Lisko, Joseph G, Curry, Matthew, Mesaros, Eugen F, Ghose, Arup K, Quail, Matthew R, Wan, Weihua, Lu, Lihui, Dobrzanski, Pawel, Albom, Mark S, Angeles, Thelma S, Wells-Knecht, Kevin, Huang, Zeqi, Aimone, Lisa D, Bruckheimer, Elizabeth, Anderson, Nathan, Friedman, Jay, Fernandez, Sandra V, Ator, Mark A, Ruggeri, Bruce A, Dorsey, Bruce D

“…Analogues structurally related to anaplastic lymphoma kinase (ALK) inhibitor 1 were optimized for metabolic stability. The results from this endeavor not only…”
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Evolution of a Total Synthesis of (−)-Kendomycin Exploiting a Petasis−Ferrier Rearrangement/Ring-Closing Olefin Metathesis Strategy by Smith, Amos B, Mesaros, Eugen F, Meyer, Emmanuel A

“…A convergent stereocontrolled total synthesis of (−)-kendomycin (1) has been achieved. The synthesis proceeds with a longest linear sequence of 21 steps,…”
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Strategies to Mitigate the Bioactivation of 2-Anilino-7-Aryl-Pyrrolo[2,1-f][1,2,4]triazines: Identification of Orally Bioavailable, Efficacious ALK Inhibitors by Mesaros, Eugen F, Thieu, Tho V, Wells, Gregory J, Zificsak, Craig A, Wagner, Jason C, Breslin, Henry J, Tripathy, Rabindranath, Diebold, James L, McHugh, Robert J, Wohler, Ashley T, Quail, Matthew R, Wan, Weihua, Lu, Lihui, Huang, Zeqi, Albom, Mark S, Angeles, Thelma S, Wells-Knecht, Kevin J, Aimone, Lisa D, Cheng, Mangeng, Ator, Mark A, Ott, Gregory R, Dorsey, Bruce D

“…Chemical strategies to mitigate cytochrome P450-mediated bioactivation of novel 2,7-disubstituted pyrrolo­[2,1-f]­[1,2,4]­triazine ALK inhibitors are described…”
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Total Synthesis of (−)-Kendomycin Exploiting a Petasis−Ferrier Rearrangement/Ring-Closing Olefin Metathesis Synthetic Strategy by Smith, Amos B, Mesaros, Eugen F, Meyer, Emmanuel A

“…The total synthesis of (−)-kendomycin (1), a novel macrocyclic polyketide with antibacterial and antitumor activity, was achieved in 21 steps (longest linear…”
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Rational Design, Synthesis, and Structure–Activity Relationship of a Novel Isoquinolinone-Based Series of HBV Capsid Assembly Modulators Leading to the Identification of Clinical Candidate AB-836 by Cole, Andrew G., Kultgen, Steven G., Mani, Nagraj, Fan, Kristi Yi, Ardzinski, Andrzej, Stever, Kim, Dorsey, Bruce D., Mesaros, Eugen F., Thi, Emily P., Graves, Ingrid, Tang, Sunny, Harasym, Troy O., Lee, Amy C. H., Olland, Andrea, Suto, Robert K., Sofia, Michael J.

“…Inhibition of Hepatitis B Virus (HBV) replication by small molecules that modulate capsid assembly and the encapsidation of pgRNA and viral polymerase by HBV…”
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Conformationally Constrained Isoquinolinones as Orally Efficacious Hepatitis B Capsid Assembly Modulators by Mesaros, Eugen F, Cole, Andrew G, Kultgen, Steven G, Mani, Nagraj, Fan, Kristi Yi, Dugan, Benjamin J, Ardzinski, Andrzej, Stever, Kim, Micolochick Steuer, Holly M, Graves, Ingrid, Tang, Sunny, Harasym, Troy O, Lam, Angela M, Thi, Emily P, Dorsey, Bruce D, Sofia, Michael J

“…Isoquinolinone-based HBV capsid assembly modulators that bind at the dimer:dimer interface of HBV core protein have been shown to suppress viral replication in…”
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Anaplastic lymphoma kinase inhibitors as anticancer therapeutics: a patent review by Mesaros, Eugen F, Ott, Gregory R, Dorsey, Bruce D

“…Anaplastic lymphoma kinase (ALK), a receptor tyrosine kinase from the insulin receptor superfamily, is implicated in the oncogenesis of numerous cancers…”
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A Selective, Orally Bioavailable 1,2,4-Triazolo[1,5-a]pyridine-Based Inhibitor of Janus Kinase 2 for Use in Anticancer Therapy: Discovery of CEP-33779 by Dugan, Benjamin J, Gingrich, Diane E, Mesaros, Eugen F, Milkiewicz, Karen L, Curry, Matthew A, Zulli, Allison L, Dobrzanski, Pawel, Serdikoff, Cynthia, Jan, Mahfuza, Angeles, Thelma S, Albom, Mark S, Mason, Jennifer L, Aimone, Lisa D, Meyer, Sheryl L, Huang, Zeqi, Wells-Knecht, Kevin J, Ator, Mark A, Ruggeri, Bruce A, Dorsey, Bruce D

“…Members of the JAK family of nonreceptor tyrosine kinases play a critical role in the growth and progression of many cancers and in inflammatory diseases. JAK2…”
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Discovery of C‑Linked Nucleoside Analogues with Antiviral Activity against SARS-CoV‑2 by Mesaros, Eugen F., Dugan, Benjamin J., Gao, Min, Sheraz, Muhammad, McGovern-Gooch, Kayleigh, Xu, Fran, Fan, Kristi Yi, Nguyen, Duyan, Kultgen, Steven G., Lindstrom, Aaron, Stever, Kim, Tercero, Breanna, Binder, Randall J., Liu, Fei, Micolochick Steuer, Holly M., Mani, Nagraj, Harasym, Troy O., Thi, Emily P., Cuconati, Andrea, Dorsey, Bruce D., Cole, Andrew G., Lam, Angela M., Sofia, Michael J.

“…The recent COVID-19 pandemic underscored the limitations of currently available direct-acting antiviral treatments against acute respiratory RNA-viral…”
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Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase by Mesaros, Eugen F., Angeles, Thelma S., Albom, Mark S., Wagner, Jason C., Aimone, Lisa D., Wan, Weihua, Lu, Lihui, Huang, Zeqi, Olsen, Mark, Kordwitz, Emily, Haltiwanger, R. Curtis, Landis, Amy J., Cheng, Mangeng, Ruggeri, Bruce A., Ator, Mark A., Dorsey, Bruce D., Ott, Gregory R.

“…[Display omitted] The diastereoselective synthesis and biological activity of piperidine-3,4-diol and piperidine-3-ol-derived pyrrolotriazine inhibitors of…”
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2,7-Disubstituted-pyrrolo[2,1-f][1,2,4]triazines: New Variant of an Old Template and Application to the Discovery of Anaplastic Lymphoma Kinase (ALK) Inhibitors with in Vivo Antitumor Activity by Ott, Gregory R, Wells, Gregory J, Thieu, Tho V, Quail, Matthew R, Lisko, Joseph G, Mesaros, Eugen F, Gingrich, Diane E, Ghose, Arup K, Wan, Weihua, Lu, Lihui, Cheng, Mangeng, Albom, Mark S, Angeles, Thelma S, Huang, Zeqi, Aimone, Lisa D, Ator, Mark A, Ruggeri, Bruce A, Dorsey, Bruce D

“…A novel 2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazine scaffold has been designed as a new kinase inhibitor platform mimicking the bioactive conformation of…”
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Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models by Mesaros, Eugen F., Burke, Jason P., Parrish, Jonathan D., Dugan, Benjamin J., Anzalone, Andrew V., Angeles, Thelma S., Albom, Mark S., Aimone, Lisa D., Quail, Matthew R., Wan, Weihua, Lu, Lihui, Huang, Zeqi, Ator, Mark A., Ruggeri, Bruce A., Cheng, Mangeng, Ott, Gregory R., Dorsey, Bruce D.

“…The synthesis and biological evaluation of potent and selective anaplastic lymphoma kinase (ALK) inhibitors from a novel class of 2,4-diaminopyrimidines,…”
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Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors by Zificsak, Craig A, Theroff, Jay P, Aimone, Lisa D, Angeles, Thelma S, Albom, Mark S, Cheng, Mangeng, Mesaros, Eugen F, Ott, Gregory R, Quail, Matthew R, Underiner, Ted L, Wan, Weihua, Dorsey, Bruce D

“…The incorporation of R,R-1,2-diaminocyclohexane at C4 in a series of 2,4-diaminopyrimidines led to a number of ALK inhibitors in which optimized activity was…”
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2,7-Disubstituted-Pyrrolotriazine Kinase Inhibitors with an Unusually High Degree of Reactive Metabolite Formation by Wells-Knecht, Kevin J, Ott, Gregory R, Cheng, Mangeng, Wells, Gregory J, Breslin, Henry J, Gingrich, Diane E, Weinberg, Linda, Mesaros, Eugen F, Huang, Zeqi, Yazdanian, Mehran, Ator, Mark A, Aimone, Lisa D, Zeigler, Kelli, Dorsey, Bruce D

“…There are numerous published studies establishing a link between reactive metabolite formation and toxicity of various drugs. Although the correlation between…”
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Design, Synthesis, and Structural Analysis of d,l-Mixed Polypyrrolinones. 2. Macrocyclic Hexapyrrolinones by Smith, III, Amos B, Xiong, Hui, Charnley, Adam K, Brenner, Meinrad, Mesaros, Eugen F, Kenesky, Craig S, Di Costanzo, Luigi, Christianson, David W, Hirschmann, Ralph

“…The design, synthesis, and structural analysis of two macrocyclic d,l-alternating hexapyrrolinones have been achieved. These cyclic peptide mimics adopt a…”
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Diastereoselective Conjugate Additions to π-Allylmolybdenum Complexes:  A Stereocontrolled Route to 3,4,5-Trisubstituted γ-Butyrolactones by Pearson, Anthony J, Mesaros, Eugen F

“…π-Allylmolybdenum complex 6b is obtained as a single isomer by Knoevenagel condensation of aldehyde 1 with Meldrum's acid. Conjugate additions of Grignard…”
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Design, Synthesis, and Binding Affinities of Pyrrolinone-Based Somatostatin Mimetics by Smith, Amos B., Charnley, Adam K., Mesaros, Eugen F., Kikuchi, Osamu, Wang, Wenyong, Benowitz, Andrew, Chu, Chi-Lien, Feng, Jin-Jye, Chen, Kuo-Hsin, Lin, Atsui, Cheng, Fong-Chi, Taylor, Laurie, Hirschmann, Ralph

“…Tetrapyrrolinone somatostatin (SRIF) mimetics (cf. 1), based on a heterochiral (d,l-mixed) pyrrolinone scaffold, were designed, synthesized, and evaluated for…”
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Stereocontrolled Construction of Tetrahydrofurans and γ-Butyrolactones Using Organomolybdenum Chemistry by Pearson, Anthony J, Mesaros, Eugen F

“…Diastereoselective conversion of π-allylmolybdenum complex aldehyde 1 to organometallic triol 4 and diols 5, 10, and 13 is described. Stereocontrolled…”
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Corrigendum to “Novel 2,3,4,5-tetrahydro-benzo[ d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models” [Bioorg. Med. Chem. Lett. 21 (2011) 463] by Mesaros, Eugen F., Burke, Jason P., Parrish, Jonathan D., Dugan, Benjamin J., Anzalone, Andrew V., Angeles, Thelma S., Albom, Mark S., Aimone, Lisa D., Quail, Matthew R., Wan, Weihua, Lu, Lihui, Huang, Zeqi, Ator, Mark A., Ruggeri, Bruce A., Cheng, Mangeng, Ott, Gregory R., Dorsey, Bruce D.

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