Search Results - "Peterson, Matt A."

Introduction of a Fluorine Atom at C3 of 3-Deazauridine Shifts Its Antimetabolic Activity from Inhibition of CTP Synthetase to Inhibition of Orotidylate Decarboxylase, an Early Event in the de Novo Pyrimidine Nucleotide Biosynthesis Pathway by Balzarini, Jan, Gago, Federico, Kulik, Wim, van Kuilenburg, André B.P., Karlsson, Anna, Peterson, Matt A., Robins, Morris J.

“…The antimetabolite prodrug 3-deazauridine (3DUrd) inhibits CTP synthetase upon intracellular conversion to its triphosphate, which selectively depletes the…”
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Synthesis and biological evaluation of novel pyrazolo[1,5-a]pyrimidines: Discovery of a selective inhibitor of JAK1 JH2 pseudokinase and VPS34 by Singleton, Justin D., Dass, Reuben, Neubert, Nathaniel R., Smith, Rachel M., Webber, Zak, Hansen, Marc D.H., Peterson, Matt A.

“…[Display omitted] A series of novel 3,6-di-substituted or 3-substituted pyrazolo[1,5-a]pyrimidines were prepared via a microwave-assisted approach that…”
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Discovery of a nanomolar inhibitor of lung adenocarcinoma in vitro by Shelton, Jadd R., Balzarini, Jan, Peterson, Matt A.

“…Efficient methods for the preparation of 5′-substituted 5′-amino-5′-deoxy-N6-ureidoadenosine derivatives are described. Compounds were screened for…”
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Efficient synthesis of 5′-O(N)-carbamyl and -polycarbamyl nucleosides by Shelton, Jadd R., Peterson, Matt A.

“…A simple and efficient method for the preparation of 5′-O(N)-carbamyl and 5′-O(N)-polycarbamyl nucleoside derivatives is reported. The method consisted of…”
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Efficient Preparation of 2-Bromo-6-lithiopyridine via Lithium−Bromine Exchange in Dichloromethane by Peterson, Matt A, Mitchell, Jared R

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Aluminoxy acetals from .alpha.-amino esters: chirality transfer via sequential addition of hydride and C-nucleophiles. 2-Amino alcohols and sphingosines by Polt, Robin, Peterson, Matt A, DeYoung, Lynn

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A broad spectrum anticancer nucleoside with selective toxicity against human colon cells in vitro by Shelton, Jadd R., Burt, Scott R., Peterson, Matt A.

“…A majority of cell lines in the NCI-60 are inhibited with an average GI 50 = 3.13 μM. Selective toxicity against human colon cancer cell lines (COLO 205,…”
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Synthesis and SAR of 2′,3′-bis-O-substituted N6, 5′-bis-ureidoadenosine derivatives: Implications for prodrug delivery and mechanism of action by Shelton, Jadd R., Cutler, Christopher E., Browning, Megan S., Balzarini, Jan, Peterson, Matt A.

“…A series of 2′,3′-bis-O-silylated or -acylated derivatives of lead compound 3a…”
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Synthesis and SAR of 2',3'-bis-O-substituted N(6), 5'-bis-ureidoadenosine derivatives: implications for prodrug delivery and mechanism of action by Shelton, Jadd R, Cutler, Christopher E, Browning, Megan S, Balzarini, Jan, Peterson, Matt A

“…A series of 2',3'-bis-O-silylated or -acylated derivatives of lead compound 3a…”
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Synthesis, SAR, and preliminary mechanistic evaluation of novel antiproliferative N6,5′-bis-ureido- and 5′-carbamoyl-N6-ureidoadenosine derivatives by Shelton, Jadd R., Cutler, Christopher E., Oliveira, Marcelio, Balzarini, Jan, Peterson, Matt A.

“…R=Phenyl, p-chlorophenyl, p-iodophenyl, m-iodophenyl, p-nitrophenyl, p-methoxyphenyl, benzyl, propyl, hexyl, cyclohexyl. We have developed efficient methods…”
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Preliminary SAR analysis of novel antiproliferative N(6),5'-bis-ureidoadenosine derivatives by Peterson, Matt A, Oliveira, Marcelio, Christiansen, Michael A, Cutler, Christopher E

“…A preliminary library of novel N(6),5'-bis-ureidoadenosine analogs and related derivatives was prepared and tested for activity against the NCI 60 panel of…”
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Synthesis and Biological Evaluation of 6-(Alkyn-1-yl)furo[2,3-d]pyrimidin-2(3H)-one Base and Nucleoside Derivatives by Robins, Morris J, Miranda, Karl, Rajwanshi, Vivek K, Peterson, Matt A, Andrei, Graciela, Snoeck, Robert, De Clercq, Erik, Balzarini, Jan

“…Derivatives of the 2‘-deoxynucleoside of furo[2,3-d]pyrimidin-2(3H)-one with long-chain alkyl (or 4-alkylphenyl) substituents at C6 exhibit remarkable anti-VZV…”
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Synthesis and Biological Evaluation of 3,3-Difluoropyridine-2,4(1H,3H)-dione and 3-Deaza-3-fluorouracil Base and Nucleoside Derivatives by Robins, Morris J, Yang, Hong, Miranda, Karl, Peterson, Matt A, Clercq, Erik De, Balzarini, Jan

“…New 3-deaza-3-halouracil nucleosides including 3-deaza-3-fluorouridine and its 2′-deoxy and arabino analogues have been prepared by fluorination of protected…”
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Preliminary SAR analysis of novel antiproliferative N6,5'-bis-ureidoadenosine derivatives by PETERSON, Matt A, OLIVEIRA, Marcelio, CHRISTIANSEN, Michael A, CUTLER, Christopher E

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Synthesis and Antiviral Evaluation of 6-(Alkyl-heteroaryl)furo[2,3-d]pyrimidin-2(3H)-one Nucleosides and Analogues with Ethynyl, Ethenyl, and Ethyl Spacers at C6 of the Furopyrimidine Core by Robins, Morris J, Nowak, Ireneusz, Rajwanshi, Vivek K, Miranda, Karl, Cannon, John F, Peterson, Matt A, Andrei, Graciela, Snoeck, Robert, De Clercq, Erik, Balzarini, Jan

“…Sonogashira coupling strategies were employed to synthesize new furo[2,3-d]pyrimidin-2(3H)-one (FuPyrm) 2‘-deoxynucleoside analogues. Partial or complete…”
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An efficient one-pot synthesis of 2-aminobenzothiazoles from substituted anilines using benzyltrimethylammonium dichloroiodate and ammonium thiocyanate in DMSO:H2O by Dass, Reuben, Peterson, Matt A.

“…[Display omitted] Treatment of a variety of substituted anilines with benzyltrimethylammonium dichloroiodate (1.2 equiv) and ammonium thiocyanate (1.0 equiv)…”
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Bergman cycloaromatization of imidazole-fused enediynes: the remarkable effect of N-aryl substitution by Zhao, Zhengrong, Peng, Yunshan, Dalley, N.Kent, Cannon, John F, Peterson, Matt A

“…N-Arylation enhanced rates relative to N-alkyl derivatives by up to sevenfold (ANOVA p<0.0001). A series of N-aryl substituted `imidazole-fused' ( Z)…”
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An efficient synthesis of 4-Thiocyanato anilines using benzyltrimethylammonium dichloroiodate and ammonium thiocyanate in DMSO:H2O by Dass, Reuben, Singleton, Justin D., Peterson, Matt A.

“…[Display omitted] Treatment of a variety of 2(3)- mono-substituted anilines with benzyltrimethylammonium dichloroiodate (1.2 equiv) and ammonium thiocyanate…”
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An efficient microwave assisted copper catalyzed C-3 amination of 3-bromopyrazolo[1,5-a]pyrimidine by Iorkula, Terungwa H., Tolman, Bryce A., Singleton, Justin D., Peterson, Matt A.

“…[Display omitted] Treatment of 3-bromopyrazolo[1,5-a]pyrimidine with a variety of 1° or 2° alkylamines with 20 mol% CuI, 40 mol% l-proline, and Et3N (2 equiv)…”
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An efficient synthesis of C-6 aminated 3-bromoimidazo[1,2-b]pyridazines by Iorkula, Terungwa H., Tolman, Bryce A., Burt, Scott R., Peterson, Matt A.

“…Treatment of 3-bromo-6-chloroimidazo[1,2-b]pyridazine with a variety of 1° or 2° alkylamines (2.0 equiv) with CsF (1.0 equiv), and BnNEt 3 Cl (10 mol %) in…”
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