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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共23条记录   Identification of a novel Smoothened antagonist that potently suppresses Hedgehog signaling [作者：WANG JIANGBO; MOOK ROBERT A JR; LU JIUYI; GOODEN DAVID M; RIBEIRO ANTHONY; GUO ANCHEN; BARAK LARRY S; LYERLY H KIM; CHEN WEI,期刊：Bioorganic & Medicinal Chemistry, 页码：6751-6757 , 文章类型： Article，,卷期：2012年20-22] The Hedgehog signaling pathway plays an essential role in embryo development and adult tissue homeostasis, in regulating stem cells and is abnormally activated in many cancers. Given the importance of this signaling path... Trimeric purine nucleoside phosphorylase: Exploring postulated one-third-of-the-sites binding in the transition state [作者：WIELGUSKUTROWSKA BEATA; BREER KATARZYNA; HASHIMOTO MARIKO; HIKISHIMA SADAO; YOKOMATSU TSUTOMU; NARCZYK MARTA; DYZMA ALICJA; GIRSTUN AGNIESZKA; STARON KRZYSZTOF; BZOWSKA AGNIESZKA,期刊：Bioorganic & Medicinal Chemistry, 页码：6758-6769 , 文章类型： Article，,卷期：2012年20-22] Transition-state analogue inhibitors, immucillins, were reported to bind to trimeric purine nucleoside phosphorylase (PNP) with the stoichiometry of one molecule per enzyme trimer [ Miles, R. W.; Tyler, P. C.; Furneaux, ... Targeting conserved water molecules: Design of 4-aryl-5-cyanopyrrolo[2,3-d]pyrimidine Hsp90 inhibitors using fragment-based screening and structure-based optimization [作者：DAVIES NICHOLAS G M; BROWNE HELEN; DAVIS BEN; DRYSDALE MARTIN J; FOLOPPE NICOLAS; GEOFFREY STEPHANIE; GIBBONS BEN; HART TERANCE; HUBBARD RODERICK; JENSEN MICHAEL RUGAARD; MANSELL HOWARD; MASSEY ANDREW; MATASSOVA NATALIA; MOORE JONATHAN D; MURRAY JAMES; PRATT ROBERT; RAY STUART; ROBERTSON ALAN; ROUGHLEY STEPHEN D; SCHOEPFER JOSEPH; SCRIVEN KIRSTEN; SIMMONITE HEATHER; STOKES STEPHEN; SURGENOR ALLAN; WEBB PAUL; WOOD MIKE; WRIGHT LISA; BROUGH PAUL,期刊：Bioorganic & Medicinal Chemistry, 页码：6770-6789 , 文章类型： Article，,卷期：2012年20-22] Inhibitors of the Hsp90 molecular chaperone are showing promise as anti-cancer agents. Here we describe a series of 4-aryl-5-cyanopyrrolo[2,3-d]pyrimidine ATP competitive Hsp90 inhibitors that were identified following s... Synthesis and structure-activity relationship of berberine analogues in LDLR up-regulation and AMPK activation [作者：WANG YANXIANG; KONG WEIJIA; LI YINGHONG; TANG SHENG; LI ZHENG; LI YANGBIAO; SHAN YONGQIANG; BI CHONGWEN; JIANG JIANDONG; SONG DANQING,期刊：Bioorganic & Medicinal Chemistry, 页码：6552-6558 , 文章类型： Article，,卷期：2012年20-22] Currently there is no approved medicine for the treatment of metabolic syndrome. A series of new derivatives of berberine (BBR) or pseudoberberine (1) was synthesized and evaluated for their activity on AMP-activated pro... Synthesis and structure-activity relationships of 8-substituted-2-aryl-5-alkylaminoquinolines: Potent, orally active corticotropin-releasing factor-1 receptor antagonists [作者：TAKEDA KUNITOSHI; TERAUCHI TARO; HASHIZUME MINAKO; SHIKATA KOHDOH; TAGUCHI RYOTA; MURATATAI KAORU; FUJISAWA MASAE; TAKAHASHI YOSHINORI; SHIN KOGYOKU; INO MITSUHIRO; SHIBATA HISASHI; YONAGA MASAHIRO,期刊：Bioorganic & Medicinal Chemistry, 页码：6559-6578 , 文章类型： Article，,卷期：2012年20-22] We previously reported a series of 8-methyl-2-aryl-5-alkylaminoquinolines as a novel class of corticotropin-releasing factor-1 (CRF1) receptor antagonists. A critical issue encountered for this series of compounds was lo... Rapid biochemical synthesis of C-11-labeled single chain variable fragment antibody for immuno-PET by cell-free protein synthesis [作者：MATSUDA TAKAYOSHI; FURUMOTO SHOZO; HIGUCHI KAE; YOKOYAMA JUN; ZHANG MINGRONG; YANAI KAZUHIKO; IWATA REN; KIGAWA TAKANORI,期刊：Bioorganic & Medicinal Chemistry, 页码：6579-6582 , 文章类型： Article，,卷期：2012年20-22] Immuno-PET is a promising approach for improved cancer diagnosis, by taking advantage of the high specificity of antibodies. Here, we present a novel cell-free protein synthesis method for preparing a positron emitter la... Molybdophyllysin, a toxic metalloendopeptidase from the tropical toadstool, Chlorophyllum molybdites [作者：YAMADA MINA; TOKUMITSU NAOKO; SAIKAWA YOKO; NAKATA MASAYA; ASANO JUNPEI; MIYAIRI KAZUO; OKUNO TOSHIKATSU; KONNO KATSUHIRO; HASHIMOTO KIMIKO,期刊：Bioorganic & Medicinal Chemistry, 页码：6583-6588 , 文章类型： Article，,卷期：2012年20-22] A toxic protein, dubbed molybdophyllysin, was isolated from the tropical toadstool Chlorophyllum molybdites by following its lethal effect in mice. Analysis of the protein using SDS-PAGE revealed a single 23-kDa band. Se... Synthesis of new antimicrobial pyrrolo[2,1-a]isoquinolin-3-ones [作者：MORENO LAURA; PARRAGA JAVIER; GALAN ABRAHAM; CABEDO NURIA; PRIMO JAIME; CORTES DIEGO,期刊：Bioorganic & Medicinal Chemistry, 页码：6589-6597 , 文章类型： Article，,卷期：2012年20-22] The attractive structure of the pyrroloisoquinoline moiety, together with its potential antimicrobial activity, encouraged us to prepare six 8-substituted and seven 8,9-disubstituted-1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]... Structure-activity relationship studies of 4-benzyl-1H-pyrazol-3-yl beta-D-glucopyranoside derivatives as potent and selective sodium glucose co-transporter 1 (SGLT1) inhibitors with therapeutic activity on postprandial hyperglycemia [作者：FUSHIMI NOBUHIKO; FUJIKURA HIDEKI; SHIOHARA HIROAKI; TERANISHI HIROTAKA; SHIMIZU KAZUO; YONEKUBO SHIGERU; OHNO KOHSUKE; MIYAGI TAKASHI; ITOH FUMIAKI; SHIBAZAKI TOSHIHIDE; TOMAE MASAKI; ISHIKAWATAKEMURA YUKIKO; NAKABAYASHI TAKESHI; KAMADA NOBORU; OZAWA TOMONAGA; KOBAYASHI SUSUMU; ISAJI MASAYUKI,期刊：Bioorganic & Medicinal Chemistry, 页码：6598-6612 , 文章类型： Article，,卷期：2012年20-22] Sodium glucose co-transporter 1 (SGLT1) plays a dominant role in the absorption of glucose in the gut and is considered a promising target in the development of treatments for postprandial hyperglycemia. A series of 4-be... 4-Isoxazolyl-1,4-dihydropyridines exhibit binding at the multidrug-resistance transporter [作者：HULUBEI VICTORIA; MEIKRANTZ SCOTT B; QUINCY DAVID A; HOULE TINA; MCKENNA JOHN I; ROGERS MARK E; STEIGER SCOTT; NATALE N R,期刊：Bioorganic & Medicinal Chemistry, 页码：6613-6620 , 文章类型： Article，,卷期：2012年20-22] The 4-isoxazolyl-dihydropyridines (IDHPs) exhibit inhibition of the multidrug-resistance transporter (MDR-1), and exhibit an SAR distinct from their activity at voltage gated calcium channels (VGCC). Among the four most ... Effect of adenosine modified with a boron cluster pharmacophore on reactive oxygen species production by human neutrophils [作者：BEDNARSKA KATARZYNA; OLEJNICZAK AGNIESZKA B; PISKALA AGNIESZKA; KLINK MAGDALENA; SULOWSKA ZOFIA; LESNIKOWSKI ZBIGNIEW J,期刊：Bioorganic & Medicinal Chemistry, 页码：6621-6629 , 文章类型： Article，,卷期：2012年20-22] Methods for the synthesis of adenosine/boron cluster conjugates are proposed and the potential of the obtained derivatives to modulate neutrophil activity, especially reactive oxygen species (ROS) production in vitro, is... Benzimidazole inhibitors of the protein kinase CHK2: Clarification of the binding mode by flexible side chain docking and protein-ligand crystallography [作者：MATIJSSEN CORNELIS; SILVASANTISTEBAN M CRIS; WESTWOOD ISAAC M; SIDDIQUE SAMERENE; CHOI VANESSA; SHELDRAKE PETER; VAN MONTFORT ROB L M; BLAGG JULIAN,期刊：Bioorganic & Medicinal Chemistry, 页码：6630-6639 , 文章类型： Article，,卷期：2012年20-22] Two closely related binding modes have previously been proposed for the ATP-competitive benzimidazole class of checkpoint kinase 2 (CHK2) inhibitors; however, neither binding mode is entirely consistent with the reported... Sulfonates-PMMA nanoparticles conjugates: A versatile system for multimodal application [作者：MONASTEROLO CLAUDIO; BALLESTRI MARCO; SOTGIU GIOVANNA; GUERRINI ANDREA; DAMBRUOSO PAOLO; SPARNACCI KATIA; LAUS MICHELE; DE CESARE MICHELANDREA; PISTONE ASSUNTA; BERETTA GIOVANNI LUCA; ZUNINO FRANCO; BENFENATI VALENTINA; VARCHI GRETA,期刊：Bioorganic & Medicinal Chemistry, 页码：6640-6647 , 文章类型： Article，,卷期：2012年20-22] We report herein the viability of a novel nanoparticles (NPs) conjugated system, namely the attachment, based on ionic and hydrophobic interactions, of different sulfonated organic salts to positively charged poly(methyl... Synthesis, biological evaluation and molecular modeling of dihydro-pyrazolyl-thiazolinone derivatives as potential COX-2 inhibitors [作者：QIU KEMING; YAN RU; XING MAN; WANG HAIHONG; CUI HONGEN; GONG HAIBIN; ZHU HAILIANG,期刊：Bioorganic & Medicinal Chemistry, 页码：6648-6654 , 文章类型： Article，,卷期：2012年20-22] A series of dihydro-pyrazolyl-thiazolinone derivatives (5a-5t) have been synthesized and their biological activities were also evaluated as potential cyclooxygenase-2 (COX-2) inhibitors. Among these compounds, compound 2... Clarifying the structure of granadaene: Total synthesis of related analogue [2]-granadaene and confirmation of its absolute stereochemistry [作者：PARADAS MIGUEL; JURADO ROCIO; HAIDOUR ALI; RODRIGUEZ GRANGER JAVIER; SAMPEDRO MARTINEZ ANTONIO; DE LA ROSA FRAILE MANUEL; ROBLES RAFAEL; JUSTICIA JOSE; CUERVA JUAN M,期刊：Bioorganic & Medicinal Chemistry, 页码：6655-6661 , 文章类型： Article，,卷期：2012年20-22] Streptococcus agalactiae is an important agent in the infection of neonates in the first world. One of the most extended methods for its identification is based on the detection of a characteristic red pigment in the pat... SAR studies of epoxycurcuphenol derivatives on leukemia CT-CD4 cells [作者：GALINDO JOSE L G; MACIAS MARIOLA; MOLINILLO JOSE M G; MUNOZSUANO ALBA; TORRES ASCENSION; VARELA ROSA M; GARCIACOZAR FRANCISCO; MACIAS FRANCISCO A,期刊：Bioorganic & Medicinal Chemistry, 页码：6662-6668 , 文章类型： Article，,卷期：2012年20-22] Bioactive natural products are a potential source of new pharmaceuticals since they offer new modes of action and more specific activities. The use of derivatization also enables the optimal structure for their biologica...