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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45条记录   ppGpp analogues inhibit synthetase activity of Rel proteins from Gram-negative and Gram-positive bacteria [作者：WEXSELBLATT EZEQUIEL; KATZHENDLER JEHOSHUA; SALEEMBATCHA RASPUDIN; HANSEN GUIDO; HILGENFELD ROLF; GLASER GAD; VIDAVSKI ROEE R,期刊：Bioorganic & Medicinal Chemistry, 页码：4485-4497 , 文章类型： Article，,卷期：2010年18-12] A prominent feature of the stringent response is the accumulation of two unusual phosphorylated derivatives of GTP and GDP (pppGpp: 5'-triphosphate-3'-diphosphate, and ppGpp: 5'-3'-bis-diphosphate), collectively called (... Novel tricyclic Delta(2)-isoxazoline and 3-oxo-2-methyl-isoxazolidine derivatives: Synthesis and binding affinity at neuronal nicotinic acetylcholine receptor subtypes [作者：DALLANOCE CLELIA; FRIGERIO FABIO; MARTELLI GIULIANA; GRAZIOSO GIOVANNI; MATERA CARLO; POME DIEGO YURI; PUCCI LUCA; CLEMENTI FRANCESCO; GOTTI CECILIA; DE AMICI MARCO,期刊：Bioorganic & Medicinal Chemistry, 页码：4498-4508 , 文章类型： Article，,卷期：2010年18-12] A group of novel tricyclic Delta(2)-isoxazolines (4b, 5b, 7a-b, and 8a-b) and 3-oxo-isoxazolidines (6a-b and 9a-b), structurally related to cytisine or norferruginine, was prepared through 1,3-dipolar cycloadditions invo... Synthesis and cytotoxicity of novel indirubin-5-carboxamides [作者：CHENG XINLAI; RASQUE PAUL; VATTER SANDRA; MERZ KARLHEINZ; EISENBRAND GERHARD,期刊：Bioorganic & Medicinal Chemistry, 页码：4509-4515 , 文章类型： Article，,卷期：2010年18-12] Indirubins have been reported to act as potent inhibitors of protein kinases relevant to tumorigenesis and of tumor cell growth, but their development to antitumor drugs suffer from their poor water solubility. We synthe... Design, synthesis and biological evaluation of trans 2-(thiophen-2-yl)vinyl heteroaromatic iodides [作者：FORTUNA COSIMO G; BARRESI VINCENZA; MUSUMARRA GIUSEPPE,期刊：Bioorganic & Medicinal Chemistry, 页码：4516-4523 , 文章类型： Article，,卷期：2010年18-12] A modeling approach based on physico-chemical and pharmacokinetic properties, called Volsurf+, was used to design new trans 2-(thiophen-2-yl)vinyl heteroaromatic iodides with antiproliferative activity. The synthesis and... Synthesis and antitumor activity of 2,5-bis(3 '-indolyl)-furans and 3,5-bis(3 '-indolyl)-isoxazoles, nortopsentin analogues [作者：DIANA PATRIZIA; CARBONE ANNA; BARRAJA PAOLA; KELTER GERHARD; FIEBIG HEINZHERBERT; CIRRINCIONE GIROLAMO,期刊：Bioorganic & Medicinal Chemistry, 页码：4524-4529 , 文章类型： Article，,卷期：2010年18-12] A series of novel 2,5-bis(3'-indolyl)furans and 3,5-bis(3'-indolyl) isoxazoles were synthesized as antitumor agents. The antiproliferative activity was evaluated in vitro toward diverse human tumor cell lines. Initially ... Synthesis and in vitro antiprotozoal evaluation of substituted phenalenone analogues [作者：ROSQUETE LAURA I; CABRERASERRA M GABRIELA; PINERO JOSE E; MARTINRODRIGUEZ PATRICIA; FERNANDEZPEREZ LEANDRO; LUIS JAVIER G; MCNAUGHTONSMITH GRANT; ABADGRILLO TERESA,期刊：Bioorganic & Medicinal Chemistry, 页码：4530-4534 , 文章类型： Article，,卷期：2010年18-12] A set of derivatives encompassing structural modifications on the privileged phenalenone scaffold were assessed for their antiparasitic activities against the most clinically relevant forms of trypanosomiasis and leishma... Development of antiproliferative phenylmaleimides that activate the unfolded protein response [作者：MUUS ULRIKE; HOSE CURTIS; YAO WEI; KOSAKOWSKACHOLODY TERESA; FARNSWORTH DAVID; DYBA MARZENA; LOUNTOS GEORGE T; WAUGH DAVID S; MONKS ANNE; BURKE TERRENCE R JR; MICHEJDA CHRISTOPHER J,期刊：Bioorganic & Medicinal Chemistry, 页码：4535-4541 , 文章类型： Article，,卷期：2010年18-12] The current paper presents the synthesis and evaluation of a series of maleimides that were designed to inhibit the Cdc25 phosphatase by alkylation of catalytically essential cysteine residues. Although in HepB3 cell cul... Identification of csypyrone B1 as the novel product of Aspergillus oryzae type III polyketide synthase CsyB [作者：SESHIME YASUYO; JUVVADI PRAVEEN RAO; KITAMOTO KATSUHIKO; EBIZUKA YUTAKA; FUJII ISAO,期刊：Bioorganic & Medicinal Chemistry, 页码：4542-4546 , 文章类型： Article，,卷期：2010年18-12] As a novel superfamily of type III polyketide synthases (PKSs) in microbes, four genes, csyA, csyB, csyC, and csyD, were found in the genome of Aspergillus oryzae, an industrially important filamentous fungus. Although o... Synthesis and biological evaluation of novel (4 or 5-aryl)pyrazolyl-indoles as inhibitors of interleukin-2 inducible T-cell kinase (ITK) [作者：VELANKAR AVDHOOT D; QUINTINI GIANLUCA; PRABHU ARATI; WEBER ALEXANDER; HUNAEUS GUNDULA; VOLAND BRITTA; WUEST MONIKA; ORJEDA CHRISTIAN; HAREL DIPAK; VARGHESE SHAJI; GORE VIKAS; PATIL MEENAL; GAYKE DEEPAK; HERDEMANN MATTHIAS; HEIT ISABELLE; ZALIANI ANDREA,期刊：Bioorganic & Medicinal Chemistry, 页码：4547-4559 , 文章类型： Article，,卷期：2010年18-12] Interleukin-2 inducible T-cell kinase (ITK) is one of five kinases that belong to the Tec kinase family that plays an important role in T-cell and mast cell signaling. Various reports point to a role of ITK in the treatm... Bacterial transferase MraY inhibitors: Synthesis and biological evaluation [作者：LECERCLE DELPHINE; CLOUET ANTHONY; ALDABBAGH BAYAN; CROUVOISIER MURIEL; BOUHSS AHMED; GRAVIERPELLETIER CHRISTINE; LE MERRER YVES,期刊：Bioorganic & Medicinal Chemistry, 页码：4560-4569 , 文章类型： Article，,卷期：2010年18-12] New inhibitors of the bacterial transferase MraY are described. Their structure is based on an aminoribosyl-O-uridine like scaffold, readily obtained in two key steps. The amino group can be coupled with proline or guany... Selective angiotensin II AT(2) receptor agonists with reduced CYP 450 inhibition [作者：MAHALINGAM A K; WAN YIQIAN; MURUGAIAH A M S; WALLINDER CHARLOTTA; WU XIONGYU; PLOUFFE BIANCA; BOTROS MILAD; NYBERG FRED; HALLBERG ANDERS; GALLOPAYET NICOLE; ALTERMAN MATHIAS,期刊：Bioorganic & Medicinal Chemistry, 页码：4570-4590 , 文章类型： Article，,卷期：2010年18-12] Structural alterations to the benzylic position of the first drug-like selective angiotensin II AT(2) receptor agonist (1) have been performed, with the emphasis to reduce the CYP 450 inhibitory property of the initial s... Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2 (vol 18, pg 707, 2010) [作者：HILTON STEPHEN; NAUD SEBASTIEN; CALDWELL JOHN J; BOXALL KATHY; BURNS SAMANTHA; ANDERSON VICTORIA E; ANTONI LAURENT; ALLEN CHARLOTTE E; PEARL LAURENCE H; OLIVER ANTONY W; AHERNE G WYNNE; GARRETT MICHELLE D; COLLINS IAN,期刊：Bioorganic & Medicinal Chemistry, 页码：4591-4591 , 文章类型： Correction，,卷期：2010年18-12] Discovery of tetrahydro-beta-carbolines as inhibitors of the mitotic kinesin KSP [作者：LIU FEI; YU LIQIN; JIANG CHENG; YANG LEI; WU WUTONG; YOU QIDONG,期刊：Bioorganic & Medicinal Chemistry, 页码：4167-4177 , 文章类型： Article，,卷期：2010年18-12] Inhibitors of kinesin spindle protein (KSP) are a promising class of anticancer agents that cause mitotic arrest in cells from a failure to form functional bipolar mitotic spindles. Here, we report the synthesis and biol... A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives [作者：KABIR M SHAHJAHAN; NAMJOSHI OJAS A; VERMA RANJIT; POLANOWSKI REBECCA; KRUEGER SARAH M; SHERMAN DAVID; ROTT MARC A; SCHWAN WILLIAM R; MONTE AARON; COOK JAMES M,期刊：Bioorganic & Medicinal Chemistry, 页码：4178-4186 , 文章类型： Article，,卷期：2010年18-12] Novel acrylic acid ethyl ester derivatives were synthesized and evaluated as potential agents against Mycobacterium species. A versatile and efficient copper-catalyzed coupling process was developed and used to prepare a... New aryldithiolethione derivatives as potent histone deacetylase inhibitors [作者：TAZZARI VALERIO; CAPPELLETTI GRAZIELLA; CASAGRANDE MANOLO; PERRINO ELENA; RENZI LUIGI; DEL SOLDATO PIERO; SPARATORE ANNA,期刊：Bioorganic & Medicinal Chemistry, 页码：4187-4194 , 文章类型： Article，,卷期：2010年18-12] A series of dithiolethione derivatives was synthesized and the in vitro HDAC inhibitory activity was tested. The most active compounds, 1 and 2, exhibited an IC50 in nM range with a strong hyperacetylation of histone H4 ... (E)-2-Styrylchromones as potential anti-norovirus agents [作者：ROCHAPEREIRA JOANA; CUNHA RICARDO; PINTO DIANA C G A; SILVA ARTUR M S; NASCIMENTO MARIA SAO JOSE,期刊：Bioorganic & Medicinal Chemistry, 页码：4195-4201 , 文章类型： Article，,卷期：2010年18-12] Human noroviruses (NoV) are now recognized as the most frequent cause of outbreaks and sporadic cases of acute gastroenteritis. Despite the significant economic impact and considerable morbidity of norovirus disease, no ...