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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16条记录   Discovery of AMG 853, a CRTH2 and DP Dual Antagonist [作者：LIU JIWEN; LI ANRONG; WANG YINGCAI; JOHNSON MIKE G; SU YONGLI; SHEN WANG; WANG XUEMEI; LIVELY SARAH; BROWN MATTHEW; LAI SUJEN; GONZALEZ FELIX; DE TURISO LOPEZ; XU QINGGE; VAN LENGERICH BETTINA; SCHMITT MIKE; FU ZICE; SUN YING; LAWLIS SHANNA; SEITZ LISA; DANAO JAY; WAIT JILL; YE QIUPING; TANG HUA LUCY; GRILLO MARK; COLLINS TASSIE L; SULLIVAN TIMOTHY F; MEDINA JULIO C,期刊：ACS Medicinal Chemistry Letters, 页码：326-330 , 文章类型： Article，,卷期：2011年2-5] Prostaglandin D-2 (PGD(2)) plays a key role in mediating allergic reactions seen in asthma, allergic rhinitis, and atopic dermatitis. PGD(2) exerts its activity through two G protein coupled receptors (GPCRs), prostanoid... Discovery of 4 ''-Ether Linked Azithromycin-Quinolone Hybrid Series: Influence of the Central Linker on the Antibacterial Activity [作者：PAVLOVIC DRAZEN; MUTAK STJEPAN,期刊：ACS Medicinal Chemistry Letters, 页码：331-336 , 文章类型： Article，,卷期：2011年2-5] A series of novel C-4"-substituted azithromycins was synthesized and evaluated for in vitro antibacterial activity against a panel of representative erythromycin-susceptible and macrolide-lincosamide-streptogramin (MLS) ... Elucidation of New Binding Interactions with the Human Tsg101 Protein Using Modified HIV-1 Gag-p6 Derived Peptide Ligands [作者：KIM SUNGEUN; LIU FA; IM YOUNG JUN; STEPHEN ANDREW G; FIVASH MATTHEW J; WAHEED ABDUL A; FREED ERIC O; FISHER ROBERT J; HURLEY JAMES H; BURKE TERRENCE R,期刊：ACS Medicinal Chemistry Letters, 页码：337-341 , 文章类型： Article，,卷期：2011年2-5] Targeting protein protein interactions is gaining greater recognition as an attractive approach to therapeutic development. An example of this may be found with the human cellular protein encoded by the tumor susceptibil... Preparation, Gram-Negative Antibacterial Activity, and Hydrolytic Stability of Novel Siderophore-Conjugated Monocarbam Diols [作者：FLANAGAN MARK E; BRICKNER STEVEN J; LALL MANJINDER; CASAVANT JEFFREY; DESCHENES LAURA; FINEGAN STEVEN M; GEORGE DAVID M; GRANSKOG KARL; HARDINK JOEL R; HUBAND MICHAEL D; THUY HOANG; LAMB LUCINDA; MARRA ANDREA; MITTONFRY MARK; MUELLER JOHN P; MULLINS LISA M; NOE MARK C; ODONNELL JOHN P; PATTAVINA DAVID; PENZIEN JOSEPH B; SCHUFF BRANDON P; SUN JIANMIN; WHIPPLE DAVID A; YOUNG JENNIFER; GOOTZ THOMAS D,期刊：ACS Medicinal Chemistry Letters, 页码：385-390 , 文章类型： Article，,卷期：2011年2-5] A novel series of monocarbam compounds exhibiting promising antibacterial activity against multidrug resistant Gram-negative microorganisms is reported, along with the synthesis of one such molecule MC-1 (1). Also report... Natural Product-Based 6-Hydroxy-2,3,4,6-tetrahydropyrrolo[1, 2-a]pyrimidinium Scaffold as a New Antifungal Template [作者：LI XINGCONG; BABU K SURESH; JACOB MELISSA R; KHAN SHABANA I; AGARWAL AMEETA K; CLARK ALICE M,期刊：ACS Medicinal Chemistry Letters, 页码：391-395 , 文章类型： Article，,卷期：2011年2-5] Synthetic analogues of the marine-derived class of natural products phloeodictines have been prepared and exhibited potent in vitro fungicidal activities against a broad array of fungal pathogens including drug-resistant... Separation of Betti Reaction Product Enantiomers: Absolute Configuration and Inhibition of Botulinum Neurotoxin A [作者：CARDELLINA JOHN H II; VIEIRA REBECCA C; ECCARD VANESSA; SKERRY JANET; MONTGOMERY VICKI; CAMPBELL YVETTE; ROXASDUNCAN VIRGINIA; LEISTER WILLIAM; LECLAIR CHRISTOPHER A; MALONEY DAVID J; PADULA DANIELE; PESCITELLI GENNARO; KHAVRUTSKII ILJA; HU XIN; WALLQVIST ANDERS; SMITH LEONARD A,期刊：ACS Medicinal Chemistry Letters, 页码：396-401 , 文章类型： Article，,卷期：2011年2-5] The racemic product of the Betti reaction of 5-chloro-8-hydroxyquinoline, benzaldehyde, and 2-aminopyridine was separated by chiral HPLC to determine which enantiomer inhibited botulinurn neurotoxin serotype A. When the ... Discovery of S-Nitrosoglutathione Reductase Inhibitors: Potential Agents for the Treatment of Asthma and Other Inflammatory Diseases [作者：SUN XICHENG; WASLEY JAN W F; QIU JIAN; BLONDER JOAN P; STOUT ADAM M; GREEN LOUIS S; STRONG SARAH A; COLAGIOVANNI DOROTHY B; RICHARDS JANE P; MUTKA SARAH C; CHUN LAWRENCE; ROSENTHAL GARY J,期刊：ACS Medicinal Chemistry Letters, 页码：402-406 , 文章类型： Article，,卷期：2011年2-5] S-Nitrosoglutathione reductase (GSNOR) regulates S-nitrosothiols (SNOs) and nitric oxide (NO) in vivo through catabolism of S-nitrosoglutathione (GSNO). GSNOR and the anti-inflammatory and smooth muscle relaxant activiti... Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors [作者：WENGLOWSKY STEVE; REN LI; AHRENDT KATERI A; LAIRD ELLEN R; ALIAGAS IGNACIO; ALICKE BRUNO; BUCKMELTER ALEX J; CHOO EDNA F; DINKEL VICTORIA; FENG BAINIAN; GLOOR SUSAN L; GOULD STEPHEN E; GROSS STEFAN; GUNZNERTOSTE JANET; HANSEN JOSHUA D; HATZIVASSILIOU GEORGIA; LIU BONNIE; MALESKY KIM; MATHIEU SIMON; NEWHOUSE BRAD; RADDATZ NICHOLAS J; RAN YINGQING; RANA SUMEET; RANDOLPH NIKOLE; RISOM TYLER; RUDOLPH JOACHIM; SAVAGE SCOTT; SELBY LEANN T; SHRAG MICHAEL; SONG KYUNG; STURGIS HILLARY L; VOEGTLI WALTER C; WEN ZHAOYANG; WILLIS BRANDON S; WOESSNER RICHARD D; WU WENI; YOUNG WENDY B; GRINA JONAS,期刊：ACS Medicinal Chemistry Letters, 页码：342-347 , 文章类型： Article，,卷期：2011年2-5] The V600E mutation of B-Raf kinase results in constitutive activation of the MAPK signaling pathway and is present in approximately 7% of all cancers. Using structure-based design, a novel series of pyrazolopyridine inhi... Design, Synthesis, and Antitumor Activity of 4-Halocolchicines and Their Pro-drugs Activated by Cathepsin B [作者：YASOBU NAOKO; KITAJIMA MARIKO; KOGURE NORIYUKI; SHISHIDO YOSHIYUKI; MATSUZAKI TAKESHI; NAGAOKA MASATO; TAKAYAMA HIROMITSU,期刊：ACS Medicinal Chemistry Letters, 页码：348-352 , 文章类型： Article，,卷期：2011年2-5] Novel colchicine derivatives possessing various substituents at the C4 position were prepared. Among them, 4-halo derivatives 3-6 were found to exhibit higher activity against cancer cell lines (A549, HT29, HCT116) as we... Indomethacin Analogues that Enhance Doxorubicin Cytotoxicity in Multidrug Resistant Cells without Cox Inhibitory Activity [作者：ARISAWA MITSUHIRO; KASAYA YAYOI; OBATA TOHRU; SASAKI TAKUMA; ITO MIKA; ABE HIROSHI; ITO YOSHIHIRO; YAMANO AKIHITO; SHUTOT SATOSHI,期刊：ACS Medicinal Chemistry Letters, 页码：353-357 , 文章类型： Article，,卷期：2011年2-5] Conformationally restricted indomethacin analogues were designed and prepared from the corresponding 2-substituted indoles, which were synthesized by a one-pot isomerization/enamide-ene metathesis as the key reaction. Co... Synthesis and Biological Evaluation of JAHAs: Ferrocene-Based Histone Deacetylase Inhibitors [作者：SPENCER JOHN; AMIN JAHANGIR; WANG MINGHUA; PACKHAM GRAHAM; ALWI SHARIFAH S SYED; TIZZARD GRAHAM J; COLES SIMON J; PARANAL RONALD M; BRADNER JAMES E; HEIGHTMAN TOM D,期刊：ACS Medicinal Chemistry Letters, 页码：358-362 , 文章类型： Article，,卷期：2011年2-5] N-1-Hydroxy-N-8-ferrocenyloctanediamide, JAHA (7), an organometallic analogue of SAHA containing a ferrocenyl group as a phenyl bioisostere, displays nanomolar inhibition of class I HDACs, excellent selectivity over clas... Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1 [作者：DOW ROBERT L; LI JIANCHENG; PENCE MICHAEL P; GIBBS E MICHAEL; LAPERLE JENNIFER L; LITCHFIELD JOHN; PIOTROWSKI DAVID W; MUNCHHOF MICHAEL J; MANION TARA B; ZAVADOSKI WILLIAM J; WALKER GREGORY S; MCPHERSON R KIRK; TAPLEY SUSAN; SUGARMAN ELIOT; GUZMANPEREZ ANGEL; DASILVAJARDINE PAUL,期刊：ACS Medicinal Chemistry Letters, 页码：407-412 , 文章类型： Article，,卷期：2011年2-5] Acyl-CoA:diacylglycerol acyltransferase-1 (DGAT-1) catalyzes the final committed step in the biosynthesis of triglycerides. DGAT-1 knockout mice have been shown to be resistant to diet-induced obesity and have increased ... Bioanalytical Screening of Riboflavin Antagonists for Targeted Drug Delivery-A Thermodynamic and Kinetic Study [作者：PLANTINGA ANNA; WITTE AMANDA; LI MINGHSIN; HARMON ANDREW; CHOI SEOK KI; HOLL MARK M BANASZAK; ORR BRADFORD G; BAKER JAMES R JR; SINNIAH KUMAR,期刊：ACS Medicinal Chemistry Letters, 页码：363-367 , 文章类型： Article，,卷期：2011年2-5] The present study screened riboflavin mimicking small molecules to determine their binding activity for the riboflavin binding protein. We performed thermodynamic and kinetic binding studies of these molecules using a co... Discovery of CS-0777: A Potent, Selective, and Orally Active S1P(1) Agonist [作者：NISHI TAKAHIDE; MIYAZAKI SHOJIRO; TAKEMOTO TOSHIYASU; SUZUKI KEISUKE; IIO YUKIKO; NAKAJIMA KATSUYOSHI; OHNUKI TAKASHI; KAWASE YUMI; NARA FUTOSHI; INABA SHINICHI; IZUMI TAKASHI; YUITA HIROSHI; OSHIMA KEIKO; DOI HIROMI; INOUE RYOTAKU; TOMISATO WATARU; KAGARI TAKASHI; SHIMOZATO TAKAICHI,期刊：ACS Medicinal Chemistry Letters, 页码：368-372 , 文章类型： Article，,卷期：2011年2-5] CS-0777 (3) is phosphorylated in vivo, and the phosphate of CS-0777 (CS-0777-P) (4) acts as a selective S1P receptor-1 (S1P(1)) modulator. We report herein the synthesis of CS-0777 and CS-0777-P, pharmacological effects ... Synthetic and Immunological Studies of sTn Derivatives Carrying Substituted Phenylacetylsialic Acids as Cancer Vaccine Candidate [作者：WANG QIANLI; GUO ZHONGWU,期刊：ACS Medicinal Chemistry Letters, 页码：373-378 , 文章类型： Article，,卷期：2011年2-5] To search for effective cancer vaccines based on sTn, a sialylated tumor-associated carbohydrate antigen (sialo-TACA) expressed by a number of tumors, four unnatural N-acyl sTn derivatives, including 5'-N-p-methylphenyla... Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors [作者：DENG XIANMING; WANG JINHUA; ZHANG JIANMING; SIM TAEBO; KIM NAM DOO; SASAKI TAKAAKI; LUTHER WILLIAM II; GEORGE RANI E; JAENNE PASI A; GRAY NATHANAEL S,期刊：ACS Medicinal Chemistry Letters, 页码：379-384 , 文章类型： Article，,卷期：2011年2-5] A series of novel 3,5-diamino-1,2,4-triazole benzyl ureas was identified as having potent anaplastic lymphoma kinase (ALK) inhibition exemplified by 15a, 20a, and 23a, which exhibited antiproliferative IC50 values of 70,...