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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18条记录   The beta-Amyloid Hypothesis in Alzheimer's Disease: Seeing Is Believing [作者：KUNG HANK F,期刊：ACS Medicinal Chemistry Letters, 页码：265-267 , 文章类型： Editorial Material，,卷期：2012年3-4] Ribonuclease-Activated Cancer Prodrug [作者：ELLIS GREGORY A; MCGRATH NICHOLAS A; PALTE MICHAEL J; RAINES RONALD T,期刊：ACS Medicinal Chemistry Letters, 页码：268-272 , 文章类型： Article，,卷期：2012年3-4] Cancer chemotherapeutic agents often have a narrow therapeutic index that challenges the maintenance of a safe and effective dose. Consistent plasma concentrations of a drug can be obtained by using a timed-release prodr... Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators [作者：PELLICCIARI ROBERTO; GIOIELLO ANTIMO; SABBATINI PAOLA; VENTURONI FRANCESCO; NUTI ROBERTO; COLLIVA CAROLINA; RIZZO GIOVANNI; ADORINI LUCIANO; PRUZANSKI MARK; RODA ALDO; MACCHIARULO ANTONIO,期刊：ACS Medicinal Chemistry Letters, 页码：273-277 , 文章类型： Article，,卷期：2012年3-4] Grounding on our former 3D QSAR studies, a knowledge-based screen of natural bile acids from diverse animal species has led to the identification of avicholic acid as a selective but weak TGRS agonist. Chemical modificat... Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization [作者：DOWLING JAMES E; CHUAQUI CLAUDIO; PONTZ TIMOTHY W; LYNE PAUL D; LARSEN NICHOLAS A; BLOCK MICHAEL H; CHEN HUAWEI; SU NANCY; WU ALLAN; RUSSELL DANIEL; POLLARD HANNAH; LEE JOHN W; PENG BO; THAKUR KUMAR; YE QING; ZHANG TAO; BRASSIL PATRICK; RACICOT VICKI; BAO LARRY; DENZ CHRISTOPHER R; COOKE EMMA,期刊：ACS Medicinal Chemistry Letters, 页码：278-283 , 文章类型： Article，,卷期：2012年3-4] In this paper we describe a series of 3-cyano-5-aryl-7-aminopyrazolo[1,5-a]-pyrimidine hits identified by kinase-focused subset screening as starting points for the structure-based design of conformationally constrained ... Type 1 Phototherapeutic Agents. 2. Cancer Cell Viability and ESR Studies of Tricyclic Diarylamines [作者：RAJAGOPALAN RAGHAVAN; LIN TIENSUNG; KARWA AMOLKUMAR S; POREDDY AMRUTA R; ASMELASH BETHEL; DORSHOW RICHARD B,期刊：ACS Medicinal Chemistry Letters, 页码：284-288 , 文章类型： Article，,卷期：2012年3-4] Type 1 phototherapeutic agents based on diarylamines were assessed for free radical generation and evaluated in vitro for cell death efficacy in the U937 leukemia cancer cell line. All of the compounds were found to prod... Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst(3) Antagonist [作者：PASTERNAK ALEXANDER; FENG ZHE; DE JESUS REYNALDA; YE ZHIXIONG; HE SHUWEN; DOBBELAAR PETER; BRADLEY SCOTT A; CHICCHI GARY G; TSAO KWEILAN; TRUSCA DORINA; EIERMANN GEORGE J; LI CAI; FENG YUE; WU MARGARET; SHAO QING; ZHANG BEI B; NARGUND RAVI; MILLS SANDER G; HOWARD ANDREW D; YANG LIHU; ZHOU YUNPING,期刊：ACS Medicinal Chemistry Letters, 页码：289-293 , 文章类型： Article，,卷期：2012年3-4] This letter provides the first pharmacological proof of principle that the sst(3) receptor mediates glucose-stimulated insulin secretion (GSIS) from pancreatic beta-cells. To enable these studies, we identified the selec... Dual-Specificity Phosphatase CDC25A/B Inhibitor Identified from a Focused Library with Nonelectrophilic Core Structure [作者：TSUCHIYA AYAKO; HIRAI GO; KOYAMA YUSUKE; OONUMA KANA; OTANI YUKO; OSADA HIROYUKI; SODEOKA MIKIKO,期刊：ACS Medicinal Chemistry Letters, 页码：294-298 , 文章类型： Article，,卷期：2012年3-4] Focused libraries of enamine derivatives with a nonacidic, nonelectrophilic core structure were screened for inhibitors of dual-specificity protein phosphatases, and an o-hydroxybenzyl derivative RE44 (10d) was identifie... Heteronuclear Gd-Tc-99m Complex of DTPA-Bis(histidylamide) Conjugate as a Bimodal MR/SPECT Imaging Probe [作者：PARK JIAE; KIM JUNG YOUNG; KIM HEEKYUNG; LEE WONHO; LIM SANG MOO; CHANG YONGMIN; KIM TAEJEONG; KIM KYEONG MIN,期刊：ACS Medicinal Chemistry Letters, 页码：299-302 , 文章类型： Article，,卷期：2012年3-4] The work describes the synthesis and in vivo application of heterotrimetallic complexes of the type {Gd(H2O)[(M(H2O)-(CO)(3))(2)(1)]} {1 = DTPA-bis(histidyl-amide); M = Re (3a); Tc-99m (3b)} for dual modality MR/SPECT im... An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus [作者：FEIL SUSANNE C; HAMILTON STEPHANIE; KRIPPNER GUY Y; LIN BO; LUTTICK ANGELA; MCCONNELL DARRYL B; NEARN ROLAND; PARKER MICHAEL W; RYAN JANE; STANISLAWSKI PAULINE C; TUCKER SIMON P; WATSON KEITH G; MORTON CRAIG J,期刊：ACS Medicinal Chemistry Letters, 页码：303-307 , 文章类型： Article，,卷期：2012年3-4] Respiratory infections caused by human rhinovirus are responsible for severe exacerbations of underlying clinical conditions such as asthma in addition to their economic cost in terms of lost working days due to illness.... Analysis of Flexibility and Hotspots in Bcl-xL and Mcl-1 Proteins for the Design of Selective Small-Molecule Inhibitors [作者：YANG CHAOYIE; WANG SHAOMENG,期刊：ACS Medicinal Chemistry Letters, 页码：308-312 , 文章类型： Article，,卷期：2012年3-4] Although Bcl-xL and Mcl-1, two antideath Bcl-2 members, have similar, flexible binding sites, they can achieve high binding selectivity to endogenous binding partners and synthetic small-molecule inhibitors. Here, we emp... Triazole Appending Agent (TAAG): A New Synthon for Preparing Iodine-Based Molecular Imaging and Radiotherapy Agents [作者：DARWISH ALLA; BLACKER MEGAN; JANZEN NANCY; RATHMANN STEPHANIE M; CZORNY SHANNON; HILLIER SHAWN M; JOYAL JOHN L; BABICH JOHN W; VALLIANT JOHN F,期刊：ACS Medicinal Chemistry Letters, 页码：313-316 , 文章类型： Article，,卷期：2012年3-4] A new prosthetic group referred to as the triazole appending agent (TAAG) was developed as a means to prepare targeted radioiodine-based molecular imaging and therapy agents. Tributyltin-TAAG and the fluorous analogue we... Discovery and Structural Modification of 1-Phenyl-3-(1-phenylethyl)urea Derivatives as Inhibitors of Complement [作者：ZHANG MEI; YANG XIAOYING; TANG WEI; GROENEVELD TOM W L; HE PEILAN; ZHU FENGHUA; LI JIA; LU WEI; BLOM ANNA M; ZUO JIANPING; NAN FAJUN,期刊：ACS Medicinal Chemistry Letters, 页码：317-321 , 文章类型： Article，,卷期：2012年3-4] A series of 1-phenyl-3-(1-phenylethyl)urea derivatives were identified as novel and potent complement inhibitors through structural modification of the original compound from high-throughput screening. Various analogues ... Missing Fragments: Detecting Cooperative Binding in Fragment-Based Drug Design [作者：NAIR PRAMOD C; MALDE ALPESHKUMAR K; DRINKWATER NYSSA; MARK ALAN E,期刊：ACS Medicinal Chemistry Letters, 页码：322-326 , 文章类型： Article，,卷期：2012年3-4] The aim of fragment-based drug design (FBDD) is to identify molecular fragments that bind to alternate subsites within a given binding pocket leading to cooperative binding when linked. In this study, the binding of frag... 3-Arylcoumarin Derivatives Manifest Anti-proliferative Activity through Hsp90 Inhibition [作者：ZHAO HUIPING; YAN BIN; PETERSON LAURA B; BLAGG BRIAN S J,期刊：ACS Medicinal Chemistry Letters, 页码：327-331 , 文章类型： Article，,卷期：2012年3-4] The potential therapeutic benefits associated with Hsp90 modulation for the treatment of cancer and neurodegenerative diseases highlight the importance of identifying novel Hsp90 scaffolds. KU-398, a novobiocin analogue,... Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor [作者：HARPER STEVEN; MCCAULEY JOHN A; RUDD MICHAEL T; FERRARA MARCO; DIFILIPPO MARCELLO; CRESCENZI BENEDETTA; KOCH UWE; PETROCCHI ALESSIA; HOLLOWAY M KATHARINE; BUTCHER JOHN W; ROMANO JOSEPH J; BUSH KIMBERLY J; GILBERT KEVIN F; MCINTYRE CHARLES J; NGUYEN KEVIN T; NIZI EMANUELA; CARROLL STEVEN S; LUDMERER STEVEN W; BURLEIN CHRISTINE; DIMUZIO JILLIAN M; GRAHAM DONALD J; MCHALE CAROLYN M; STAHLHUT MARK W; OLSEN DAVID B; MONTEAGUDO EDITH; CIANETTI SIMONA; GIULIANO CLAUDIO; PUCCI VINCENZO; TRAINOR NICOLE; FANDOZZI CHRISTINE M; ROWLEY MICHAEL; COLEMAN PAUL J; VACCA JOSEPH P; SUMMA VINCENZO; LIVERTON NIGEL J,期刊：ACS Medicinal Chemistry Letters, 页码：332-336 , 文章类型： Article，,卷期：2012年3-4] A new class of HCV NS3/4a protease inhibitors containing a P2 to P4 macrocyclic constraint was designed using a molecular modeling-derived strategy. Building on the profile of previous clinical compounds and exploring th... Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine [作者：LUO GUANGLIN; CHEN LING; CONWAY CHARLES M; DENTON REX; KEAVY DEBORAH; GULIANELLO MICHAEL; HUANG YANLING; KOSTICH WALTER; LENTZ KIMBERLEY A; MERCER STEPHEN E; SCHARTMAN RICHARD; SIGNOR LAURA; BROWNING MARC; MACOR JOHN E; DUBOWCHIK GENE M,期刊：ACS Medicinal Chemistry Letters, 页码：337-341 , 文章类型： Article，,卷期：2012年3-4] Calcitonin gene-related peptide (CGRP) receptor antagonists have been clinically shown to be effective in the treatment of migraine, but identification of potent and orally bioavailable compounds has been challenging. He...