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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26条记录   Discovery of an Orally Efficacious Inhibitor of Anaplastic Lymphoma Kinase [作者：GINGRICH DIANE E; LISKO JOSEPH G; CURRY MATTHEW A; CHENG MANGENG; QUAIL MATTHEW; LU LIHUI; WAN WEIHUA; ALBOM MARK S; ANGELES THELMA S; AIMONE LISA D; HALTIWANGER R CURTIS; WELLSKNECHT KEVIN; OTT GREGORY R; GHOSE ARUP K; ATOR MARK A; RUGGERI BRUCE; DORSEY BRUCE D,期刊：Journal of Medicinal Chemistry, 页码：4580-4593 , 文章类型： Article，,卷期：2012年55-10] Anaplastic lymphoma kinase (ALK) is a promising therapeutic target for the treatment of cancer, supported by considerable favorable preclinical and clinical activities over the past several years and culminating in the r... Discovery of Novel Allosteric Mitogen-Activated Protein Kinase Kinase (MEK) 1,2 Inhibitors Possessing Bidentate Ser212 Interactions [作者：HEALD ROBERT A; JACKSON PHILIP; SAVY PASCAL; JONES MARK; GANCIA EMANUELA; BURTON BRENDA; NEWMAN RICHARD; BOGGS JASON; CHAN EMILY; CHAN JOCELYN; CHOO EDNA; MERCHANT MARK; RUDEWICZ PATRICK; ULTSCH MARK; WIESMANN CHRISTIAN; YUE QIN; BELVIN MARCIA; PRICE STEVE,期刊：Journal of Medicinal Chemistry, 页码：4594-4604 , 文章类型： Article，,卷期：2012年55-10] Using structure-based design, two novel series of highly potent biaryl amine mitogen-activated protein kinase kinase (MEK) inhibitors have been discovered. These series contain an H-bond acceptor, in a shifted position c... Disulfide Prodrugs of Albitiazolium (T3/SAR97276): Synthesis and Biological Activities [作者：CADARELLI SERGIO A; HAMEL MATTHIEU; DUCKERT JEANFREDERIC; OUATTARA MAHAMA; CALAS MICHELE; MAYNADIER MARJORIE; WEIN SHARON; PERIGAUD CHRISTIAN; PELLET ALAIN; VIAL HENRI J; PEYROTTES SUZANNE,期刊：Journal of Medicinal Chemistry, 页码：4619-4628 , 文章类型： Article，,卷期：2012年55-10] We report herein the design, synthesis, and biological screening of a series of 15 disulfide prodrugs as precursors of albitiazolium bromide (T3/SAR97276, compound 1), a choline analogue which is currently being evaluate... Novel Phosphoramidate Prodrugs of N-Acetyl-(D)-Glucosamine with Antidegenerative Activity on Bovine and Human Cartilage Explants [作者：SERPI MICHAELA; BIBBO RITA; RAT STEPHANIE; ROBERTS HELEN; HUGHES CLAIRE; CATERSON BRUCE; JOSE ALCARAZ MARIA; TORRENT GIBERT ANNA; ALAEZ VERSON CARLOS RAUL; MCGUIGAN CHRISTOPHER,期刊：Journal of Medicinal Chemistry, 页码：4629-4639 , 文章类型： Article，,卷期：2012年55-10] (D)-Glucosamine and other nutritional supplements have emerged as safe alternative therapies for osteoarthritis (OA), a chronic and degenerative articular joint disease. In our preceding paper, a series of novel O-6 phos... Discovery of the First Irreversible Small Molecule Inhibitors of the Interaction between the Vitamin D Receptor and Coactivators [作者：NANDHIKONDA PREMCHENDAR; LYNT WEN Z; MCCALLUM MEGAN M; ARA TAHNIYATH; BARANOWSKI ATHENA M; YUAN NINA Y; PEARSON DANA; BIKLE DANIEL D; GUY R KIPLIN; ARNOLD LEGGY A,期刊：Journal of Medicinal Chemistry, 页码：4640-4651 , 文章类型： Article，,卷期：2012年55-10] The vitamin D receptor (VDR) is a nuclear hormone receptor that regulates cell proliferation, cell differentiation, and calcium homeostasis. The receptor is activated by vitamin D analogues that induce the disruption of ... Ferrocenylselenoamides: Synthesis, Characterization and Cytotoxic Properties [作者：GUTIERREZHERNANDEZ ALEJANDRO I; LOPEZCORTES JOSE G; CARMEN ORTEGAALFARO M; TERESA RAMIREZAPAN M; DE JESUS CAZARESMARINERO JOSE; TOSCANO RUBEN A,期刊：Journal of Medicinal Chemistry, 页码：4652-4663 , 文章类型： Article，,卷期：2012年55-10] A new series of ferrocenyl selenoamides 7-11 (FcSeNH-(CH2)(n)CH2(R)OH, n = 1, 2, 3, R = H, Me, Ph) were prepared in good yields by selenative demetalation of Fischer aminocarbene complexes. The crystal structures of 7 [F... Design of Bcl-2 and Bcl-xL Inhibitors with Subnanomolar Binding Affinities Based upon a New Scaffold [作者：ZHOU HAIBIN; CHEN JIANFANG; MEAGHER JENNIFER L; YANG CHAOYIE; AGUILAR ANGELO; LIU LIU; BAI LONGCHUAN; GONG XIN; CAI QIAN; FANG XUELIANG; STUCKEY JEANNE A; WANG SHAOMENG,期刊：Journal of Medicinal Chemistry, 页码：4664-4682 , 文章类型： Article，,卷期：2012年55-10] Employing a structure-based strategy, we have designed a new class of potent small-molecule inhibitors of the anti-apoptotic proteins Bcl-2 and Bcl-xL. An initial lead compound with a new scaffold was designed based upon... Synthesis and Nicotinic Receptor Activity of Chemical Space Analogues of N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4-chlorobenzamide (PNU-282,987) and 1,4-Diazabicyclo[3.2.2]nonane-4-carboxylic Acid 4-Bromophenyl Ester (SSR180711) [作者：BRETHOUS LISE; GARCIADELGADO NOEMI; SCHWARTZ JULIAN; BERTRAND SONIA; BERTRAND DANIEL; REYMOND JEANLOUIS,期刊：Journal of Medicinal Chemistry, 页码：4605-4618 , 文章类型： Article，,卷期：2012年55-10] The Chemical Universe Generated Databases up to 11 atoms of CNOF (GDB-11) and up to 13 atoms of CNOClS (GDB-13) were used to enumerate analogues of the diamine part of two known alpha 7 nicotinic receptor agonists and co... Chalcogenopyrylium Compounds as Modulators of the ATP-Binding Cassette Transporters P-Glycoprotein (P-gp/ABCB1) and Multidrug Resistance Protein 1 (MRP1/ABCC1) [作者：EBERT SEAN P; WETZEL BRYAN; MYETTE ROBERT L; CONSEIL GWENAELLE; COLE SUSAN P C; SAWADA GERI A; LOO TIP W; BARTLETT M CLAIRE; CLARKE DAVID M; DETTY MICHAEL R,期刊：Journal of Medicinal Chemistry, 页码：4683-4699 , 文章类型： Article，,卷期：2012年55-10] Twenty-seven chalcogenopyrylium derivatives varying in the heteroatom of the pyrylium core and substituents at the 2-, 4-, and 6-positions were examined for their effect on human MRPI-mediated uptake of tritiated estradi... Antiadhesion Therapy for Urinary Tract Infections-A Balanced PK/PD Profile Proved To Be Key for Success [作者：JIANG XIAOHUA; ABGOTTSPON DANIELA; KLEEB SIMON; RABBANI SAID; SCHARENBERG MEIKE; WITTWER MATTHIAS; HAUG MARTINA; SCHWARDT OLIVER; ERNST BEAT,期刊：Journal of Medicinal Chemistry, 页码：4700-4713 , 文章类型： Article，,卷期：2012年55-10] The initial step for the successful establishment of urinary tract infections (UTIs), predominantly caused by uropathogenic Escherichia coli, is the adhesion of bacteria to urothelial cells. This attachment is mediated b...