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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   Design and synthesis of de novo cytotoxic alkaloids by mimicking the bioactive conformation of palitaxel [作者：SUN LIANG; VEITH JEAN M; PERA PAULA; BERNACKI RALPH J; OJIMA IWAO,期刊：Bioorganic & Medicinal Chemistry, 页码：7101-7112 , 文章类型： Article，,卷期：2010年18-19] Novel paclitaxel-mimicking alkaloids were designed and synthesized based on a bioactive conformation of paclitaxel, that is, REDOR-Taxol. The alkaloid 2 bearing a 5-7-6 tricyclic scaffold mimics REDOR-Taxol best among th... Thieno[3,2-c]pyrazoles: A novel class of Aurora inhibitors with favorable antitumor activity [作者：BINDI SIMONA; FANCELLI DANIELE; ALLI CRISTINA; BERTA DANIELA; BERTRAND JAY A; CAMERON ALEXANDER D; CAPPELLA PAOLO; CARPINELLI PATRIZIA; CERVI GIOVANNI; CROCI VALTER; DANELLO MATTEO; FORTE BARBARA; GIORGINI M LAURA; MARSIGLIO AURELIO; MOLL JUERGEN; PESENTI ENRICO; PITTALA VALERIA; PULICI MAURIZIO; RICCARDISIRTORI FEDERICO; ROLETTO FULVIA; SONCINI CHIARA; STORICI PAOLA; VARASI MARIO; VOLPI DANIELE; ZUGNONI PAOLA; VIANELLO PAOLA,期刊：Bioorganic & Medicinal Chemistry, 页码：7113-7120 , 文章类型： Article，,卷期：2010年18-19] A novel series of 3-amino-1H-thieno[3,2-c] pyrazole derivatives demonstrating high potency in inhibiting Aurora kinases was developed. Here we describe the synthesis and a preliminary structure-activity relationship, whi... Development of a plate-based scintillation proximity assay for the mycobacterial AftB enzyme involved in cell wall arabinan biosynthesis [作者：ZHANG JIAN; AMIN ANITA G; HOELEMANN ALEXANDRA; SEEBERGER PETER H; CHATTERJEE DELPHI,期刊：Bioorganic & Medicinal Chemistry, 页码：7121-7131 , 文章类型： Article，,卷期：2010年18-19] A number of mycobacterial arabinosyltransferases, such as the Emb proteins, AftA, AftB, AftC, and AftD have been characterized and implicated to be involved in the cell wall arabinan assembly. These arabinosyltransferase... Synthesis and biological activities of new di- and trimeric quinoline derivatives [作者：BROCH SIDONIE; HENON HELENE; DEBAUD ANNELAURE; FOGERON MARIELAURE; BONNEFOYBERARD NATHALIE; ANIZON FABRICE; MOREAU PASCALE,期刊：Bioorganic & Medicinal Chemistry, 页码：7132-7143 , 文章类型： Article，,卷期：2010年18-19] The synthesis of non-peptidic helix mimetics based on a trimeric quinoline scaffold is described. The ability of these new compounds, as well as their synthetic dimeric intermediates, to bind to various members of the Bc... Thioether benzenesulfonamide inhibitors of carbonic anhydrases II and IV: Structure-based drug design, synthesis, and biological evaluation (vol 18, pg 3307, 2010) [作者：VERNIER WILLIAM F; CHONG WESLEY K M; REWOLINSKI DAVID A; GREASLEY SAMANTHA E; PAULY THOMAS A; SHAW MORENA N; DINH DAC M; FERRE ROSE ANN A; MEADOR JAMES W III; NUKUI SEIJI; ORNELAS MARTHA A; PAZ ROBERT L; REYNER ERIC L,期刊：Bioorganic & Medicinal Chemistry, 页码：7144-7144 , 文章类型： Correction，,卷期：2010年18-19] 20-Aminosteroids as a novel class of selective and complete androgen receptor antagonists and inhibitors of prostate cancer cell growth [作者：FOUSTERIS MANOLIS A; SCHUBERT UNDINE; ROELL DANIELA; ROEDIGER JULIA; BAILIS NIKOLAOS; NIKOLAROPOULOS SOTIRIS S; BANIAHMAD ARIA; GIANNIS ATHANASSIOS,期刊：Bioorganic & Medicinal Chemistry, 页码：6960-6969 , 文章类型： Article，,卷期：2010年18-19] Here, the synthesis and the evaluation of novel 20-aminosteroids on androgen receptor (AR) activity is reported. Compounds 11 and 18 of the series inhibit both the wild type and the T877A mutant AR-mediated transactivati... Synthesis and biological evaluation of diastereoisomerically pure N,O-nucleosides [作者：BORTOLINI OLGA; DE NINO ANTONIO; ELISEO TOMMASO; GAVIOLI RICCARDO; MAIUOLO LOREDANA; RUSSO BEATRICE; SFORZA FABIO,期刊：Bioorganic & Medicinal Chemistry, 页码：6970-6976 , 文章类型： Article，,卷期：2010年18-19] Several N,O-nucleosides have been synthesized in good yields by direct 1,3-dipolar cyclization methodology, in the absence of solvent. A remarkable cis stereoselectivity (de 98%) was observed by tuning the substituents o... Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib [作者：MANLEY PAUL W; STIEFL NIKOLAUS; COWANJACOB SANDRA W; KAUFMAN SUSAN; MESTAN JUERGEN; WARTMANN MARKUS; WIESMANN MARION; WOODMAN RICHARD; GALLAGHER NEIL,期刊：Bioorganic & Medicinal Chemistry, 页码：6977-6986 , 文章类型： Article，,卷期：2010年18-19] Although orphan drug applications required by the EMEA must include assessments of similarity to preexisting products, these can be difficult to quantify. Here we illustrate a paradigm in comparing nilotinib to the proto... Identification of small molecule inhibitors of telomerase activity through transcriptional regulation of hTERT and calcium induction pathway in human lung adenocarcinoma A549 cells [作者：RAO YERRA KOTESWARA; KAO TEYU; WU MINGFANG; KO JIUNNLIANG; TZENG YEWMIN,期刊：Bioorganic & Medicinal Chemistry, 页码：6987-6994 , 文章类型： Article，,卷期：2010年18-19] High telomerase activity (TA) is detected in most cancer cells; and thus, TA inhibition by drug or dietary food components is a new strategy for cancer prevention. In this report, we examined the effects of fourteen natu... Gentisides C-K: Nine new neuritogenic compounds from the traditional Chinese medicine Gentiana rigescens Franch [作者：GAO LIJUAN; XIANG LAN; LUO YAN; WANG GUANGFA; LI JINYOU; QI JIANHUA,期刊：Bioorganic & Medicinal Chemistry, 页码：6995-7000 , 文章类型： Article，,卷期：2010年18-19] Nine new alkyl 2,3-dihydroxybenzoates, gentisides C-K, were isolated from the traditional Chinese medicine Gentiana rigescens Franch. Their structures and stereochemistry were elucidated by spectroscopic methods, and com... Identification of organoselenium compounds that possess chemopreventive properties in human prostate cancer LNCaP cells [作者：TERAZAWA RIYAKO; GARUD DINESH R; HAMADA NANAKO; FUJITA YASUNORI; ITOH TOMOHIRO; NOZAWA YOSHINORI; NAKANE KEITA; DEGUCHI TAKASHI; KOKETSU MAMORU; ITO MASAFUMI,期刊：Bioorganic & Medicinal Chemistry, 页码：7001-7008 , 文章类型： Article，,卷期：2010年18-19] The process of cancer development consists of three sequential stages termed initiation, promotion, and progression. Oxidative stress damages DNA and introduces mutations into oncogenes or tumor suppressor genes, thus co... Synthesis, anti-fungal and 1,3-beta-D-glucan synthase inhibitory activities of caffeic and quinic acid derivatives [作者：MA CHAOMEI; ABE TAKASHI; KOMIYAMA TADAZUMI; WANG WEI; HATTORI MASAO; DANESHTALAB MOHSEN,期刊：Bioorganic & Medicinal Chemistry, 页码：7009-7014 , 文章类型： Article，,卷期：2010年18-19] New derivatives of caffeic acid and quinic acid were synthesized and their anti-fungal and inhibitory activities on fungal 1,3-beta-glucan synthase were determined in comparison with those of the corresponding chlorogeni... Design, synthesis, and binding of homologated truncated 4 '-thioadenosine derivatives at the human A(3) adenosine receptors [作者：LEE HYUK WOO; KIM HEA OK; CHOI WON JUN; CHOI SUN; LEE JIN HEE; PARK SEULGI; YOO LENA; JACOBSON KENNETH A; JEONG LAK SHIN,期刊：Bioorganic & Medicinal Chemistry, 页码：7015-7021 , 文章类型： Article，,卷期：2010年18-19] We synthesized homologated truncated 4'-thioadenosine analogues 3 in which a methylene (CH2) group was inserted in place of the glycosidic bond of a potent and selective A(3) adenosine receptor antagonist 2. The analogue... Retinobenzaldehydes as proper-trafficking inducers of folding-defective P23H rhodopsin mutant responsible for Retinitis Pigmentosa [作者：OHGANE KENJI; DODO KOSUKE; HASHIMOTO YUICHI,期刊：Bioorganic & Medicinal Chemistry, 页码：7022-7028 , 文章类型： Article，,卷期：2010年18-19] The Retinitis pigmentosa (RP)-causing mutant of rhodopsin, P23H rhodopsin, is folding-defective and unable to traffic beyond the endoplasmic reticulum (ER). This ER retention, and in some cases aggregation, are proposed ... Delphinidin, a dietary anthocyanidin in berry fruits, inhibits human glyoxalase I [作者：TAKASAWA RYOKO; SAEKI KAZUNORI; TAO AKINOBU; YOSHIMORI ATSUSHI; UCHIRO HIROMI; FUJIWARA MUTSUNORI; TANUMA SEIICHI,期刊：Bioorganic & Medicinal Chemistry, 页码：7029-7033 , 文章类型： Article，,卷期：2010年18-19] Glyoxalase I (GLO I) is the rate-limiting enzyme for detoxification of methylglyoxal (MG), a side-product of glycolysis, which is able to induce apoptosis. Since GLO I is known to be highly expressed in the most tumor ce... A fluorescein-containing, small-molecule, water-soluble receptor for cytosine free bases [作者：JIANG YU LIN; PATEL PUNEET; KLEIN SUZANE M,期刊：Bioorganic & Medicinal Chemistry, 页码：7034-7042 , 文章类型： Article，,卷期：2010年18-19] In this study, we synthesized small-molecule, water-soluble, fluorescein-containing ureido compounds 6 and 8 as target receptors for cytosine free bases and then investigated the binding of cytosine free bases with the r...