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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85条记录   Triaryl (Z)-olefins suitable for radiolabeling with carbon-11 or fluorine-18 radionuclides for positron emission tomography imaging of cyclooxygenase-2 expression in pathological disease [作者：Abdellatif, KRA; Velazquez, CA; Huang, ZJ; Chowdhury, MA; Knaus, EE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5245-5250 , 文章类型： Article，,卷期：2010年20-17] A group of (Z)-1,1-diphenyl-2-(4-methylsulfonylphenyl) alk-1-enes were synthesized using methodologies that will allow incorporation of a [C-11] OCH3 substituent at the para-position of the C-1 phenyl ring, a [C-11] SO2C... Assessing the ability of a short fluorinated antifreeze glycopeptide and a fluorinated carbohydrate derivative to inhibit ice recrystallization [作者：Chaytor, JL; Ben, RN,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5251-5254 , 文章类型： Article，,卷期：2010年20-17] A short fluorinated antifreeze glycopeptide (2) was synthesized and evaluated for ice recrystallization inhibition (IRI) activity. The activity of 2 was compared to native biological antifreeze AFGP 8 and a rationally de... Synthesis and antituberculosis activity of new fatty acid amides [作者：D'Oca, CDM; Coelho, T; Marinho, TG; Hack, CRL; Duarte, RD; da Silva, PA; D'Oca, MGM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5255-5257 , 文章类型： Article，,卷期：2010年20-17] This work reports the synthesis of new fatty acid amides from C16: 0, 18: 0, 18: 1, 18: 1 (OH), and 18: 2 fatty acids families with cyclic and acyclic amines and demonstrate for the first time the activity of these compo... A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements [作者：Jain, D; Koh, JT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5258-5261 , 文章类型： Article，,卷期：2010年20-17] Estrogen receptors (ERs) regulate gene transcription through classic estrogen response elements (EREs) as well as AP-1 responsive genes. The common SERMs Raloxifene, Tamoxifen, and ICI164384 function as ER antagonists on... Oxidative stimuli-responsive nanoprodrug of camptothecin kills glioblastoma cells [作者：Lee, BS; Nalla, AK; Stock, IR; Shear, TC; Black, KL; Yu, JS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5262-5268 , 文章类型： Article，,卷期：2010年20-17] The purpose of this study was to prepare and characterize nanometer-sized prodrug (nanoprodrug) of camptothecin. The camptothecin prodrug was synthesized using tetraethylene glycol spacer linked via carbonate bond to cam... Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists [作者：Zhong, M; Shen, W; Barr, KJ; Arbitrario, JP; Arkin, MR; Bui, M; Chen, T; Cunningham, BC; Evanchik, MJ; Hanan, EJ; Hoch, U; Huen, K; Hyde, J; Kumer, JL; Lac, T; Lawrence, CE; Martell, JR; Oslob, JD; Paulvannan, K; Prabhu, S; Silverman, JA; Wright, J; Yu, CH; Zhu, JA; Flanagan, WM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5269-5273 , 文章类型： Article，,卷期：2010年20-17] This letter describes the discovery of a novel series of tetrahydroisoquinoline (THIQ)-derived small molecules that potently inhibit both human T-cell migration and super-antigen induced T-cell activation through disrupt... Hsp90 inhibition: Elimination of shock and stress [作者：Duerfeldt, AS; Blagg, BSJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4983-4987 , 文章类型： Article，,卷期：2010年20-17] The 90 kDa heat shock proteins (Hsp90) represent a class of molecular chaperones responsible for the maturation and stabilization of many oncogenic proteins. Disrupting the ability of ATP to bind and facilitate the opera... Antimicrobial phenolic abietane diterpene from Lycopus europaeus L. (Lamiaceae) [作者：Radulovic, N; Denic, M; Stojanovic-Radic, Z,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4988-4991 , 文章类型： Article，,卷期：2010年20-17] A new acetylated highly oxygenated abietane-type diterpenoid named euroabienol was isolated in pure state from Lycopus europaeus L. (Lamiaceae) fruits and its structure elucidated through both extensive spectral and chem... Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists [作者：Lange, JHM; Attali, A; van der Neut, MAW; Wals, HC; Mulder, A; Zilaout, H; Duursma, A; van Aken, HHM; van Vliet, BJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4992-4998 , 文章类型： Article，,卷期：2010年20-17] The synthesis and SAR of 3-alkyl-4-aryl-4,5-dihydropyrazole-1-carboxamides 1-23 and 1-alkyl-5-aryl-4,5-dihydropyrazole-3-carboxamides 24-27 as two novel cannabinoid CB1 receptor agonist classes were described. The target... Synthesis of novel tetrahydroisoquinoline bronchodilators [作者：Dalence-Guzman, MF; Toftered, J; Oltner, VT; Wensbo, D; Johansson, MH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4999-5003 , 文章类型： Article，,卷期：2010年20-17] The synthesis and bronchorelaxing effects of a series of novel tetrahydroisoquinoline amides are described. The compounds were evaluated for their ability to relax LTD4 contracted isolated human small airways ex-vivo. Se... Factorizing the role of a critical leucine residue in the binding of substrate to human 20 alpha-hydroxysteroid dehydrogenase (AKR1C1): Molecular modeling and kinetic studies of the Leu308Val mutant enzyme [作者：Dhagat, U; Endo, S; Soda, M; Hara, A; El-Kabbani, O,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5274-5276 , 文章类型： Article，,卷期：2010年20-17] A comparison of the structures and kinetic properties of human 20 alpha-hydroxysteroid dehydrogenase (AKR1C1) and its mutant enzymes (Leu308Val and Leu308Ala) indicates that Leu308 is a selectivity determinant for substr... Synthesis, in vitro and in vivo evaluation of 3-arylisoquinolinamines as potent antitumor agents [作者：Yang, SH; Van, HTM; Le, TN; Khadka, DB; Cho, SH; Lee, KT; Chung, HJ; Lee, SK; Ahn, CH; Lee, YB; Cho, WJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5277-5281 , 文章类型： Article，,卷期：2010年20-17] In the search for potent water-soluble 3-arylisoquinolines, several 3-arylisoquinolinamines were designed and synthesized. Various substituted 3-arylisoquinolinamines exhibited strong cytotoxic activity against eight dif... Novel Notch-sparing gamma-secretase inhibitors derived from a peroxisome proliferator-activated receptor agonist library [作者：Kurosumi, M; Nishio, Y; Osawa, S; Kobayashi, H; Iwatsubo, T; Tomita, T; Miyachi, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5282-5285 , 文章类型： Article，,卷期：2010年20-17] Screening of our library of peroxisome proliferator-activated receptor (PPAR) agonists yielded several phenylpropanoic acid-derived gamma-secretase inhibitors (GSIs). Structure-activity relationship studies indicated tha... Biaryl substituted hydantoin compounds as TACE inhibitors [作者：Yu, WS; Tong, L; Kim, SH; Wong, MKC; Chen, L; Yang, DY; Shankar, BB; Lavey, BJ; Zhou, GW; Kosinski, A; Rizvi, R; Li, DS; Feltz, RJ; Piwinski, JJ; Rosner, KE; Shih, NY; Siddiqui, MA; Guo, ZY; Orth, P; Shah, H; Sun, J; Umland, S; Lundell, DJ; Niu, XD; Kozlowski, JA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5286-5289 , 文章类型： Article，,卷期：2010年20-17] We disclose further optimization of hydantoin TNF-alpha convertase enzyme (TACE) inhibitors. SAR with respect to the non-prime region of TACE active site was explored. A series of biaryl substituted hydantoin compounds w... The synthesis and structure-activity relationship of 4-benzimidazolyl-piperidinylcarbonyl-piperidine analogs as histamine H-3 antagonists [作者：Ting, PC; Lee, JF; Albanese, MM; Wu, J; Aslanian, R; Favreau, L; Nardo, C; Korfmacher, WA; West, RE; Williams, SM; Anthes, JC; Rivelli, MA; Corboz, MR; Hey, JA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5004-5008 , 文章类型： Article，,卷期：2010年20-17] A structure-activity relationship study of the lead piperazinylcarbonylpiperidine compound 3 resulted in the identification of 4-benzimidazolyl-piperidinylcarbonyl-piperidine 6h as a histamine-3 (H-3) receptor antagonist... Natural products-based insecticidal agents 7. Semisynthesis and insecticidal activity of novel 4 alpha-alkyloxy-2-chloropodophyllotoxin derivatives against Mythimna separata Walker in vivo [作者：Xu, H; Xiao, X; Wang, QT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5009-5012 , 文章类型： Article，,卷期：2010年20-17] In continuation of our program aimed at the discovery and development of natural products-based insecticidal agents, 16 novel 4 alpha-alkyloxy-2-chloropodophyllotoxin derivatives were semisynthesized from podophyllotoxin...