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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61条记录   Activation and inhibition of leukotriene A(4) hydrolase aminopeptidase activity by diphenyl ether and derivatives [作者：Jiang, XL; Zhou, L; Wei, DG; Meng, H; Liu, Y; Lai, LH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6549-6552 , 文章类型： Article，,卷期：2008年18-24] The synthesis and biological evaluation of a series of diphenyl ether derivatives were described. The compounds can either activate or inhibit the aminopeptidase activity of leukotriene A(4) hydrolase, while at the same ... Synthesis of trans-caffeate analogues and their bioactivities against HIV-1 integrase and cancer cell lines [作者：Xia, CN; Li, HB; Liu, F; Hu, WX,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6553-6557 , 文章类型： Article，,卷期：2008年18-24] Forty caffeate analogues were synthesized via a convenient method starting from vanillin with moderate to good yields. The testing of biological activity of these compounds against HIV-1 integrase indicates that four com... A micellar prodrug of paclitaxel conjugated to cyclotriphosphazene [作者：Jun, YJ; Min, JH; Ji, DE; Yoo, JH; Kim, JH; Lee, HJ; Jeong, B; Sohn, YS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6410-6413 , 文章类型： Article，,卷期：2008年18-24] A novel water soluble and biodegradable cyclotriphosphazene-paclitaxel conjugate was prepared by reacting 2'-succinyl paclitaxel with cyclotriphosphazenes bearing equimolar glycyl-L-lysine and methoxy poly(ethylene glyco... Cytotoxic bromotyrosine derivatives from a two-sponge association of Jaspis sp and Poecillastra sp. [作者：Shinde, PB; Lee, YM; Dang, HT; Hong, J; Lee, CO; Jung, JH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6414-6418 , 文章类型： Article，,卷期：2008年18-24] Bioassay-guided chemical investigation of the lipophilic extract of a two-sponge association (Jaspis sp. and Poecillastra sp.) led to the isolation of two new bromotyrosine derivatives (1 and 2), along with known derivat... Design, synthesis, and evaluation of orally active inhibitors of plasminogen activator inhibitor-1 (PAI-1) production [作者：Miyazaki, H; Ogiku, T; Sai, H; Ohmizu, H; Murakami, J; Ohtani, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6419-6422 , 文章类型： Article，,卷期：2008年18-24] A novel series of butadiene-imide 1 (T-686) derivatives having an inhibitory activity against PAI-1 production was synthesized and evaluated their biological activities and DMPK profiles, in which 15k (T-2639) was select... Identification of small molecule agonists of the motilin receptor [作者：Heightman, TD; Conway, E; Corbett, DF; Macdonald, GJ; Stemp, G; Westaway, SM; Celestini, P; Gagliardi, S; Riccaboni, M; Ronzoni, S; Vaidya, K; Butler, S; Mckay, F; Muir, A; Powney, B; Winborn, K; Wise, A; Jarvie, EM; Sanger, GJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6423-6428 , 文章类型： Article，,卷期：2008年18-24] High-throughput screening resulted in the identification of a series of novel motilin receptor agonists with relatively low molecular weights. The series originated from an array of biphenyl derivatives designed to targe... The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor [作者：Westaway, SM; Brown, SL; Conway, E; Heightman, TD; Johnson, CN; Lapsley, K; Macdonald, GJ; MacPherson, DT; Mitchell, DJ; Myatt, JW; Seal, JT; Stanway, SJ; Stemp, G; Thompson, M; Celestini, P; Colombo, A; Consonni, A; Gagliardi, S; Riccaboni, M; Ronzoni, S; Briggs, MA; Matthews, KL; Stevens, AJ; Bolton, VJ; Boyfield, I; Jarvie, EM; Stratton, SC; Sanger, GJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6429-6436 , 文章类型： Article，,卷期：2008年18-24] Optimisation of urea (5), identified from high throughput screening and subsequent array chemistry, has resulted in the identification of pyridine carboxamide (33) which is a potent motilin receptor agonist possessing fa... Novel 2-imidazoles as potent, selective and CNS penetrant alpha(1A) adrenoceptor partial agonists [作者：Roberts, LR; Bryans, J; Conlon, K; McMurray, G; Stobie, A; Whitlock, GA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6437-6440 , 文章类型： Article，,卷期：2008年18-24] A novel series of central nervous system (CNS) penetrant indane 2-imidazoles have been identified as potent, partial agonists of the alpha(1A) adrenergic receptor, having good selectivity over the alpha(1B), alpha(1D) an... Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin [作者：Li, MZ; Tang, WD; Zeng, FX; Lou, LA; You, TP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6441-6443 , 文章类型： Article，,卷期：2008年18-24] A series of E-ring gamma-lactone camptothecin derivatives were synthesized by semi-synthesis via a three-step domino reaction. Their biological activity was evaluated on two types of human tumor cell lines A549 and HT-29... 2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 3: Synthesis and activity of isosteric analogs [作者：Kai, H; Morioka, Y; Koriyama, Y; Okamoto, K; Hasegawa, Y; Hattori, M; Koike, K; Chiba, H; Shinohara, S; Iwamoto, Y; Takahashi, K; Tanimoto, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6444-6447 , 文章类型： Article，,卷期：2008年18-24] Structure-activity relationships and efforts to optimize the pharmacokinetic pro. le of isosteric analogs of 2-arylimino-5,6-dihydro-4H-1,3-thiazines as cannabinoid receptor agonists are described. Among those examined, ... The effects of ascorbic acid on homolytic processes involving alpha-hydroxyl-containing carbon-centered radicals [作者：Brinkevich, SD; Shadyro, OI,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6448-6450 , 文章类型： Article，,卷期：2008年18-24] Effects of ascorbic acid and 5,6-O-isopropylidene-2,3-O-dimethylascorbic acid on final product formation in radiolysis of ethanol, aqueous solutions of ethanol, ethylene glycol, alpha-methylglycoside, maltose, alpha-glyc... Synthesis of C4-fluorinated solamins and their growth inhibitory activity against human cancer cell lines [作者：Kojima, N; Hayashi, H; Suzuki, S; Tominaga, H; Maezaki, N; Tanaka, T; Yamori, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6451-6453 , 文章类型： Article，,卷期：2008年18-24] C4-Fluorinated analogues of solamin, an antitumor acetogenin, were synthesized and investigated for their antitumor activities against 39 tumor cell lines. C4-Fluorinated solamins showed more potent growth inhibitory act... N-((8-Hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2) [作者：Gilbert, AM; Bursavich, MG; Lombardi, S; Georgiadis, KE; Reifenberg, E; Flannery, CR; Morris, EA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6454-6457 , 文章类型： Article，,卷期：2008年18-24] N-((8-Hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2) have been prepared. Selected compounds 10, 14, 25, and 53 show sub-mu M ADAMTS-5 potency and go... Design and synthesis of a bis(cycloisodityrosine) analogue of RA-VII, an antitumor bicyclic hexapeptide [作者：Lee, JE; Hitotsuyanagi, Y; Nakagawa, Y; Kato, S; Fukaya, H; Takeya, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6458-6461 , 文章类型： Article，,卷期：2008年18-24] An analogue of an antitumor bicyclic hexapeptide RA-VII was prepared, in which the Ala-2 and Tyr-3 residues of RA-VII were replaced by a cycloisodityrosine unit. In the crystalline state, the peptide backbone structures ... Synthesis and in vitro evaluation of the antifungal activities of dihydropyrimidinones [作者：Singh, OM; Singh, SJ; Devi, MB; Devi, LN; Singh, NI; Lee, SG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6462-6467 , 文章类型： Article，,卷期：2008年18-24] Copper (II) chloride in the absence of any solvent, efficiently catalyses the synthesis of dihydropyrimidinones (80-96% yields) by the Biginelli reaction. Six compounds were selected and examined their antifungal activit... Synthesis and structure-activity relationship of 7-azaindole piperidine derivatives as CCR2 antagonists [作者：Xia, MG; Hou, CF; DeMong, D; Pollack, S; Pan, M; Singer, M; Matheis, M; Murray, W; Cavender, D; Wachter, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6468-6470 , 文章类型： Article，,卷期：2008年18-24] The synthesis and structure-activity relationship of a series of 7-azaindole piperidine derivatives are described. SAR studies led to the discovery of the potent CCR2 antagonists displaying IC50 values in the nanomolar r...