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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79条记录   Pyrazolopyrimidines as dual Akt/p70S6K inhibitors [作者：Rice, KD; Kim, MH; Bussenius, J; Anand, NK; Blazey, CM; Bowles, OJ; Canne-Bannen, L; Chan, DSM; Chen, BL; Co, EW; Costanzo, S; DeFina, SC; Dubenko, L; Engst, S; Franzini, M; Huang, P; Jammalamadaka, V; Khoury, RG; Klein, RR; Laird, AD; Le, DT; Mac, MB; Matthews, DJ; Markby, D; Miller, N; Nuss, JM; Parks, JJ; Tsang, TH; Tsuhako, AL; Wang, Y; Xu, W,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2693-2697 , 文章类型： Article，,卷期：2012年22-8] Activation of the PI3K/Akt/mTOR kinase pathway is frequently associated with human cancer. Selective inhibition of p70S6Kinase, which is the last kinase in the PI3K pathway, is not sufficient for strong tumor growth inhi... The chemical synthesis of metabolically stabilized 2-OMe-LPA analogues and preliminary studies of their inhibitory activity toward autotaxin [作者：Gendaszewska-Darmach, E; Laska, E; Rytczak, P; Okruszek, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2698-2700 , 文章类型： Article，,卷期：2012年22-8] The chemical synthesis of five new metabolically stabilized 2-OMe-LPA analogues (1a-e) possessing different fatty acid residues has been performed by phosphorylation of corresponding 1-O-acyl-2-OMe-glycerols which were p... Design and synthesis of thiourea derivatives containing a benzo[5,6]cyclohepta[1,2-b]pyridine moiety as potential antitumor and anti-inflammatory agents [作者：Liu, WK; Zhou, JP; Zhang, T; Zhu, HY; Qian, H; Zhang, HB; Huang, WL; Gust, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2701-2704 , 文章类型： Article，,卷期：2012年22-8] Thiourea derivatives (6a-e) were developed and screened for antitumor and anti-inflammatory activity. Most of the compounds exhibited growth inhibitory effects comparable to 5-fluorouracil in vitro against mammary (MCF-7... Synthesis and antiviral activity of a series of 1 '-substituted 4-aza-7,9-dideazaadenosine C-nucleosides [作者：Cho, A; Saunders, OL; Butler, T; Zhang, LJ; Xu, J; Vela, JE; Feng, JY; Ray, AS; Kim, CU,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2705-2707 , 文章类型： Article，,卷期：2012年22-8] A series of 1 '-substituted analogs of 4-aza-7,9-dideazaadenosine C-nucleoside were prepared and evaluated for the potential as antiviral agents. These compounds showed a broad range of inhibitory activity against variou... Synthesis and in vitro anticancer and antitubercular activity of diarylpyrazole ligated dihydropyrimidines possessing lipophilic carbamoyl group [作者：Yadlapalli, RK; Chourasia, OP; Vemuri, K; Sritharan, M; Perali, RS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2708-2711 , 文章类型： Article，,卷期：2012年22-8] A series of dihydropyrimidine derivatives were synthesized by utilizing Biginelli reaction and evaluated for their in vitro anticancer activity against MCF-7 human breast cancer (HBC) cell line using sulforhodamine B (SR... Synthesis and biological activity of bi/tricyclic azasugars fused thiazolidin-4-one and thiazinan-4-one by microwave-assisted tandem Staudinger/aza-Wittig/cyclization [作者：Li, XL; Qin, ZB; Yang, TY; Zhang, HZ; Wei, SA; Li, CX; Chen, H; Meng, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2712-2716 , 文章类型： Article，,卷期：2012年22-8] A convenient synthesis of novel bi/tricyclic azasugars fused thiazolidin-4-one and thiazinan-4-one by the one-pot tandem Staudinger/aza-Wittig/cyclization reaction under microwave radiation was demonstrated. The reaction... Synthesis and evaluation of 1-(substituted)-3-prop-2-ynylureas as antiangiogenic agents [作者：Sanphanya, K; Wattanapitayakul, SK; Prangsaengtong, O; Jo, M; Koizumi, K; Shibahara, N; Priprem, A; Fokin, VV; Vajragupta, O,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3001-3005 , 文章类型： Article，,卷期：2012年22-8] Novel urea derivatives of alkynes have been designed, synthesized, and evaluated as potential cancer therapeutics leads. The most active 1-((3-chloromethyl)phenyl)-3-prop-2-ynylurea (1) exhibited cytotoxic effect against... Identification of novel telomeric G-quadruplex-targeting chemical scaffolds through screening of three NCI libraries [作者：Rahman, KM; Tizkova, K; Reszka, AP; Neidle, S; Thurston, DE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3006-3010 , 文章类型： Article，,卷期：2012年22-8] Thirteen compounds with diverse chemical structures have been identified as selective telomeric G-quadruplex-binding ligands through screening the NCI Diversity Set II, the NCI Natural Products Set II and the NCI Mechani... Footprint-based identification of viral entry inhibitors targeting HIVgp41 [作者：Holden, PM; Kaur, H; Goyal, R; Gochin, M; Rizzo, RC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3011-3016 , 文章类型： Article，,卷期：2012年22-8] A targeted virtual screen to the N-helix hydrophobic pocket on HIVgp41 was performed using DOCK followed by re-ranking with a new footprint-based scoring function which employed native gp41 C-helix residues as a referenc... Pimarane diterpenes from the fungus Epicoccum sp HS-1 associated with Apostichopus japonicus [作者：Xia, XK; Zhang, JY; Zhang, YG; Wei, F; Liu, X; Jia, AR; Liu, CH; Li, W; She, ZG; Lin, YC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3017-3019 , 文章类型： Article，,卷期：2012年22-8] Three new pimarane diterpenes (1, 2 and 3) as well as a known compound 4, were isolated from the marine-derived fungus HS-1 from Apostichopus japonicus. Their structures and relative stereochemistry of 1-3 were elucidate... Antitumor activity of annonaceous acetogenins in HepS and S180 xenografts bearing mice [作者：Chen, Y; Chen, JW; Xu, SS; Wang, Y; Li, X; Cai, BC; Fan, NB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2717-2719 , 文章类型： Article，,卷期：2012年22-8] Annonaceous acetogenins (ACGs), as one of the most powerful groups of mitochondrial complex I inhibitors, exhibit potent cytotoxic activity against a variety of human tumor cell lines. In this study, the antitumor activi... 5-Benzylidenerhodanine and 5-benzylidene-2-4-thiazolidinedione based antibacterials [作者：Zvarec, O; Polyak, SW; Tieu, W; Kuan, K; Dai, HQ; Pedersen, DS; Morona, R; Zhang, LX; Booker, GW; Abell, AD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2720-2722 , 文章类型： Article，,卷期：2012年22-8] Herein we outline the antibacterial activity of amino acid containing thiazolidinediones and rhodanines against Gram-positive bacteria Staphylococcus aureus ATCC 31890, Staphylococcus epidermidis and Bacillus subtilis AT... Sinularioside, a triacetylated glycolipid from the Indonesian soft coral Sinularia sp., is an inhibitor of NO release [作者：Putra, MY; Ianaro, A; Panza, E; Bavestrello, G; Cerrano, C; Fattorusso, E; Taglialatela-Scafati, O,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2723-2725 , 文章类型： Article，,卷期：2012年22-8] Chemical analysis of the Indonesian soft coral Sinularia sp. (order Alcyonacea, family Alcyoniidae) afforded a known glucosylcerebroside of the sarcoehrenoside-type and sinularioside (2), a new naturally triacetylated gl... Design, synthesis and cytotoxic activities of novel hybrid compounds between 2-phenylbenzofuran and imidazole [作者：Yang, XD; Wan, WC; Deng, XY; Li, Y; Yang, LJ; Li, L; Zhang, HB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2726-2729 , 文章类型： Article，,卷期：2012年22-8] A series of novel hybrid compounds between 2-phenylbenzofuran and imidazole have been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that substitution of the imidazolyl-3-p... Lead optimisation of the N1 substituent of a novel series of indazole arylsulfonamides as CCR4 antagonists and identification of a candidate for clinical investigation [作者：Procopiou, PA; Ford, AJ; Graves, RH; Hall, DA; Hodgson, ST; Lacroix, YML; Needham, D; Slack, RJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2730-2733 , 文章类型： Article，,卷期：2012年22-8] Synthesis and preliminary SAR of the N1 substituent of a novel series of indazole sulfonamide chemokine receptor 4 (CCR4) antagonist is reported. Compound 7r was identified for further development. (C) 2012 Elsevier Ltd.... Preparation and photophysical properties of a caged kynurenine [作者：Maitrani, C; Heyes, DJ; Hay, S; Arumugam, S; Popik, VV; Phillips, RS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2734-2737 , 文章类型： Article，,卷期：2012年22-8] We have prepared L-kyurenine 4-hydroxyphenacyl ester, a caged derivative of L-kynurenine. N-alpha-tBOC-L-tryptophan was reacted with 4-hydroxyphenacyl bromide in DMF with K2CO3 as the base to give the N-alpha-tBOC 4-hydr...