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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149条记录   Design and diversity-oriented synthesis of novel 1,4-thiazepan-3-ones fused with bioactive heterocyclic skeletons and evaluation of their antioxidant and cytotoxic activities [作者：Shi, F; Zeng, XN; Cao, XD; Zhang, S; Jiang, B; Zheng, WF; Tu, SJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：743-746 , 文章类型： Article，,卷期：2012年22-1] This study has achieved the design and diversity-oriented synthesis of novel 1,4-thiazepine derivatives embedded with carbazole, pyrazole or isoxazole motif via microwave-assisted multicomponent reactions under solvent-f... Synthesis and biological evaluation of novel derivatives of gambogic acid as anti-hepatocellular carcinoma agents [作者：He, LQ; Ling, Y; Fu, L; Yin, DK; Wang, XS; Zhang, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：289-292 , 文章类型： Article，,卷期：2012年22-1] A series of novel derivatives of gambogic acid (GA) were synthesized and evaluated for their in vitro cytotoxicity against human hepatocellular carcinoma (HCC) cells. All derivatives showed better aqueous solubility than... Potent adjuvantic activity of a CCR1-agonistic bis-quinoline [作者：Ukani, R; Lewis, TC; Day, TP; Wu, WY; Malladi, SS; Warshakoon, HJ; David, SA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：293-295 , 文章类型： Article，,卷期：2012年22-1] A bis-quinoline compound, (7-chloro-N-(4-(7-chloroquinolin-4-ylamino) butyl) quinolin-4-amine; RE-660) was found to have C-C chemokine receptor type 1 (CCR1)-agonistic properties. RE-660 displayed strong adjuvantic activ... Structural requirements for hybridization at the 5 '-position are different in alpha-L-LNA as compared to beta-D-LNA [作者：Seth, PP; Allerson, CR; Ostergaard, ME; Swayze, EE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：296-299 , 文章类型： Article，,卷期：2012年22-1] The synthesis and biophysical evaluation of R and S-5'-Me-alpha-L-LNA nucleoside phosphoramidites and modified oligo-2'-deoxyribonucleotides is reported. Synthesis of the nucleoside phosphoramidites was accomplished in m... 3-Heterocyclyl quinolone inhibitors of the HCV NS5B polymerase [作者：Kumar, DV; Rai, R; Brameld, KA; Riggs, J; Somoza, JR; Rajagopalan, R; Janc, JW; Xia, YM; Ton, TL; Hu, HY; Lehoux, I; Ho, JD; Young, WB; Hart, B; Green, MJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：300-304 , 文章类型： Article，,卷期：2012年22-1] The discovery and optimization of a novel class of quinolone small-molecules that inhibit NS5B polymerase, a key enzyme of the HCV viral life-cycle, is described. Our research led to the replacement of a hydrolytically l... Structure-based design of PDK1 inhibitors [作者：Poulsen, A; Blanchard, S; Soh, CK; Lee, C; Williams, M; Wang, HS; Dymock, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：305-307 , 文章类型： Article，,卷期：2012年22-1] A macrocyclic 2-anilino-4-phenyl-pyrimidine CDK/Flt3/JAK2 inhibitor was found to have moderate PDK1 activity. After docking into a PDK1 X-ray structure it was suggested that the pyrimidine ring could be substituted for a... Synthesis, cytostatic activity and ADME properties of C-5 substituted and N-acyclic pyrimidine derivatives [作者：Kraljevic, TG; Klika, M; Kralj, M; Martin-Kleiner, I; Jurmanovic, S; Milic, A; Padovan, J; Raic-Malic, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：308-312 , 文章类型： Article，,卷期：2012年22-1] The synthesis of the novel 5-alkyl pyrimidine derivatives, 5,6-dihydrofuro[2,3-d] pyrimidines and 5-alkyl N-methoxymethyl pyrimidine derivatives and evaluation of their cytostatic activities are described. The mechanism ... Discovery and optimization of thieno[2,3-d]pyrimidines as B-Raf inhibitors [作者：Packard, GK; Papa, P; Riggs, JR; Erdman, P; Tehrani, L; Robinson, D; Harris, R; Shevlin, G; Perrin-Ninkovic, S; Hilgraf, R; McCarrick, MA; Tran, T; Fleming, Y; Bai, A; Richardson, S; Katz, J; Tang, Y; Leisten, J; Moghaddam, M; Cathers, B; Zhu, D; Sakata, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：747-752 , 文章类型： Article，,卷期：2012年22-1] The serine/threonine specific protein kinase B-Raf is part of the MAPK pathway and is an interesting oncology target. We have identified thieno[2,3-d]pyrimidines as a core scaffold of small molecule B-Raf inhibitors. The... Antagonists of inhibitor of apoptosis proteins based on thiazole amide isosteres (vol 20, pg 2229, 2010) [作者：Cohen, F; Koehler, MFT; Bergeron, P; Elliott, LO; Flygare, JA; Franklin, MC; Gazzard, L; Keteltas, SF; Lau, K; Ly, CQ; Tsui, V; Fairbrother, WJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：753-754 , 文章类型： Correction，,卷期：2012年22-1] Identification of 5,6-substituted 4-aminothieno[2,3-d]pyrimidines as LIMK1 inhibitors (vol 21, pg 5992, 2011) [作者：Sleebs, BE; Nikolakopoulos, G; Street, IP; Falk, H; Baell, JB,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：755-757 , 文章类型： Correction，,卷期：2012年22-1] Synthesis of bivalent lactosides and their activity as sensors for differences between lectins in inter- and intrafamily comparisons [作者：Andre, S; Jarikote, DV; Yan, DD; Vincenz, L; Wang, GN; Kaltner, H; Murphy, PV; Gabius, HJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：313-318 , 文章类型： Article，,卷期：2012年22-1] The synthesis of nine bivalent lactosides (based on ditriazoles, diamides, a glycocyclophane and an acyclic analogue of the glycocyclophane) and one monovalent lactosyl triazole facilitated the assessment of the sensitiv... Synthesis of [F-18]-labeled (2-(2-fluoroethoxy)ethyl) triphenylphosphonium cation as a potential agent for myocardial imaging using positron emission tomography [作者：Kim, DY; Kim, HJ; Yu, KH; Min, JJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：319-322 , 文章类型： Article，,卷期：2012年22-1] [F-18]-labeled molecular probe for the detection of myocardial perfusion deficit is driving particular interest due to its high clinical applicability. Thus, we synthesized (2-(2-[F-18] fluoroethoxy) ethyl) triphenylphos... Emodin inhibits migration and invasion of DLD-1 (PRL-3) cells via inhibition of PRL-3 phosphatase activity [作者：Han, YM; Lee, SK; Jeong, DG; Ryu, SE; Han, DC; Kim, DK; Kwon, BM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：323-326 , 文章类型： Article，,卷期：2012年22-1] Anthraquinones have been reported as phosphatase inhibitors. Therefore, anthraquinone derivatives were screened to identify a potent phosphatase inhibitor against the phosphatase of regenerating liver-3 (PRL-3). Emodin s... Synthesis and anticonvulsant evaluation of some new 2,3,8-trisubstituted-4(3H)-quinazoline derivatives [作者：El-Azab, AS; ElTahir, KEH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：327-333 , 文章类型： Article，,卷期：2012年22-1] A new series of 2,3,8-trisubstituted-4(3H)-quinazoline derivatives were synthesized, evaluated for their anticonvulsant activity against electrically (MES) and chemically (PTZ, picrotoxin and Strychnine) induced seizures... Discovery of cyclic amine-substituted benzoic acids as PPAR alpha agonists [作者：Nomura, M; Yumoto, K; Shinozaki, T; Isogai, S; Takano, Y; Murakami, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：334-338 , 文章类型： Article，,卷期：2012年22-1] A series of novel cyclic amine-substituted benzoic acid derivatives were synthesized and evaluated for their PPAR alpha agonist activity. Strucure-activity relationship studies led to the identification of (S)-3-[3[2-(4-... Discovery and bioactivity of 4-(2-arylpyrido[3 ',2 ':3,4]pyrrolo[1,2-f][1,2,4]-triazin-4-yl) morpholine derivatives as novel PI3K inhibitors [作者：Wang, J; Wang, X; Chen, YH; Chen, SM; Chen, G; Tong, LJ; Meng, LH; Xie, YY; Ding, J; Yang, CH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：339-342 , 文章类型： Article，,卷期：2012年22-1] PI3K is a promising therapeutic target for cancer. With PI-103 as the lead compound, we designed and synthesized 4-(2-arylpyrido[3',2':3,4] pyrrolo[1,2-f][1,2,4]triazin-4-yl)morpholine derivatives. 9, 10a, 10d, 10e had t...