- Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors
[作者：Sun, LQ; Qin, BJ; Huang, L; Qian, KD; Chen, CH; Lee, KH; Xie, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2376-2379 , 文章类型： Article，,卷期：2012年22-7]
- The current optimization of 2,4-diarylaniline analogs (DAANs) on the central phenyl ring provided a series of new active DAAN derivatives 9a-9e, indicating an accessible modification approach that could improve anti-HIV ...
- Consequences of linker length alteration of the alpha 7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333
[作者：Beinat, C; Banister, SD; van Prehn, S; Doddareddy, MR; Hibbs, D; Sako, M; Chebib, M; Tran, T; Al-Muhtasib, N; Xiao, YX; Kassiou, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2380-2384 , 文章类型： Article，,卷期：2012年22-7]
- A series of ligands based on SEN12333, containing either contracted or elongated alkyl chains, were synthesized and evaluated in molecular docking studies against a homology model of the alpha 7 nicotinic acetylcholine r...
- Design and synthesis of a vialinin A analog with a potent inhibitory activity of TNF-alpha production and its transformation into a couple of bioprobes
[作者：Ye, YQ; Onose, J; Abe, N; Koshino, H; Takahashi, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2385-2387 , 文章类型： Article，,卷期：2012年22-7]
- Vialinin A (1) is an extremely potent inhibitor against tumor necrosis factor (TNF)-alpha production in rat basophilic leukemia (RBL-2H3) cells. This Letter describes the design and synthesis of its advanced analog, 50,6...
- Short cyclic peptides derived from the C-terminal sequence of alpha 1-antitrypsin exhibit significant anti-HIV-1 activity
[作者：Jia, QY; Jiang, XF; Yu, F; Qiu, JY; Kang, XY; Cai, LF; Li, L; Shi, WG; Liu, SW; Jiang, SB; Liu, KL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2393-2395 , 文章类型： Article，,卷期：2012年22-7]
- Serpin A1 (alpha 1-AT), the largest subgroup of serpins, presents in human plasma at high concentration and plays important regulatory roles in physiological and pathological processes. Accumulated evidence suggests that...
- Facile synthesis of triterpenoid saponins bearing beta-Glu/Gal-(1 -> 3)-beta-GluA methyl ester and their cytotoxic activities
[作者：Gao, J; Li, X; Gu, GF; Liu, SS; Cui, M; Lou, HX,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2396-2400 , 文章类型： Article，,卷期：2012年22-7]
- Convenient synthetic strategy toward spinasaponin A methyl ester 1 and calenduloside G methyl ester 2, two natural oleanane-type triterpenoid saponins bearing an unique beta-D-glucosyl/galactosyl-(1 -> 3)-beta-D-glucuron...
- Scabronine M, a novel inhibitor of NGF-induced neurite outgrowth from PC12 cells from the fungus Sarcodon scabrosus
[作者：Liu, L; Shi, XW; Zong, SC; Tang, JJ; Gao, JM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2401-2406 , 文章类型： Article，,卷期：2012年22-7]
- A novel cyathane diterpenoid, designated scabronine M (1), was isolated from the fruiting bodies of the mushroom Sarcodon scabrosus together with 10 known compounds. The structure of the new compound was elucidated on th...
- Discovery of a new binding mode for a series of liver X receptor agonists
[作者：Kopecky, DJ; Jiao, XY; Fisher, B; McKendry, S; Labelle, M; Piper, DE; Coward, P; Shiau, AK; Escaron, P; Danao, J; Chai, A; Jaen, J; Kayser, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2407-2410 , 文章类型： Article，,卷期：2012年22-7]
- Structural modification of a series of dual LXR alpha/beta agonists led to the identification of a new class of LXR beta partial agonists. An X-ray co-crystal structure shows that a representative member of this series, ...
- Design and synthesis of orally available MEK inhibitors with potent in vivo antitumor efficacy
[作者：Adams, ME; Wallace, MB; Kanouni, T; Scorah, N; O'Connell, SM; Miyake, H; Shi, LH; Halkowycz, P; Zhang, L; Dong, Q,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2411-2414 , 文章类型： Article，,卷期：2012年22-7]
- The structure-based design, synthesis, and biological evaluation of two novel series of potent and selective MEK kinase inhibitors are described herein. The elaboration of a lead pyrrole derivative to a bicyclic dihydroi...
- The first stereoselective total synthesis of (Z)-cryptomoscatone D2, a natural G(2) checkpoint inhibitor
[作者：Reddy, GC; Balasubramanyam, P; Salvanna, N; Reddy, TS; Das, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2415-2417 , 文章类型： Article，,卷期：2012年22-7]
-
- Synthesis, crystal structures, in vitro biological evaluation of zinc(II) and bismuth(III) complexes of 2-acetylpyrazine N(4)-phenylthiosemicarbazone
[作者：Li, MX; Zhang, LZ; Yang, M; Niu, JY; Zhou, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2418-2423 , 文章类型： Article，,卷期：2012年22-7]
- Two metal complexes formulated as [Zn(L)(2)](2)center dot H2O (1) and [Bi(L)(NO3)(2)(CH3OH)] (2), where HL = 2-acetylpyrazine N(4)-phenylthiosemicarbazone, have been synthesized and characterized by elemental analysis, I...
- Radical-regulating and antiviral properties of ascorbic acid and its derivatives
[作者：Brinkevich, SD; Boreko, EI; Savinova, OV; Pavlova, NI; Shadyro, OI,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2424-2427 , 文章类型： Article，,卷期：2012年22-7]
- The ability of ascorbic acid and a number of its derivatives to suppress replication of Herpes simplex virus type I was investigated in human rhabdomyosarcoma cell line. In parallel, interaction of the test compounds wit...
- Structure aided design of chimeric antibiotics
[作者：Karoli, T; Mamidyala, SK; Zuegg, J; Fry, SR; Tee, EHL; Bradford, TA; Madala, PK; Huang, JX; Ramu, S; Butler, MS; Cooper, MA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2428-2433 , 文章类型： Article，,卷期：2012年22-7]
- The rise of antibiotic resistance is of great clinical concern. One approach to reducing the development of resistance is to co-administer two or more antibiotics with different modes of action. However, it can be diffic...
- Synthesis and pharmacological evaluation of carbamic acid 1-phenyl-3-(4-phenyl-piperazine-1-yl)-propyl ester derivatives as new analgesic agents
[作者：Chae, E; Yi, H; Choi, Y; Cho, H; Lee, K; Moon, H,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2434-2439 , 文章类型： Article，,卷期：2012年22-7]
- A series of carbamic acid 1-phenyl-3-(4-phenyl-piperazine-1-yl)-propyl ester derivatives were synthesized through discovery strategies for balancing target-based in vitro screening and phenotypic in vivo screening. All t...
- Determination of intracellular pH using sensitive, clickable fluorescent probes
[作者：Yapici, NB; Mandalapu, SR; Chew, TL; Khuon, S; Bi, LR,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2440-2443 , 文章类型： Article，,卷期：2012年22-7]
- We synthesized and evaluated a series of acidic fluorescent pH probes exhibiting robust pH dependence, high sensitivity and photostability, and excellent cell membrane permeability. Titration analyses indicated that prob...
- Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor
[作者：Cumming, JN; Smith, EM; Wang, LY; Misiaszek, J; Durkin, J; Pan, JP; Iserloh, U; Wu, YS; Zhu, ZN; Strickland, C; Voigt, J; Chen, X; Kennedy, ME; Kuvelkar, R; Hyde, LA; Cox, K; Favreau, L; Czarniecki, MF; Greenlee, WJ; McKittrick, BA; Parker, EM; Stamford, AW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：2444-2449 , 文章类型： Article，,卷期：2012年22-7]
- From an initial lead 1, a structure-based design approach led to identification of a novel, high-affinity iminohydantoin BACE1 inhibitor that lowers CNS-derived Ab following oral administration to rats. Herein we report ...
|