- Biological evaluation and docking studies of natural isocoumarins as inhibitors for human kallikrein 5 and 7
[作者:Teixeira, TSP; Freitas, RF; Abrahao, O; Devienne, KF; de Souza, LR; Blaber, SI; Blaber, M; Kondo, MY; Juliano, MA; Juliano, L; Puzer, L,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6112-6115 , 文章类型: Article,,卷期:2011年21-20]
- Human kallikrein 5 and 7 (KLK5 and KLK7) are trypsin-like and chymotrypsin-like serine proteases, respectively, and promising targets for the treatment of skin desquamation, inflammation and cancer. In an effort to devel...
- Synthesis, biological evaluation and molecular docking studies of 1,3,4-thiadiazole derivatives containing 1,4-benzodioxan as potential antitumor agents
[作者:Sun, J; Yang, YS; Li, W; Zhang, YB; Wang, XL; Tang, JF; Zhu, HL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6116-6121 , 文章类型: Article,,卷期:2011年21-20]
- A series of 1,3,4-thiadiazole derivatives containing 1,4-benzodioxan (2a-2s) have been synthesized to screen for FAK inhibitory activity. Compound 2p showed the most potent biological activity against HEPG2 cancer cell l...
- Design and synthesis of potent, orally-active DGAT-1 inhibitors containing a dioxino[2,3-d]pyrimidine core
[作者:Dow, RL; Andrews, M; Aspnes, GE; Balan, G; Gibbs, EM; Guzman-Perez, A; Karki, K; LaPerle, JL; Li, JC; Litchfield, J; Munchhof, MJ; Perreault, C; Patel, L,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6122-6125 , 文章类型: Article,,卷期:2011年21-20]
- A novel series of potent DGAT-1 inhibitors was developed originating from the lactam-based clinical candidate PF-04620110. Incorporation of a dioxino[2,3-d]pyrimidine-based core afforded good alignment of pharmacophore f...
- Synthesis and structure-activity relationships of 4,5-fused pyridazinones as histamine H(3) receptor antagonists
[作者:Tao, M; Raddatz, R; Aimone, LD; Hudkins, RL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6126-6130 , 文章类型: Article,,卷期:2011年21-20]
- Three series of novel 4,5-fused pyridazinones were synthesized as histamine H(3) receptor antagonists. The 2,5,6,7-tetrahydrocyclopenta[d]pyridazin-1-one 5q and 5,6,7,8-tetrahydro-2H-phthalazin-1-one 5u displayed high af...
- Oleanane-type triterpene saponins from the bark of Aralia elata and their NF-kappa B inhibition and PPAR activation signal pathway
[作者:Nhiem, NX; Lim, HY; Kiem, PV; Minh, CV; Thu, VK; Tai, BH; Quang, TH; Song, SB; Kim, YH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6143-6147 , 文章类型: Article,,卷期:2011年21-20]
- Two new oleanane-type triterpene saponins, tarasaponin IV (1) and elatoside L (2), and four known; stipuleanoside R(2) (3), kalopanax-saponin F (4), kalopanax-saponin F methylester (5), and elatoside D (6) were isolated ...
- Substitution of the GalNAc-alpha-O-Thr(11) residue in drosocin with O-linked glyco-peptoid residue: Effect on antibacterial activity and conformational change
[作者:Ahn, M; Murugan, RN; Nan, YH; Cheong, C; Sohn, H; Kim, EH; Hwang, E; Ryu, EK; Kang, SW; Shin, SY; Bang, JK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6148-6153 , 文章类型: Article,,卷期:2011年21-20]
- One of the obvious disadvantages of natural peptides is their liability to proteases. Among the several solutions for this issue, peptoids or oligomers of N-substituted glycine have emerged as a promising tool that may e...
- Conformationally constrained farnesoid X receptor (FXR) agonists: Alternative replacements of the stilbene
[作者:Akwabi-Ameyaw, A; Caravella, JA; Chen, LH; Creech, KL; Deaton, DN; Madauss, KP; Marr, HB; Miller, AB; Navas, F; Parks, DJ; Spearing, PK; Todd, D; Williams, SP; Wisely, B,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6154-6160 , 文章类型: Article,,卷期:2011年21-20]
- To further explore the optimum placement of the acid moiety in conformationally constrained analogs of GW 4064 1a, a series of stilbene replacements were prepared. The benzothiophene If and the indole 1g display the opti...
- A new N-methyl thymine derivative comprising a dihydroxyisobutenyl unit as ligand for thymidine kinase of herpes simplex virus type 1 (HSV-1 TK)
[作者:Kristafor, S; Novakovic, I; Kraljevic, TG; Pavelic, SK; Lucin, P; Westermaier, Y; Pernot, L; Scapozza, L; Ametamey, SM; Raic-Malic, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6161-6165 , 文章类型: Article,,卷期:2011年21-20]
- Molecular modeling and phosphorylation assay in vitro were employed to select a novel unsaturated 1,3-dihydroxyisobutenyl thymine derivative 6 as ligand for HSV-1 TK which may be of interest as lead for the development o...
- Benzotriazinone and benzopyrimidinone derivatives as potent positive allosteric AMPA receptor modulators
[作者:Mueller, R; Rachwal, S; Lee, S; Zhong, S; Li, YX; Haroldsen, P; Herbst, T; Tanimura, S; Varney, M; Johnson, S; Rogers, G; Street, LJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6170-6175 , 文章类型: Article,,卷期:2011年21-20]
- AMPA receptors (AMPARs) have been demonstrated to be an important therapeutic CNS target. A series of substituted benzotriazinone and benzopyrimidinone derivatives were prepared with the aim to improve in vivo activity o...
- Acylglycinamides as inhibitors of glycine transporter type 1
[作者:Blunt, R; Porter, R; Johns, A; Nash, D; Puckey, G; Wyman, P; Herdon, H; Teague, S; Hadden, V; Fontana, S; Gordon, L,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6176-6179 , 文章类型: Article,,卷期:2011年21-20]
- A screening hit was used as the basis for the core structure of a new series of acylglycinamide GlyT-1 inhibitors. Investigation of the SAR around four areas of diversity used facile chemistry to prepare compounds quickl...
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