- Enhanced selectivity profile of pyrazole-urea based DFG-out p38 alpha inhibitors
[作者：Liu, H; Kuhn, C; Feru, F; Jacques, SL; Deshmukh, GD; Ye, P; Rennie, GR; Johnson, T; Kazmirski, S; Low, S; Coli, R; Ding, YH; Cheng, AC; Tecle, H; English, JM; Stanton, R; Wu, JC,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4885-4891 , 文章类型： Article，,卷期：2010年20-16]
- By targeting an extended region of the conventional 'DFG-out' pocket of p38 alpha, while minimizing interactions with the specificity pocket and eliminating interactions with the adenine binding site, we are able to desi...
- Synthesis and vasodilative activity of tanshinone IIA derivatives
[作者：Bi, YF; Xu, HW; Liu, XQ; Zhang, XJ; Wang, ZJ; Liu, HM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4892-4894 , 文章类型： Article，,卷期：2010年20-16]
- A series of 2,2'-(substituted methylene)bis-(1,6,6-trimethyl-6,7,8,9-tetrahydrophenanthro[1,2-b]furan-10,11-dione) derivatives were synthesized by the reaction of tanshinone IIA (D-1) and aromatic aldehyde in the presenc...
- Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4 '-piperidine] based melanocortin subtype-4 receptor agonists
[作者：Guo, LQ; Ye, ZX; Liu, JA; He, SW; Bakshi, RK; Sebhat, IK; Dobbelaar, PH; Hong, QM; Jian, TY; Dellureficio, JP; Tsou, NN; Ball, RG; Weinberg, DH; MacNeil, T; Tang, R; Tamvakopoulos, C; Peng, QP; Chen, HY; Chen, ARS; Martin, WJ; MacIntyre, DE; Strack, AM; Fong, TM; Wyvratt, MJ; Nargund, RP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4895-4900 , 文章类型： Article，,卷期：2010年20-16]
- Design, synthesis, and SAR of a series of 3H-spiro[isobenzofuran-1,4'-piperidine] based compounds as potent, selective and orally bioavailable melanocortin subtype-4 receptor (MC4R) agonists are disclosed. (c) 2010 Elsev...
- An orally bioavailable positive allosteric modulator of the mGlu(4) receptor with efficacy in an animal model of motor dysfunction
[作者：East, SP; Bamford, S; Dietz, MGA; Eickmeier, C; Flegg, A; Ferger, B; Gemkow, MJ; Heilker, R; Hengerer, B; Kotey, A; Loke, P; Schanzle, G; Schubert, HD; Scott, J; Whittaker, M; Williams, M; Zawadzki, P; Gerlach, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4901-4905 , 文章类型： Article，,卷期：2010年20-16]
- A high-throughput screening campaign identified 4-((E)-styryl)-pyrimidin-2- ylamine (11) as a positive allosteric modulator of the metabotropic glutamate (mGlu) receptor subtype 4. An evaluation of the structure-activity...
- Synthesis of sialyllactosamine clusters using carbosilane as core scaffolds by means of chemical and enzymatic approaches
[作者：Matsuoka, K; Kaneko, R; Koyama, T; Ma, XT; Esumi, Y; Nakamura, T; Hatano, K; Terunuma, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4906-4910 , 文章类型： Article，,卷期：2010年20-16]
- An efficient synthesis of sialyllactosamine (SiaLacNAc) clusters using carbosilanes as core scaffolds has been accomplished by means of chemical and enzymatic approaches. N-Acetyl-D-glucosamine (GlcNAc) clusters having O...
- Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists
[作者：Abel, U; Schluter, T; Schulz, A; Hambruch, E; Steeneck, C; Hornberger, M; Hoffmann, T; Perovic-Ottstadt, S; Kinzel, O; Burnet, M; Deuschle, U; Kremoser, C,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4911-4917 , 文章类型： Article，,卷期：2010年20-16]
- To overcome the known liabilities of GW4064 a series of analogs were synthesized where the stilbene double bond is replaced by an oxymethylene or amino-methylene linker connecting a terminal benzoic acid with a substitut...
- Design, synthesis, and structure-activity relationship study of conformationally constrained analogs of indole-3-carboxamides as novel CB1 cannabinoid receptor agonists
[作者：Kiyoi, T; York, M; Francis, S; Edwards, D; Walker, G; Houghton, AK; Cottney, JE; Baker, J; Adam, JM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4918-4921 , 文章类型： Article，,卷期：2010年20-16]
- Novel tricyclic indole-3-carboxamides were synthesized as structurally restricted analogs of bicyclic indoles, and found to be potent CB1 cannabinoid receptor agonists. The CB1 agonist activity depended on the absolute c...
- Synthesis, selective anti-Helicobacter pylori activity, and cytotoxicity of novel N-substituted-2-oxo-2H-1-benzopyran-3-carboxamides
[作者：Chimenti, F; Bizzarri, B; Bolasco, A; Secci, D; Chimenti, P; Granese, A; Carradori, S; Rivanera, D; Zicari, A; Scaltrito, MM; Sisto, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4922-4926 , 文章类型： Article，,卷期：2010年20-16]
- N-substituted-3-carboxamido-coumarin derivatives were prepared and evaluated for selective antibacterial activity against 20 isolates of Helicobacter pylori clinical strains, including five metronidazole resistant ones. ...
- Structure-activity relationship of lupane-triterpene glycosides from Acanthopanax koreanum on spleen lymphocyte IL-2 and IFN-gamma
[作者：Nguyen, XN; Phan, VK; Chau, VM; Bui, HT; Nguyen, HT; Ha, DT; Soung, KS; Kim, JH; Ahn, JY; Lee, YM; Kim, YH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4927-4931 , 文章类型： Article，,卷期：2010年20-16]
- Phytochemical investigation resulted in the isolation of three new lupane-triterpene glycosides acankoreosides M-O (1, 2 and 8) together with eight known lupane-triterpene glycosides (3-7, 9-11) from the leaves of Acanth...
- Smoothened antagonists for hair inhibition
[作者：Li, JJ; Shanmugasundaram, V; Reddy, S; Fleischer, LL; Wang, ZQ; Smith, Y; Harter, WG; Yue, WS; Swaroop, M; Li, L; Ji, CX; Dettling, D; Osak, B; Fitzgerald, LR; Conradi, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4932-4935 , 文章类型： Article，,卷期：2010年20-16]
- A series of aminomethylpyrazoles were prepared and evaluated using cell-based Smoothened beta-lactamase reporter assay and Smoothened binding assay. Potent Smoothened antagonists 10k and 10l were found to inhibit hair gr...
- Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones
[作者：Power, DP; Lozach, O; Meijer, L; Grayson, DH; Connon, SJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4940-4944 , 文章类型： Article，,卷期：2010年20-16]
- A remarkably concise, chromatography-free route to the parent compound of the paullone family of cyclin-dependent kinase (CDK) inhibitors is reported. A similar strategy allowed the synthesis of the hitherto missing 9-az...
- Synthesis and docking studies on styryl chromones exhibiting cytotoxicity in human breast cancer cell line
[作者：Bhatnagar, S; Sahi, S; Kackar, P; Kaushik, S; Dave, MK; Shukla, A; Goel, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4945-4950 , 文章类型： Article，,卷期：2010年20-16]
- The search for small molecules that preferentially target the functionally important surfaces of estrogen receptor and disrupt the transcriptional activity in the cell has emerged as a promising area towards rationale ba...
- Synthesis and biological activity of a series of tetrasubstituted-imidazoles as P2X(7) antagonists
[作者：Gleave, RJ; Walter, DS; Beswick, PJ; Fonfria, E; Michel, AD; Roman, SA; Tang, SP,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：4951-4954 , 文章类型： Article，,卷期：2010年20-16]
- A series of analogues of the pyrazole lead 1 were synthesized in which the heterocyclic core was replaced with an imidazole. A number of potent antagonists were identified and structure-activity relationships (SAR) were ...
- Structure-guided design of alpha-amino acid-derived Pin1 inhibitors (vol 20, pg 586, 2010)
[作者：Potter, AJ; Ray, S; Gueritz, L; Nunns, CL; Bryant, CJ; Scrace, SF; Matassova, N; Baker, L; Dokurno, P; Robinson, DA; Surgenor, AE; Davis, B; Murray, JB; Richardson, CM; Moore, JD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：E1-E1 , 文章类型： Correction，,卷期：2010年20-16]
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