- Structure-activity relationship of isoform selective inhibitors of Rac1/1b GTPase nucleotide binding
[作者：Beausoleil, E; Chauvignac, C; Taverne, T; Lacombe, S; Pognante, L; Leblond, B; Pallares, D; De Oliveira, C; Bachelot, F; Carton, R; Peillon, H; Coutadeur, S; Picard, V; Lambeng, N; Desire, L; Schweighoffer, F,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5594-5598 , 文章类型： Article，,卷期：2009年19-19]
- The synthesis of a series of berberine, phenantridine and isoquinoline derivatives was realized to explore their Rho GTPase nucleotide inhibitory activity. The compounds were evaluated in a nucleotide binding competition...
- Pyrazole NNRTIs 1: Design and initial optimisation of a novel template
[作者：Mowbray, CE; Burt, C; Corbau, R; Perros, M; Tran, I; Stupple, PA; Webster, R; Wood, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5599-5602 , 文章类型： Article，,卷期：2009年19-19]
- The design and synthesis of a novel series of non-nucleoside HIV reverse transcriptase inhibitors (NNR-TIs) based on a pyrazole template is described. These compounds are active against wild type reverse transcriptase (R...
- Pyrazole NNRTIs 3: Optimisation of physicochemical properties
[作者：Mowbray, CE; Corbau, R; Hawes, M; Jones, LH; Mills, JE; Perros, M; Selby, MD; Stupple, PA; Webster, R; Wood, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5603-5606 , 文章类型： Article，,卷期：2009年19-19]
- Our efforts to reduce overall lipophilicity and increase ligand-lipophilicity efficiency (LLE) by modification of the 3- and 5-substituents of pyrazole 1, a novel non-nucleoside HIV reverse transcriptase inhibitor (NNRTI...
- Structure-based design of novel human Pin1 inhibitors (I)
[作者：Guo, CX; Hou, XJ; Dong, LM; Dagostino, E; Greasley, S; Ferre, R; Marakovits, J; Johnson, MC; Matthews, D; Mroczkowski, B; Parge, H; VanArsdale, T; Popoff, I; Piraino, J; Margosiak, S; Thomson, J; Los, G; Murray, BW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5613-5616 , 文章类型： Article，,卷期：2009年19-19]
- Pin1 is a member of the cis-trans peptidyl-prolyl isomerase family with potential anti-cancer therapeutic value. Here we report structure-based de novo design and optimization of novel Pin1 inhibitors. Without a viable l...
- The discovery of tertiary-amine LXR agonists with potent cholesterol efflux activity in macrophages
[作者：Marino, JP; Kallander, LS; Ma, C; Oh, HJ; Lee, D; Gaitanopoulos, DE; Krawiec, JA; Parks, DJ; Webb, CL; Ziegler, K; Jaye, M; Thompson, SK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5617-5621 , 文章类型： Article，,卷期：2009年19-19]
- The liver X receptors (LXR) play a key role in cholesterol homeostasis and lipid metabolism. SAR studies around tertiary-amine lead molecule 2, an LXR full agonist, revealed that steric and conformational changes to the ...
- Design, synthesis, screening, and molecular modeling study of a new series of ROS1 receptor tyrosine kinase inhibitors
[作者：El-Deeb, IM; Park, BS; Jung, SJ; Yoo, KH; Oh, CH; Cho, SJ; Han, DK; Lee, JY; Lee, SH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5622-5626 , 文章类型： Article，,卷期：2009年19-19]
- A series of rationally designed ROS1 tyrosine kinase inhibitors was synthesized and screened. Compound 12b has showed good potency with IC50 value of 209 nM, which is comparable with that of the reference lead compound 1...
- O-Spiro C-aryl glucosides as novel sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors
[作者：Xu, BH; Lv, BH; Feng, Y; Xu, G; Du, JY; Welihinda, A; Sheng, ZL; Seed, B; Chen, YW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5632-5635 , 文章类型： Article，,卷期：2009年19-19]
- Two series of O-spiro C-aryl glucosides were synthesized and tested for inhibition of hSGLT1 and hSGLT2. 60-O-Spiro C-aryl glucosides exhibited potent in vitro hSGLT2 inhibitory activity but 20-O-spiro C-aryl glucosides ...
- Fully automated synthesis and initial PET evaluation of [C-11]PBR28
[作者：Wang, M; Yoder, KK; Gao, MZ; Mock, BH; Xu, XM; Saykin, AJ; Hutchins, GD; Zheng, QH,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5636-5639 , 文章类型： Article，,卷期：2009年19-19]
- Fully automated synthesis and initial PET evaluation of a TSPO radioligand, [C-11]PBR28 (N-(2[C-11]methoxybenzyl)-N-(4-phenoxypyridin-3-yl)acetamide), are reported. These results facilitate the potential preclinical and ...
- Functional analyses of cytochrome P450 genes responsible for the early steps of brassicicene C biosynthesis
[作者：Hashimoto, M; Higuchi, Y; Takahashi, S; Osada, H; Sakaki, T; Toyomasu, T; Sassa, T; Kato, N; Dairi, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5640-5643 , 文章类型： Article，,卷期：2009年19-19]
- We previously revealed that Orf8 and Orf6, which were identified in the brassicicene C biosynthetic gene cluster in Alternaria brassicicola strain ATCC96836, were fusicoccadiene (FD) synthase and 16-O-methyltransferase, ...
- Synthesis and in vitro evaluation of 2,4-diamino-1,3,5-triazine derivatives as neuronal voltage-gated sodium channel blockers
[作者：Ma, X; Poon, TY; Wong, PTH; Chui, WK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5644-5647 , 文章类型： Article，,卷期：2009年19-19]
- Neuronal sodium channels blockers interfere with ion flux and have been used for managing neuropathic pain, epilepsy, and cerebral ischemic disorders. In the current study, four groups of 2,4-diamino-1,3,5-triazine deriv...
- Non-nucleoside inhibitors of HCV polymerase NS5B. Part 3: Synthesis and optimization studies of benzothiazine-substituted tetramic acids
[作者：de Vicente, J; Hendricks, RT; Smith, DB; Fell, JB; Fischer, J; Spencer, SR; Stengel, PJ; Mohr, P; Robinson, JE; Blake, JF; Hilgenkamp, RK; Yee, C; Zhao, JP; Elworthy, TR; Tracy, J; Chin, E; Li, J; Lui, A; Wang, BH; Oshiro, C; Harris, SF; Ghate, M; Leveque, VJP; Najera, I; Le Pogam, S; Rajyaguru, S; Ao-Ieong, G; Alexandrova, L; Fitch, B; Brandl, M; Masjedizadeh, M; Wu, SY; de Keczer, S; Voronin, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5648-5651 , 文章类型： Article，,卷期：2009年19-19]
- Benzothiazine-substituted tetramic acids were discovered as highly potent non-nucleoside inhibitors of HCV NS5B polymerase. X-ray crystallography studies confirmed the binding mode of these inhibitors with HCV NS5B polym...
- Non-nucleoside inhibitors of HCV polymerase NS5B. Part 4: Structure-based design, synthesis, and biological evaluation of benzo[d]isothiazole-1,1-dioxides
[作者：de Vicente, J; Hendricks, RT; Smith, DB; Fell, JB; Fischer, J; Spencer, SR; Stengel, PJ; Mohr, P; Robinson, JE; Blake, JF; Hilgenkamp, RK; Yee, C; Adjabeng, G; Elworthy, TR; Li, J; Wang, BH; Bamberg, JT; Harris, SF; Wong, A; Leveque, VJP; Najera, I; Le Pogam, S; Rajyaguru, S; Ao-Ieong, G; Alexandrova, L; Larrabee, S; Brandl, M; Briggs, A; Sukhtankar, S; Farrell, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5652-5656 , 文章类型： Article，,卷期：2009年19-19]
- A series of benzo[d]isothiazole-1,1-dioxides were designed and evaluated as inhibitors of HCV polymerase NS5B. Structure-based design led to the incorporation of a high affinity methyl sulfonamide group. Structure-activi...
- Synthesis and in vitro DMPK profiling of a 1,2-dioxolane-based library with activity against Plasmodium falciparum
[作者：Martyn, DC; Beletsky, G; Cortese, JF; Tyndall, E; Liu, HL; Fitzgerald, MM; O'Shea, TJ; Liang, BR; Clardy, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5657-5660 , 文章类型： Article，,卷期：2009年19-19]
- A 43-member 1,2-dioxolane library was synthesized by coupling a 1,2-dioxolane-3-acetic acid derivative to a range of amines. Ten compounds had EC(50)s <= 30 nM against Plasmodium falciparum 3D7 and Dd2 strains, and anoth...
- Synthesis and anticancer activity of novel 3,4-diarylthiazol-2(3H)-ones (imines)
[作者：Liu, ZY; Wang, YM; Li, ZR; Jiang, JD; Boykin, DW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5661-5664 , 文章类型： Article，,卷期：2009年19-19]
- A series of 3,4-diarylthiazol-2(3H)-ones and three 3,4-diarylthiazol-2(3H)-imines were synthesized and evaluated for their cytotoxicity in a panel of human cancer cell lines. Compounds 21 and 22 showed potential anticanc...
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