- Synthesis and biological activity of 2-aminothiazoles as novel inhibitors of PGE(2) production in cells
[作者:Smith, B; Chang, HH; Medda, F; Gokhale, V; Dietrich, J; Davis, A; Meuillet, EJ; Hulme, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3567-3570 , 文章类型: Article,,卷期:2012年22-10]
- This Letter presents the synthesis and biological evaluation of a collection of 2-aminothiazoles as a novel class of compounds with the capability to reduce the production of PGE(2) in HCA-7 human adenocarcinoma cells. A...
- Identification of a selective small molecule inhibitor of breast cancer stem cells
[作者:Germain, AR; Carmody, LC; Morgan, B; Fernandez, C; Forbeck, E; Lewis, TA; Nag, PP; Ting, A; VerPlank, L; Feng, YX; Perez, JR; Dandapani, S; Palmer, M; Lander, ES; Gupta, PB; Schreiber, SL; Munoz, B,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3571-3574 , 文章类型: Article,,卷期:2012年22-10]
- A high-throughput screen (HTS) with the National Institute of Health-Molecular Libraries Small Molecule Repository (NIH-MLSMR) compound collection identified a class of acyl hydrazones to be selectively lethal to breast ...
- The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-Raf(V600E) kinase
[作者:Ren, L; Ahrendt, KA; Grina, J; Laird, ER; Buckmelter, AJ; Hansen, JD; Newhouse, B; Moreno, D; Wenglowsky, S; Dinkel, V; Gloor, SL; Hastings, G; Rana, S; Rasor, K; Risom, T; Sturgis, HL; Voegtli, WC; Mathieu, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3387-3391 , 文章类型: Article,,卷期:2012年22-10]
- Herein we describe the discovery of a novel series of ATP competitive B-Raf inhibitors via structure based drug design (SBDD). These pyridopyrimidin-7-one based inhibitors exhibit both excellent cellular potency and stri...
- Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring
[作者:Boys, ML; Bian, F; Kramer, JB; Chio, CL; Ren, XD; Chen, HF; Barrett, SD; Sexton, KE; Iula, DM; Filzen, GF; Nguyen, MN; Angell, P; Downs, VL; Wang, Z; Raheja, N; Ellsworth, EL; Fakhoury, S; Bratton, LD; Keller, PR; Gowan, R; Drummond, EM; Maiti, SN; Hena, MA; Lu, L; McConnell, P; Knafels, JD; Thanabal, V; Sun, F; Alessi, D; McCarthy, A; Zhang, EL; Finzel, BC; Patel, S; Ciotti, SM; Eisma, R; Payne, NA; Gilbertsen, RB; Kostlan, CR; Pocalyko, DJ; Lala, DS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3392-3397 , 文章类型: Article,,卷期:2012年22-10]
- A series of 2-(1H-pyrazol-1-yl)pyridines are described as inhibitors of ALK5 (TGF beta receptor I kinase). Modeling compounds in the ALK5 kinase domain enabled some optimization of potency via substitutions on the pyrazo...
- Ianthellamide A, a selective kynurenine-3-hydroxylase inhibitor from the Australian marine sponge Ianthella quadrangulata
[作者:Feng, YJ; Bowden, BF; Kapoor, V,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3398-3401 , 文章类型: Article,,卷期:2012年22-10]
- Ianthellamide A (1), a novel octopamine derivative, was isolated from the Australian marine sponge Ianthella quadrangulata. Compound 1 selectively inhibited the activity of kynurenine 3-hydroxylase with an IC50 value of ...
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