- Effect of chirality of small molecule organofluorine inhibitors of amyloid self-assembly on inhibitor potency
[作者：Sood, A; Abid, M; Hailemichael, S; Foster, M; Torok, B; Torok, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6931-6934 , 文章类型： Article，,卷期：2009年19-24]
- The effect of enantiomeric trifluoromethyl-indolyl-acetic acid ethyl esters on the fibrillogenesis of Alzheimer's amyloid beta (A beta) peptide is described. These compounds have been previously identified as effective i...
- 1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines are 5-HT6 receptor ligands
[作者：Bernotas, RC; Antane, SA; Lenicek, SE; Haydar, SN; Robichaud, AJ; Harrison, BL; Zhang, GM; Smith, D; Coupet, J; Schechter, LE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6935-6938 , 文章类型： Article，,卷期：2009年19-24]
- 1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines were prepared. Binding assays indicated they are 5-HT6 receptor ligands, among which 6f and 6g showed high affinity for 5-HT6 receptors with K-i = 3.9 and 1.7 nM, res...
- Synthesis and biological evaluation of 2-amino-7,7-dimethyl 4-substituted-5-oxo-1-(3,4,5-trimethoxy)-1,4,5,6,7,8-hexahydro-quinoline-3-carbonitrile derivatives as potential cytotoxic agents
[作者：Alqasoumi, SI; Al-Taweel, AM; Alafeefy, AM; Hamed, MM; Noaman, E; Ghorab, MM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6939-6942 , 文章类型： Article，,卷期：2009年19-24]
- A large number of antimitotic drugs, derived from natural sources or chemically synthesized, have been identified and shown to interfere with the tubulin system. Inhibition of tubulin polymerization is among the importan...
- Physicochemical property profiles of marketed drugs, clinical candidates and bioactive compounds
[作者：Tyrchan, C; Blomberg, N; Engkvist, O; Kogej, T; Muresan, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6943-6947 , 文章类型： Article，,卷期：2009年19-24]
- We performed a comparison of several simple physicochemical properties between marketed drugs, clinical candidates and bioactive compounds using commercially available databases (GVKBIO, Hyderabad, India). In contrast to...
- N-Bridged bicyclic sulfonamides as inhibitors of gamma-secretase
[作者：Bowers, S; Probst, GD; Truong, AP; Hom, RK; Konradi, AW; Sham, HL; Garofalo, AW; Wong, K; Goldbach, E; Quinn, KP; Sauer, JM; Wallace, W; Nguyen, L; Hemphill, SS; Bova, MP; Basi, GS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6952-6956 , 文章类型： Article，,卷期：2009年19-24]
- The structural modification of a series of [3.3.1] bicyclic sulfonamide based gamma-secretase inhibitors is described. Appropriate substitution on the bicyclic scaffold provides a significant increase in the metabolic st...
- Novel pyrazolopyrimidines as highly potent B-Raf inhibitors
[作者：Di Grandi, MJ; Berger, DM; Hopper, DW; Zhang, CC; Dutia, M; Dunnick, AL; Torres, N; Levin, JI; Diamantidis, G; Zapf, CW; Bloom, JD; Hu, YB; Powell, D; Wojciechowicz, D; Collins, K; Frommer, E,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6957-6961 , 文章类型： Article，,卷期：2009年19-24]
- A novel series of pyrazolo[1,5-a]pyrimidines bearing a 3-hydroxyphenyl group at C(3) and substituted tropanes at C(7) have been identified as potent B-Raf inhibitors. Exploration of alternative functional groups as a rep...
- Synthesis and evaluation of a thio analogue of duocarmycin SA
[作者：MacMillan, KS; Lajiness, JP; Cara, CL; Romagnoli, R; Robertson, WM; Hwang, I; Baraldi, PG; Boger, DL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6962-6965 , 文章类型： Article，,卷期：2009年19-24]
- The design, synthesis, and preliminary evaluation of methyl 1,2,8,8a-tetrahydrocyclopropa[c]thieno[3,2-e]indol-4-one-6-carboxylate (CTI) derivatives are detailed representing a single atom change (N to S) embedded in the...
- Terpenoids. III: Synthesis and biological evaluation of 23-hydroxybetulinic acid derivatives as novel inhibitors of glycogen phosphorylase
[作者：Zhu, PQ; Bi, Y; Xu, JY; Li, Z; Liu, J; Zhang, LY; Ye, WC; Wu, XM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6966-6969 , 文章类型： Article，,卷期：2009年19-24]
- A series of 23-hydroxybetulinic acid derivatives were prepared and tested in vitro as a new class of inhibitors of glycogen phosphorylase (GP). Within this series of compounds, 12b (IC50 = 3.5 mu M) is the most potent GP...
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