- Discovery of N-aryl-9-oxo-9H-fluorene-1-carboxamides as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the carboxamide group
[作者：Kemnitzer, W; Sirisoma, N; Nguyen, B; Jiang, S; Kasibhatla, S; Crogan-Grundy, C; Tseng, B; Drewe, J; Cai, SX,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3045-3049 , 文章类型： Article，,卷期：2009年19-11]
- N-(2-Methylphenyl)-9-oxo-9H-fluorene-1-carboxamide (2a) was identified as a novel apoptosis inducer through our caspase- and cell-based high-throughput screening assay. Compound 2a was found to be active with sub-micromo...
- Orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors
[作者：Koltun, DO; Vasilevich, NI; Parkhill, EQ; Glushkov, AI; Zilbershtein, TM; Mayboroda, EI; Boze, MA; Cole, AG; Henderson, I; Zautke, NA; Brunn, SA; Chu, N; Hao, J; Mollova, N; Leung, K; Chisholm, JW; Zablocki, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3050-3053 , 文章类型： Article，,卷期：2009年19-11]
- We discovered a structurally novel SCD (Delta 9 desaturase) inhibitor 4a (CVT-11,563) that has 119 nM potency in a human cell-based (HEPG2) SCD assay and selectivity against Delta 5 and Delta 6 desaturases. This compound...
- Application of combinatorial biocatalysis for a unique ring expansion of dihydroxymethylzearalenone
[作者：Rich, JO; Budde, CL; McConeghey, LD; Cotterill, IC; Mozhaev, VV; Singh, SB; Goetz, MA; Zhao, A; Michels, PC; Khmelnitsky, YL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3059-3062 , 文章类型： Article，,卷期：2009年19-11]
- Combinatorial biocatalysis was applied to generate a diverse set of dihydroxymethylzearalenone analogs with modified ring structure. In one representative chemoenzymatic reaction sequence, dihydroxymethylzearalenone was ...
- Aryl sulfonamido tetralin inhibitors of the Kv1.5 ion channel
[作者：Gross, MF; Castle, NA; Zou, AR; Wickenden, AD; Yu, WF; Spear, KL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3063-3066 , 文章类型： Article，,卷期：2009年19-11]
- Aryl sulfonamido tetralins based on lead compound 2a were synthesized and evaluated for Kv1.5 inhibitory activity. Several compounds having IC50 values less then 0.1 mu M were identified. Kv1.5 inhibitors have the potent...
- Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists
[作者：Suzuki, T; Moriya, M; Sakamoto, T; Suga, T; Kishino, H; Takahashi, H; Ishikawa, M; Nagai, K; Imai, Y; Sekino, E; Ito, M; Iwaasa, H; Ishihara, A; Tokita, S; Kanatani, A; Sato, N; Fukami, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3072-3077 , 文章类型： Article，,卷期：2009年19-11]
- Optimization of high-throughput screening hit 1a led to the identification of a novel spiro-piperidine class of melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. Compound 3c was identified as a highly potent...
- Novel carbazole and acyl-indole antimitotics
[作者：Barta, TE; Barabasz, AF; Foley, BE; Geng, LF; Hall, SE; Hanson, GJ; Jenks, M; Ma, W; Rice, JW; Veal, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3078-3080 , 文章类型： Article，,卷期：2009年19-11]
- In the course of our Heat Shock 90 program, certain carbazole compounds were identified which had an off-target antiproliferative activity. To understand the off-target activity, we studied one analog with strong activit...
- Histone deacetylase inhibitors with a primary amide zinc binding group display antitumor activity in xenograft model
[作者：Attenni, B; Ontoria, JM; Cruz, JC; Rowley, M; Schultz-Fademrecht, C; Steinkuhler, C; Jones, P,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3081-3084 , 文章类型： Article，,卷期：2009年19-11]
- Histone deacetylase (HDAC) inhibition causes hyperacetylation of histones leading to differentiation, growth arrest and apoptosis of malignant cells, representing a new strategy in cancer therapy. Many of the known HDAC ...
- Regioselective preparation of 5-hydroxypropranolol and 4 '-hydroxydiclofenac with a fungal peroxygenase
[作者：Kinne, M; Poraj-Kobielska, M; Aranda, E; Ullrich, R; Hammel, KE; Scheibner, K; Hofrichter, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3085-3087 , 文章类型： Article，,卷期：2009年19-11]
- An extracellular peroxygenase of Agrocybe aegerita catalyzed the H2O2-dependent hydroxylation of the multi-function beta-adrenergic blocker propranolol (1-naphthalen-1-yloxy-3-(propan-2-ylamino)propan-2-ol) and the non-s...
- Synthesis of phenylisothiourea derivatives as inhibitors of NO production in LPS activated macrophages
[作者：Jin, GH; Lee, DY; Cheon, YJ; Gim, HJ; Kim, DH; Kim, HD; Ryu, JH; Jeon, R,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3088-3092 , 文章类型： Article，,卷期：2009年19-11]
- A series of phenylisothioureas were synthesized as inhibitors of NO production in lipopolysaccharide-activated macrophages. We investigated the effect of lipophilic moiety and N- or S-substituents of the phenylisothioure...
- (S)-Camphorsulfonic acid catalyzed highly stereoselective synthesis of pseudoglycosides
[作者：Gorityala, BK; Cai, ST; Ma, JM; Liu, XW,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3093-3095 , 文章类型： Article，,卷期：2009年19-11]
- A mild and efficient synthesis of pseudoglycosides has been developed using metal free (S)-camphorsulfonic acid. (S)-CSA acts as an excellent catalyst for conversion of 2,4,6-tri-O-acetyl-D-glucal to 2,3-unsaturated O-gl...
- 2-Cyclohexylcarbonylbenzimidazoles as potent, orally available and brain-penetrable opioid receptor-like 1 (ORL1) antagonists
[作者：Kobayashi, K; Uchiyama, M; Takahashi, H; Kawamoto, H; Ito, S; Yoshizumi, T; Nakashima, H; Kato, T; Shimizu, A; Yamamoto, I; Asai, M; Miyazoe, H; Ohno, A; Hirayama, M; Ozaki, S; Tani, T; Ishii, Y; Tanaka, T; Mochidome, T; Tadano, K; Fukuroda, T; Ohta, H; Okamoto, O,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3096-3099 , 文章类型： Article，,卷期：2009年19-11]
- The synthesis and biological evaluation of new potent opioid receptor-like 1 (ORL1) antagonists are presented. Conversion of the thioether linkage of the prototype [It is reported prior to this communication as a consecu...
- Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity
[作者：Kobayashi, K; Kato, T; Yamamoto, I; Shimizu, A; Mizutani, S; Asai, M; Kawamoto, H; Ito, S; Yoshizumi, T; Hirayama, M; Ozaki, S; Ohta, H; Okamoto, O,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3100-3103 , 文章类型： Article，,卷期：2009年19-11]
- A structure-activity relationship (SAR) study on the benzimidazole series of opioid receptor-like 1 (ORL1) antagonists related to 1 is described. Optimization of 1 by introduction of a hydrophilic substituent into the th...
- A simple method for monitoring protein-DNA interactions
[作者：Fulop, A; Arian, D; Lysenko, A; Mokhir, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3104-3107 , 文章类型： Article，,卷期：2009年19-11]
- A simple, efficient and cheap method is reported for monitoring interactions between single stranded desoxyribonucleic acids and proteins, using fluorescence spectroscopy and complexes of 5'-dye-DNA conjugates with bovin...
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