- Design of a fluorescence polarization assay platform for the study of human Hsp70
[作者:Kang, YL; Taldone, T; Clement, CC; Fewell, SW; Aguirre, J; Brodsky, JL; Chiosis, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3749-3751 , 文章类型: Article,,卷期:2008年18-13]
- The 70 kDa heat shock proteins (Hsp70) are molecular chaperones that assist in folding of newly synthesized polypeptides, refolding or denaturation of misfolded proteins, and translocation of proteins across biological m...
- Development of a novel fluorescent probe for fluorescence correlation spectroscopic detection of kinase inhibitors
[作者:Kawaguchi, M; Terai, T; Utata, R; Kato, M; Tsuganezawa, K; Tanaka, A; Kojima, H; Okabe, T; Nagano, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3752-3755 , 文章类型: Article,,卷期:2008年18-13]
- We have developed a fluorescently labeled probe for high-throughput screening of kinase inhibitors using fluorescence correlation spectroscopy. With this probe, we have successfully evaluated the inhibitory activities of...
- Chrobisiamone A, a new bischromone from Cassia siamea and a biomimetic transformation of 5-acetonyl-7-hydroxy-2-methylchromone into cassiarin A
[作者:Oshimi, S; Tomizawa, Y; Hirasawa, Y; Honda, T; Ekasari, W; Widyawaruyanti, A; Rudyanto, M; Indrayanto, G; Zaini, NC; Morita, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3761-3763 , 文章类型: Article,,卷期:2008年18-13]
- A new bischromone, chrobisiamone A (1) with an antiplasmodial activity has been isolated from the leaves of Cassia siamea and the structure was elucidated by 2D NMR analysis. Cyclization of 5-acetonyl-7-hydroxy-2-methylc...
- 2-Aminopropane-1,2,3-tricarboxylic acid: Synthesis and co-crystallization with the class A beta-lactamase BS3 of Bacillus licheniformis
[作者:Beck, J; Sauvage, E; Charlier, P; Marchand-Brynaert, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3764-3768 , 文章类型: Article,,卷期:2008年18-13]
- The title compound 4 has been prepared in four steps from ethylglycinate in 63% overall yield. This amino analog of citric acid has been co-crystallized with the class A beta-lactamase BS3 of Bacillus licheniformis and t...
- Synthesis and biological activities of reveromycin A and spirofungin A derivatives
[作者:Shimizu, T; Usui, T; Fujikura, M; Kawatani, M; Satoh, T; Machida, K; Kanoh, N; Woo, JT; Osada, H; Sodeoka, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3756-3760 , 文章类型: Article,,卷期:2008年18-13]
- Various derivatives of reveromycin A, an inhibitor of eukaryotic cell growth, and spirofungin A, focusing on the 5S hydroxyl group and C18 hemisuccinyl group, were synthesized and their inhibitory effects on both the iso...
- Pyrrolo[2,1-c][1,4]benzodiazepine-beta-glucuronide prodrugs with a potential for selective therapy of solid tumors by PMT and ADEPT strategies
[作者:Kamal, A; Tekumalla, V; Raju, P; Naidu, VGM; Diwan, PV; Sistla, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3769-3773 , 文章类型: Article,,卷期:2008年18-13]
- Pyrrolo[2,1-c][1,4]benzodiazepine-beta-glucuronide prodrugs 15a-b, with a potential for selective therapy of solid tumors by PMT and ADEPT have been designed, synthesized and evaluated for selective cytotoxicity in the p...
- Design, synthesis, and structure-activity relationship study of a novel class of ORL1 receptor antagonists based on N-biarylmethyl spiropiperidine
[作者:Yoshizumi, T; Miyazoe, H; Ito, H; Tsujita, T; Takahashi, H; Asai, M; Ozaki, S; Ohta, H; Okamoto, O,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3778-3782 , 文章类型: Article,,卷期:2008年18-13]
- Based on reported structures, a focused library of biarylmethyl bound to the nitrogen atom of spiropiperidine was designed. Systematic modi. cations allowed the discovery of a synthetically feasible and highly potent ORL...
- Sucutiniranes A and B, new cassane-type diterpenes from Bowdichia nitida
[作者:Matsuno, Y; Deguchi, J; Hirasawa, Y; Ohyama, K; Toyoda, H; Hirobe, C; Ekasari, W; Widyawaruyanti, A; Zaini, NC; Morita, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3774-3777 , 文章类型: Article,,卷期:2008年18-13]
- Two new cassane-type diterpenes, sucutiniranes A (1) and B (2), have been isolated from the seeds of Bowdichia nitida together with 6 alpha-acetoxyvouacapane (3) and 6 alpha,7 beta-diacetoxyvouacapane (4), and the struct...
- Synthesis and in vitro anti-hepatitis B virus activities of 4-aryl-6-chloroquinolin-2-one and 5-aryl-7-chloro-1,4-benzodiazepine derivatives
[作者:Cheng, P; Zhang, Q; Ma, YB; Jiang, ZY; Zhang, XM; Zhang, FX; Chen, JJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3787-3789 , 文章类型: Article,,卷期:2008年18-13]
- A series of 4-aryl-6-chloro-quinolin-2-ones and 5-aryl-7-chloro-1,4-benzodiazepine were synthesized and assayed for their in vitro anti-hepatitis B virus activities and cytotoxicities for the first time. Some of the test...
- Design, synthesis and evaluation of isaindigotone derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors
[作者:Pan, L; Tan, JH; Hou, JQ; Huang, SL; Gu, LQ; Huang, ZS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3790-3793 , 文章类型: Article,,卷期:2008年18-13]
- A series of isaindigotone derivatives 5a-d and 6a-d were designed, synthesized and evaluated as acetylcholinesterase and butyrylcholinesterase inhibitors. Results showed that the novel class of isaindigotone derivatives ...
- Preliminary in vivo evaluation of a novel Tc-99m-Labeled HYNIC-cys-annexin A5 as an apoptosis imaging agent
[作者:Fonge, H; Hubert, MD; Vunckx, K; Rattat, D; Nuyts, J; Bormans, G; Ni, YC; Reutelingsperger, C; Verbruggen, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3794-3798 , 文章类型: Article,,卷期:2008年18-13]
- A novel cys-annexin A5 with a single cysteine-residue at its concave side has been developed by site-directed mutagenesis to allow conjugation through thiol-chemistry without affecting its apoptotic cell binding properti...
- Effect of linkage geometry on biological activity in thiourea- and guanidine-substituted acridines and platinum-acridines
[作者:Ma, ZD; Saluta, G; Kucera, GL; Bierbach, U,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3799-3801 , 文章类型: Article,,卷期:2008年18-13]
- Novel thiourea- and guanidine-modified acridine-4-carboxamides (4, 7) and a corresponding platinum intercalator conjugate (4') have been synthesized and evaluated as cytotoxic agents in human promyelocytic leukemia, HL-6...
- Ring-closing metathesis for the synthesis of a highly G-quadruplex selective macrocyclic hexaoxazole having enhanced cytotoxic potency
[作者:Satyanarayana, M; Rzuczek, SG; LaVoie, EJ; Pilch, DS; Liu, A; Liu, LF; Rice, JE,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3802-3804 , 文章类型: Article,,卷期:2008年18-13]
- The synthesis of a 24-membered macrocyclic hexaoxazole via ring-closing metathesis is described. The target compound selectively stabilizes G-quadruplex DNA with no detectable stabilization of duplex DNA. An MTT cytotoxi...
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