- Synthesis and preliminary evaluation of neuroprotection of celastrol analogues in PC12 cells
[作者:Sun, HL; Xu, LP; Yu, P; Jiang, J; Zhang, GX; Wang, YQ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3844-3847 , 文章类型: Article,,卷期:2010年20-13]
- A series of celastrol analogues were synthesized, and their neuroprotective effect against t-BHP-induced cytotoxicity was investigated in neuronal PC12 cells. Their effects on Hsp70 protein expression were quantified by ...
- Inhibition of ABCG2-mediated drug efflux by naphthopyrones from marine crinoids
[作者:Bokesch, HR; Cartner, LK; Fuller, RW; Wilson, JA; Henrich, CJ; Kelley, JA; Gustafson, KR; McMahon, JB; McKee, TC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3848-3850 , 文章类型: Article,,卷期:2010年20-13]
- Five new naphthopyrones (1-5) along with the known compounds TMC-256A1, 5,8-dihydroxy-6-methoxy-2-propyl-4H-naphtho[2,3-b]pyran-4-one, TMC-256C1, comaparvin, 6-methoxycomaparvin, and 6-methoxycomaparvin 5-methyl ether (6...
- Activity of substituted thiophene sulfonamides against malarial and mammalian cyclin dependent protein kinases
[作者:Caridha, D; Kathcart, AK; Jirage, D; Waters, NC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3863-3867 , 文章类型: Article,,卷期:2010年20-13]
- Cyclin dependent protein kinases (CDKs) are pursued as drug targets for several eukaryotic pathogens. In this study, we identified thiophene and benzene sulfonamides as potent inhibitors of Pfmrk, a Plasmodium falciparum...
- Synthesis and evaluation of novel phosphate ester analogs as neutral sphingomyelinase inhibitors
[作者:Imagawa, H; Oda, M; Takemoto, T; Yamauchi, R; Yoshikawa, T; Yamamoto, H; Nishizawa, M; Takahashi, H; Hashimoto, M; Yabiku, K; Nagahama, M; Sakurai, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3868-3871 , 文章类型: Article,,卷期:2010年20-13]
- A novel sphingomyelin inhibitor RY221B-a, which contains a bipyridyl moiety as a metal coordination site was designed based upon the mechanism of phosphate ester hydrolysis. RY221B-a was synthesized from N-Boc-sphingosin...
- Inhibitors for expression of IgE receptor on human mast cell from Puerariae Flos
[作者:Tamura, S; Yoshihira, K; Tokumaru, M; Xu, ZS; Murakami, N,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3872-3875 , 文章类型: Article,,卷期:2010年20-13]
- Bioassay-guided separation of the extract of the medicinal plant, Puerariae Flos, disclosed the two isoflavones tectorigenin (1) and genistein (2) as the inhibitors for expression of IgE receptor (Fc epsilon RI), the key...
- Synthesis of novel beta-carbolines with efficient DNA-binding capacity and potent cytotoxicity
[作者:Chen, ZY; Cao, RH; Shi, BX; Yi, W; Yu, LA; Song, HC; Ren, ZH; Peng, WL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3876-3879 , 文章类型: Article,,卷期:2010年20-13]
- A series of water-soluble beta-carbolines, bearing a flexible amino side chain, was prepared and evaluated in vitro against a panel of human tumor cell lines. The N-9-arylated alkyl substituted beta-carbolines represente...
- Cell cycle arrest and cytochrome c-mediated apoptotic induction by MCS-5A is associated with up-regulation of p16(INK4a) in HL-60 cells
[作者:Choi, BY; Lee, CH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3880-3884 , 文章类型: Article,,卷期:2010年20-13]
- MCS-5A, an analog of sangivamycin, selectively inhibits the cyclin-dependent kinases CDK1 and 4 in HL60 cells in vitro (IC50: 9.6 and 8.8 mu M, respectively), while weakly inhibiting other housekeeping protein kinases. M...
- Development of dual functional SPECT/fluorescent probes for imaging cerebral beta-amyloid plaques
[作者:Ono, M; Ishikawa, M; Kimura, H; Hayashi, S; Matsumura, K; Watanabe, H; Shimizu, Y; Cheng, Y; Cui, MC; Kawashima, H; Saji, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3885-3888 , 文章类型: Article,,卷期:2010年20-13]
- he imaging of beta-amyloid (A beta) aggregates in the brain may lead to the early detection of Alzheimer's disease (AD) and monitoring of the progression and effectiveness of treatment. The purpose of this study was to d...
- A novel synthesis of 3-aryl coumarins and evaluation of their antioxidant and lipoxygenase inhibitory activity
[作者:Roussaki, M; Kontogiorgis, CA; Hadjipavlou-Litina, D; Hamilakis, S; Detsi, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3889-3892 , 文章类型: Article,,卷期:2010年20-13]
- A series of coumarin analogues bearing a substituted phenyl ring on position 3 were synthesized via a novel methodology, through an intermolecular condensation reaction of 2-hydroxyacetophenones and 2-hydroxybenzaldehyde...
- Novel pyridobenzimidazole derivatives exhibiting antifungal activity by the inhibition of beta-1,6-glucan synthesis
[作者:Takeshita, H; Watanabe, J; Kimura, Y; Kawakami, K; Takahashi, H; Takemura, M; Kitamura, A; Someya, K; Nakajima, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3893-3896 , 文章类型: Article,,卷期:2010年20-13]
- Based on the HTS hit compound 1a, an inhibitor of beta-1,6-glucan synthesis, we synthesized novel pyridobenzimidazole derivatives and evaluated their antifungal activity. Among the compounds synthesized, we identified th...
- Design and synthesis of benzoazepin-2-one analogs as allosteric binders targeting the PIF pocket of PDK1
[作者:Wei, LY; Gao, XQ; Warne, R; Hao, XS; Bussiere, D; Gu, XJ; Uno, T; Liu, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3897-3902 , 文章类型: Article,,卷期:2010年20-13]
- A novel series of benzoazepin-2-ones were designed and synthesized targeting the PIF pocket of AGC protein kinases, among which a series of thioether-linked benzoazepin-2-ones were discovered to bind to the PIF pocket of...
- 2-Aryl-4,5,6,7-tetrahydro-1,3-benzothiazol-7-ols as a class of antitumor agents selectively active in securin(-/-) cells
[作者:Zhang, N; Ayral-Kaloustian, S; Niu, CS; Nguyen, T; Upeslacis, E; Mansour, TS; Ragunathan, S; Rosfjord, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3903-3905 , 文章类型: Article,,卷期:2010年20-13]
- A series of 2-(4-aminophenyl)-4,5,6,7-tetrahydro-1,3-benzothiazol-7-ols have been developed as antitumor agents that showed high selectivity against aneuploid cell lines (vs diploid cell lines). Structure-activity relati...
- Design, synthesis and anticancer activity of piperazine hydroxamates and their histone deacetylase (HDAC) inhibitory activity
[作者:Chetan, B; Bunha, M; Jagrat, M; Sinha, BN; Saiko, P; Graser, G; Szekeres, T; Raman, G; Rajendran, P; Moorthy, D; Basu, A; Jayaprakash, V,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3906-3910 , 文章类型: Article,,卷期:2010年20-13]
- Six compounds were synthesized with piperazine in linker region and hydroxamate as Zinc Binding Group ( ZBG). They were screened against three cancer cell-lines (NCIH460; HCT116; U251). Compounds 5c and 5f with GI(50) va...
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