- Syntheses of structurally-simplified and fluorescently-labeled neovibsanin derivatives and analysis of their neurite outgrowth activity in PC12 cells
[作者:Imagawa, H; Saijo, H; Yamaguchi, H; Maekawa, K; Kurisaki, T; Yamamoto, H; Nishizawa, M; Oda, M; Kabura, M; Nagahama, M; Sakurai, J; Kubo, M; Nakai, M; Makino, K; Ogata, M; Takahashi, H; Fukuyama, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2089-2093 , 文章类型: Article,,卷期:2012年22-5]
- The syntheses of several neovibsanin derivatives were carried out in order to elucidate the simple structure required for displaying neurite outgrowth activity. In addition, a fluorescent probe molecule was synthesized a...
- Discovery of the first small molecule inhibitor of human DDX3 specifically designed to target the RNA binding site: Towards the next generation HIV-1 inhibitors
[作者:Radi, M; Falchi, F; Garbelli, A; Samuele, A; Bernardo, V; Paolucci, S; Baldanti, F; Schenone, S; Manetti, F; Maga, G; Botta, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2094-2098 , 文章类型: Article,,卷期:2012年22-5]
- Efficacy of currently approved anti-HIV drugs is hampered by mutations of the viral enzymes, leading invariably to drug resistance and chemotherapy failure. Recent data suggest that cellular co-factors also represent use...
- Towards the preparation of radiolabeled 1-aryl-3-benzyl ureas: Radiosynthesis of [C-11-carbonyl] AR-A014418 by [C-11]CO2 fixation
[作者:Hicks, JW; Wilson, AA; Rubie, EA; Woodgett, JR; Houle, S; Vasdev, N,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2099-2101 , 文章类型: Article,,卷期:2012年22-5]
- The highly selective glycogen synthase kinase-3 (GSK-3) inhibitor N-(4-methoxybenzyl)-N'-(5-nitro-1,3-thiazol-2-yl) urea (AR-A014418) was radiolabeled with carbon-11 (C-11; half-life = 20.4 min) at the urea moiety via [C...
- Methoxychalcone inhibitors of androgen receptor translocation and function
[作者:Kim, YS; Kumar, V; Lee, S; Iwai, A; Neckers, L; Malhotra, SV; Trepel, JB,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2105-2109 , 文章类型: Article,,卷期:2012年22-5]
- Androgen receptor activity drives incurable castrate-resistant prostate cancer. All approved antiandrogens inhibit androgen receptor-driven transcription, and in addition the second-generation antiandrogen MDV3100 inhibi...
- Adamantyl N-benzylbenzamide: New series of depigmentation agents with tyrosinase inhibitory activity
[作者:Baek, HS; Hong, YD; Lee, CS; Rho, HS; Shin, SS; Park, YH; Joo, YH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2110-2113 , 文章类型: Article,,卷期:2012年22-5]
- A new series of polyhydroxylated N-benzylbenzamide derivatives containing an adamantyl moiety has been synthesized, and the depigmenting and tyrosinase inhibitory activities of the molecules were evaluated. The lipophili...
- A resveratrol analog, phoyunbene B, induces G2/M cell cycle arrest and apoptosis in HepG2 liver cancer cells
[作者:Wang, GH; Guo, XY; Chen, HF; Lin, T; Xu, Y; Chen, QC; Liu, J; Zeng, JZ; Zhang, XK; Yao, XS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2114-2118 , 文章类型: Article,,卷期:2012年22-5]
- Among the seven natural resveratrol analogs separated and identified from Pholidota yunnanensis R-OLFE, we found phoyunbene B (PYB, trans-3,4'-dihydroxy-2',3',5-trimethoxystilbene) was more effective in inhibiting the gr...
- Discovery of 3,4-dihydropyrimidin-2(1H)-ones with inhibitory activity against HIV-1 replication
[作者:Kim, J; Park, C; Ok, T; So, W; Jo, M; Seo, M; Kim, Y; Sohn, JH; Park, Y; Ju, MK; Kim, J; Han, SJ; Kim, TH; Cechetto, J; Nam, J; Sommer, P; No, Z,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2119-2124 , 文章类型: Article,,卷期:2012年22-5]
- 3,4-Dihydropyrimidin-2(1H)-ones (DHPMs) were selected and derivatized through a HIV-1 replication assay based on GFP reporter cells. Compounds 14, 25, 31, and 36 exhibited significant inhibition of HIV-1 replication with...
- Potent mGluR5 antagonists: Pyridyl and thiazolyl-ethynyl-3,5-disubstituted-phenyl series (vol 21, pg 3243, 2011)
[作者:Alagille, D; DaCosta, H; Chen, YL; Hemstapat, K; Rodriguez, A; Baldwin, RM; Conn, PJ; Tamagnan, GD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2130-2130 , 文章类型: Correction,,卷期:2012年22-5]
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- Absolute configurations of tubulin inhibitors taltobulin (HTI-286) and HTI-042 characterized by X-ray diffraction analysis and NMR studies (vol 20, pg 1535, 2010)
[作者:Niu, CS; Ho, DM; Williamson, RT; Zask, A; Ayral-Kaloustian, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2131-2131 , 文章类型: Correction,,卷期:2012年22-5]
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