- Growth inhibitory activities of oxyprenylated and non-prenylated naturally occurring phenylpropanoids in cancer cell lines
[作者:Bruyere, C; Genovese, S; Lallemand, B; Ionescu-Motatu, A; Curini, M; Kiss, R; Epifano, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4174-4179 , 文章类型: Article,,卷期:2011年21-14]
- A series of 25 selected oxyprenylated natural phenylpropanoids were synthesized, and their growth inhibitory activities were evaluated in vitro together with 14 other commercially available non-alkylated compounds belong...
- Efficient synthesis of 3-O-thia-cPA and preliminary analysis of its biological activity toward autotaxin
[作者:Tanaka, R; Kato, M; Suzuki, T; Nakazaki, A; Nozaki, E; Gotoh, M; Murakami-Murofushi, K; Kobayashi, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4180-4182 , 文章类型: Article,,卷期:2011年21-14]
- The efficient synthesis of 3-O-thia-cPAs (4a-d), sulfur analogues of cyclic phosphatidic acid (cPA), has been achieved. The key step of the synthesis is an intramolecular Arbuzov reaction to construct the cyclic thiophos...
- A reverse method for diversity introduction of benzimidazole to synthesize H(+)/K(+)-ATP enzyme inhibitors
[作者:Yan, Y; Liu, ZJ; Zhang, JJ; Xu, RM; Hu, X; Liu, G,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4189-4192 , 文章类型: Article,,卷期:2011年21-14]
- A series of 2-[(2-pyridylmethyl)sulfinyl]benzimidazole derivatives were synthesized via a solution phase synthetic route using a reversal method of diversity introduction. Using this synthetic strategy, we obtained two k...
- Novel quinoxaline derivatives for in vivo imaging of beta-amyloid plaques in the brain
[作者:Cui, MC; Ono, M; Kimura, H; Liu, BL; Saji, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4193-4196 , 文章类型: Article,,卷期:2011年21-14]
- In a search for new probes to detect beta-amyloid plaques in the brain of patients with Alzheimer's disease (AD), we have synthesized and evaluated a series of quinoxaline derivatives containing a '6+6-6' ring system. Th...
- 7-Alkyl-N(2)-substituted-3-deazaguanines. Synthesis, DNA polymerase III inhibition and antibacterial activity
[作者:Xu, WC; Wright, GE; Brown, NC; Long, ZY; Zhi, CX; Dvoskin, S; Gambino, JJ; Barnes, MH; Butler, MM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4197-4202 , 文章类型: Article,,卷期:2011年21-14]
- Several 2-anilino- and 2-benzylamino-3-deaza-6-oxopurines [3-deazaguanines] and selected 8-methyl and 8-aza analogs have been synthesized. 7-Substituted N(2)-(3-ethyl-4-methylphenyl)-3-deazaguanines were potent and selec...
- Synthesis and evaluation of nitric oxide-releasing derivatives of 3-n-butylphthalide as anti-platelet agents
[作者:Li, Y; Wang, XL; Fu, R; Yu, WY; Wang, XL; Lai, YS; Peng, SX; Zhang, YH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4210-4214 , 文章类型: Article,,卷期:2011年21-14]
- Most ischemic stroke results from brain blood vessel blockage by platelet-mediated thrombus, and antiplatelet therapy has been demonstrated clinical benefits in the treatment of this disease. In the present work, novel n...
- Selective non zinc binding inhibitors of MMP13
[作者:De Savi, C; Morley, AD; Ting, A; Nash, I; Karabelas, K; Wood, CM; James, M; Norris, SJ; Karoutchi, G; Rankine, N; Hamlin, G; MacFaul, PA; Ryan, D; Baker, SV; Hargreaves, D; Gerhardt, S,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4215-4219 , 文章类型: Article,,卷期:2011年21-14]
- Directed screening has identified a novel series of MMP13 inhibitors that possess good levels of activity whilst possessing excellent selectivity over related MMPs. The binding mode of the series has been solved by co-cr...
- Eudistomidins H-K, new beta-carboline alkaloids from the Okinawan marine tunicate Eudistoma glaucus
[作者:Suzuki, T; Kubota, T; Kobayashi, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4220-4223 , 文章类型: Article,,卷期:2011年21-14]
- Four new beta-carboline alkaloids, eudistomidins H-K (1-4), were isolated from an Okinawan marine tunicate Eudistoma glaucus and the structures of 1-4 were elucidated on the basis of spectroscopic data. Eudistomidins H (...
- MAO inhibitory activity modulation: 3-Phenylcoumarins versus 3-benzoylcoumarins
[作者:Matos, MJ; Vazquez-Rodriguez, S; Uriarte, E; Santana, L; Vina, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4224-4227 , 文章类型: Article,,卷期:2011年21-14]
- With the aim of finding the structural features for the human MAO inhibitory activity and selectivity, in the present communication we report the synthesis, pharmacological evaluation and a comparative study of a new ser...
- Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights
[作者:Gradler, U; Fuchss, T; Ulrich, WR; Boer, R; Strub, A; Hesslinger, C; Anezo, C; Diederichs, K; Zaliani, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4228-4232 , 文章类型: Article,,卷期:2011年21-14]
- Inducible arginine oxidation and subsequent NO production by correspondent synthase (iNOS) are important cellular answers to proinflammatory signals. Prolonged NO production has been proved in higher organisms to cause s...
- Anti-leishmanial activity of disubstituted purines and related pyrazolo[4,3-d]pyrimidines
[作者:Jorda, R; Sacerdoti-Sierra, N; Voller, J; Havlicek, L; Kracalikova, K; Nowicki, MW; Nasereddin, A; Krystof, V; Strnad, M; Walkinshaw, MD; Jaffe, CL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4233-4237 , 文章类型: Article,,卷期:2011年21-14]
- We report here results of screening directed to finding new anti-leishmanial drugs among 2,6-disubstituted purines and corresponding 3,7-disubstituted pyrazolo[4,3-d]pyrimidines. These compounds have previously been show...
- Small molecule inhibitors of SHP2 tyrosine phosphatase discovered by virtual screening
[作者:Yu, ZH; Chen, L; Wu, L; Liu, SJ; Wang, L; Zhang, ZY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4238-4242 , 文章类型: Article,,卷期:2011年21-14]
- SHP2, encoded by PTPN11, is a non-receptor protein tyrosine phosphatase (PTP) containing two tandem Src homology-2 (SH2) domains. It is expressed ubiquitously and plays critical roles in growth factor mediated processes,...
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