- Benzothiazole-based N-(phenylsulfonyl)amides as a novel family of PPAR alpha antagonists
[作者:Ammazzalorso, A; Giancristofaro, A; D'Angelo, A; De Filippis, B; Fantacuzzi, M; Giampietro, L; Maccallini, C; Amoroso, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4869-4872 , 文章类型: Article,,卷期:2011年21-16]
- The discovery of PPAR antagonists is emerging as an useful tool for elucidating the biological role of the receptor. Here we report the identification of N-(phenylsulfonyl)amides containing the benzothiazole scaffold, a ...
- Novel hybrids of fluconazole and furanones: Design, synthesis and antifungal activity
[作者:Borate, HB; Sawargave, SP; Chavan, SP; Chandavarkar, MA; Iyer, R; Tawte, A; Rao, D; Deore, JV; Kudale, AS; Mahajan, PS; Kangire, GS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4873-4878 , 文章类型: Article,,卷期:2011年21-16]
- During our efforts to develop new antifungal agents, a number of hybrid molecules containing furanones and fluconazole pharmacophores were designed and synthesized. The new chemical entities thus synthesized were tested ...
- Discovery of 1,2,4-thiadiazolidine-3,5-dione analogs that exhibit unusual and selective rapid cell death kinetics against acute myelogenous leukemia cells in culture
[作者:Nasim, S; Guzman, ML; Jordan, CT; Crooks, PA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4879-4883 , 文章类型: Article,,卷期:2011年21-16]
- 4-Benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione (TDZD-8) was previously identified as an antileukemic agent exhibiting no evident toxicity toward normal hematopoietic cells. An SAR study has been carried out to examine...
- Carbonic anhydrase I and II activation with mono- and dihalogenated histamine derivatives
[作者:Saada, MC; Vullo, D; Montero, JL; Scozzafava, A; Winum, JY; Supuran, CT,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4884-4887 , 文章类型: Article,,卷期:2011年21-16]
- Mono- and dihalogenated histamine derivatives incorporating fluorine, chlorine and bromine have been prepared together with the corresponding boc-protected compounds at the aminoethyl group. They have been investigated a...
- 6-Aryl-3-pyrrolidinylpyridines as mGlu5 receptor negative allosteric modulators
[作者:Weiss, JM; Jimenez, HN; Li, GY; April, M; Uberti, MA; Bacolod, MD; Brodbeck, RM; Doller, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4891-4899 , 文章类型: Article,,卷期:2011年21-16]
- A series of 6-aryl-3-pyrrolidinylpyridine analogs was explored as structurally novel negative allosteric modulators of the mGlu5 receptor lacking an alkyne or oxadiazole moiety. Compounds in this series were characterize...
- Phosphopeptides with improved cellular uptake properties as ligands for the polo-box domain of polo-like kinase 1
[作者:Richter, S; Neundorf, I; Loebner, K; Graber, M; Berg, T; Bergmann, R; Steinbach, J; Pietzsch, J; Wuest, F,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4686-4689 , 文章类型: Article,,卷期:2011年21-16]
- Human polo-like kinase 1 (Plk1) is involved in cell proliferation and overexpressed in a broad variety of different cancer types. Due to its crucial role in cancerogenesis Plk1 is a potential target for diagnostic and th...
- Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase
[作者:Ducray, R; Simpson, I; Jung, FH; Nissink, JWM; Kenny, PW; Fitzek, M; Walker, GE; Ward, LT; Hudson, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4698-4701 , 文章类型: Article,,卷期:2011年21-16]
- We disclose a novel series of insulin-like growth factor-1 receptor kinase inhibitors based on the 3-(pyrimidin-4-yl)-imidazo[1,2-a]pyridine scaffold. The influence on the inhibitory activity of substitution on the imida...
- Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: Optimization of the aniline
[作者:Ducray, R; Jones, CD; Jung, FH; Simpson, I; Curwen, J; Pass, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4702-4704 , 文章类型: Article,,卷期:2011年21-16]
- Following the discovery of imidazopyridine 1 as a potent IGF-1R tyrosine kinase inhibitor, the aniline part has been modified with the aim to optimize the properties of this series. The structure-activity relationships a...
- Thrombin inhibitors with lipid peroxidation and lipoxygenase inhibitory activities
[作者:Ilic, M; Kontogiorgis, C; Hadjipavlou-Litina, D; Ilas, J; Kikelj, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4705-4709 , 文章类型: Article,,卷期:2011年21-16]
- Vascular oxidative stress, endothelial injury, and thrombosis are intertwined processes that display a synergistic pathological effect in many cardiovascular diseases. Antithrombotic therapy with anticoagulant and/or ant...
- Opioid delta(1) receptor antagonist 7-benzylidenenaltrexone as an effective resistance reverser for chloroquine-resistant Plasmodium chabaudi
[作者:Miyata, Y; Fujii, H; Osa, Y; Kobayashi, S; Takeuchi, T; Nagase, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:4710-4712 , 文章类型: Article,,卷期:2011年21-16]
- We evaluated antimalarial and/or chloroquine-resistance reversing effects of five opioid receptor antagonists. Although none of the evaluated compounds showed antimalarial effects, some of them, especially the delta(1) r...
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