- Analogs of a 4-aminothieno[2,3-d]pyrimidine lead (QB13) as modulators of P-glycoprotein substrate specificity
[作者:Hacker, HG; de la Haye, A; Sterz, K; Schnakenburg, G; Wiese, M; Gutschow, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6102-6105 , 文章类型: Article,,卷期:2009年19-21]
- P-glycoprotein (P-gp) is an important factor in the development of multidrug resistance (MDR) in cancer cells. In literature reports, a thieno[ 2,3-d] pyrimidine (QB13) was described as P-gp modulator and opposed effects...
- Benzoxazole piperidines as selective and potent somatostatin receptor subtype 5 antagonists
[作者:Martin, RE; Mohr, P; Maerki, HP; Guba, W; Kuratli, C; Gavelle, O; Binggeli, A; Bendels, S; Alvarez-Sanchez, R; Alker, A; Polonchuk, L; Christ, AD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6106-6113 , 文章类型: Article,,卷期:2009年19-21]
- SAR studies of a recently described SST5R selective benzoxazole piperidine lead series are described with particular focus on the substitution pattern on the benzyl and benzoxazole side-chains. Introduction of a second m...
- Pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione derivatives: Their cytoprotection effect from rotenone toxicity and preliminary DMPK properties
[作者:Zhou, YF; Liu, G; Chen, JH; Reddy, PSMM; Yoon, IS; Zhang, MH; Zhang, B; Barber, JR; Ng, SC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6114-6118 , 文章类型: Article,,卷期:2009年19-21]
- Pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione derivatives exhibited potent cytoprotective effect from rotenone toxicity. Lead optimization focused on the CC50/EC50 ratio and DMPK properties led to the overall improveme...
- Discovery of novel sphingosine kinase 1 inhibitors
[作者:Xiang, YB; Asmussen, G; Booker, M; Hirth, B; Kane, JL; Liao, JK; Noson, KD; Yee, C,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6119-6121 , 文章类型: Article,,卷期:2009年19-21]
- Sphingosine kinase 1 (SK1) is an important enzyme that regulates the balance between ceramide and sphingosine-1-phosphate (S1P). Potent and novel SK1 inhibitors (6ag, 9ab and 12aa) have been discovered through a series o...
- Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors
[作者:Qiao, LX; Choi, S; Case, A; Gainer, TG; Seyb, K; Glicksman, MA; Lo, DC; Stein, RL; Cuny, GD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6122-6126 , 文章类型: Article,,卷期:2009年19-21]
- A structure-activity relationship study for a 2-chloroanilide derivative of pyrazolo[1,5-a]pyridine revealed that increased EphB3 kinase inhibitory activity could be accomplished by retaining the 2-chloroanilide and intr...
- Pyrazole-based cathepsin S inhibitors with arylalkynes as P1 binding elements
[作者:Ameriks, MK; Axe, FU; Bembenek, SD; Edwards, JP; Gu, Y; Karlsson, L; Randal, M; Sun, SQ; Thurmond, RL; Zhu, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6131-6134 , 文章类型: Article,,卷期:2009年19-21]
- A crystal structure of 1 bound to a Cys25Ser mutant of cathepsin S helped to elucidate the binding mode of a previously disclosed series of pyrazole-based CatS inhibitors and facilitated the design of a new class of aryl...
- Pyrazole-based arylalkyne cathepsin S inhibitors. Part II: Optimization of cellular potency
[作者:Ameriks, MK; Cai, H; Edwards, JP; Gebauer, D; Gleason, E; Gu, Y; Karlsson, L; Nguyen, S; Sun, SQ; Thurmond, RL; Zhu, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6135-6139 , 文章类型: Article,,卷期:2009年19-21]
- Basic lipophilic substituents dramatically improved the cellular potency of a previously disclosed series of pyrazole-based arylalkyne cathepsin S inhibitors. The incorporation of substituted benzylamines in the para pos...
- Puupehanol, a sesquiterpene-dihydroquinone derivative from the marine sponge Hyrtios sp.
[作者:Xu, WH; Ding, YQ; Jacob, MR; Agarwal, AK; Clark, AM; Ferreira, D; Liang, ZS; Li, XC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6140-6143 , 文章类型: Article,,卷期:2009年19-21]
- Puupehanol (1), a new sesquiterpene-dihydroquinone derivative, was isolated from the marine sponge Hyrtios sp., along with the known compounds puupehenone (2) and chloropuupehenone (3) that are responsible for the antifu...
- Piperazinyl-glutamate-pyrimidines as potent P2Y(12) antagonists for inhibition of platelet aggregation
[作者:Parlow, JJ; Burney, MW; Case, BL; Girard, TJ; Hall, KA; Hiebsch, RR; Huff, RM; Lachance, RM; Mischke, DA; Rapp, SR; Woerndle, RS; Ennis, MD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6148-6156 , 文章类型: Article,,卷期:2009年19-21]
- Piperazinyl-glutamate-pyrimidines were prepared with oxygen, nitrogen, and sulfur substitution at the 4-position of the pyrimidine leading to highly potent P2Y(12) antagonists. In particular, 4-substituted piperidine-4-p...
- Discovery of 4-functionalized phenyl-O-beta-D-glycosides as a new class of mushroom tyrosinase inhibitors
[作者:Yi, W; Cao, RH; Wen, H; Yan, Q; Zhou, BH; Ma, L; Song, HC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6157-6160 , 文章类型: Article,,卷期:2009年19-21]
- A series of 4-functionalized phenyl-O-beta-D-glycosides were designed, synthesized and evaluated as a new class of mushroom tyrosinase inhibitors. The results demonstrated that compounds 6a-13a bearing a thiosemicarbazid...
- Thiazolidinedione derivatives as PTP1B inhibitors with antihyperglycemic and antiobesity effects
[作者:Bhattarai, BR; Kafle, B; Hwang, JS; Khadka, D; Lee, SM; Kang, JS; Ham, SW; Han, IO; Park, H; Cho, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6161-6165 , 文章类型: Article,,卷期:2009年19-21]
- Benzylidene-2,4-thiazolidinedione derivatives with substitutions on the phenyl ring at the ortho or para positions of the thiazolidinedione (TZD) group were synthesized as PTP1B inhibitors with IC50 values in a low micro...
- Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: In vitro profiling and in vivo evaluation
[作者:Semple, G; Tran, TA; Kramer, B; Hsu, D; Han, S; Choi, J; Vallar, P; Casper, MD; Zou, N; Hauser, EK; Thomsen, W; Whelan, K; Sengupta, D; Morgan, M; Sekiguchi, Y; Kanuma, K; Chaki, S; Grottick, AJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6166-6171 , 文章类型: Article,,卷期:2009年19-21]
- A series of pyrimidine analogues derived from ATC0175 were potent antagonists of human MCH-R1 in vitro. Significantly improved receptor selectivity was achieved with several analogues from this series, but no improvement...
- New inhibitors of the complement system inspired in K76-COOH. A SAR study of filifolinol derivatives through modifications of the C3 ' position
[作者:Larghi, EL; Operto, MA; Torres, R; Kaufman, TS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6172-6175 , 文章类型: Article,,卷期:2009年19-21]
- A new series of tricyclic carboxylic acids with a 3H-spiro[benzofuran-2,10-cyclohexane] skeleton were synthesized from filifolinol, as analogs of the natural complement inhibitor K76-COOH. Their complement inhibitory act...
- Synthesis and structure-activity relationships of 2-(1,4 '-bipiperidin-1 '-yl)thiazolopyridine as H-3 receptor antagonists
[作者:Rao, AU; Palani, A; Chen, X; Huang, Y; Aslanian, RG; West, RE; Williams, SM; Wu, RL; Hwa, J; Sondey, C; Lachowicz, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:6176-6180 , 文章类型: Article,,卷期:2009年19-21]
- A series of 2-(1,4'-bipiperidine-1'-yl)thiazolopyridines was synthesized and evaluated as a new lead of non-imidazole histamine H-3 receptor antagonists. Introduction of diversity at the 6-position of the pyridine ring w...
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