- An Hsp90 modulator that exhibits a unique mechanistic profile
[作者:Ramsey, DM; McConnell, JR; Alexander, LD; Tanaka, KW; Vera, CM; McAlpine, SR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3287-3290 , 文章类型: Article,,卷期:2012年22-9]
- Described is the synthesis of two biotinylated derivatives of a cytotoxic macrocycle. Pull-down assays indicate that this macrocycle targets the N-middle domain of Hsp90. Untagged compound can effectively compete away ta...
- Steroidal C-21 heteroaryl thioethers. Part 3: Pregn-4-eno-[3,2-c]pyrazole fused A ring modified steroids as selective glucocorticoid receptor modulators (dissociated steroids)
[作者:Biju, P; Wang, HW; Anthes, J; McCormick, K; Aslanian, R; Berlin, M; Bitar, R; Lim, YH; Lee, YJ; Prelusky, D; Mcleod, R; Jia, YL; Fernandez, X; Lieber, G; Jimenez, J; Eckel, S; House, A; Chapman, R; Phillips, J,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3291-3295 , 文章类型: Article,,卷期:2012年22-9]
- The introduction of A ring pyrazole modification to the hydrocortisone C-21 heteroaryl thioethers generated compounds with excellent transrepression potency (IL-8 inhibition) compared to their hydrocortisone analogs. How...
- X-ray crystallographic structure-based design of selective thienopyrazole inhibitors for interleukin-2-inducible tyrosine kinase
[作者:McLean, LR; Zhang, Y; Zaidi, N; Bi, XP; Wang, R; Dharanipragada, R; Jurcak, JG; Gillespy, TA; Zhao, ZC; Musick, KY; Choi, YM; Barrague, M; Peppard, J; Smicker, M; Duguid, M; Parkar, A; Fordham, J; Kominos, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3296-3300 , 文章类型: Article,,卷期:2012年22-9]
- Beginning with a screening hit, unique thienopyrazole-indole inhibitors of Itk (interleukin-2-inducible tyrosine kinase) were designed, synthesized, and crystallized in the target kinase. Although initial compounds were ...
- Isoquinoline derivatives as potent CRTH2 receptor antagonists: Synthesis and SAR
[作者:Nishikawa-Shimono, R; Sekiguchi, Y; Koami, T; Kawamura, M; Wakasugi, D; Watanabe, K; Wakahara, S; Matsumoto, K; Takayama, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3305-3310 , 文章类型: Article,,卷期:2012年22-9]
- Synthesis and structure-activity relationship of a novel series of isoquinoline CRTH2 receptor antagonists are described. One of the most potent compounds, TASP0376377 (6m), showed not only potent binding affinity (IC50 ...
- Discovery of an orally-bioavailable CC Chemokine Receptor 2 antagonist derived from an acyclic diaminoalcohol backbone
[作者:Carter, PH; Brown, GD; King, SR; Voss, ME; Tebben, AJ; Cherney, RJ; Mandlekar, S; Lo, YC; Yang, GJ; Miller, PB; Scherle, PA; Zhao, QH; Decicco, CP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3311-3316 , 文章类型: Article,,卷期:2012年22-9]
- We describe an isostere-driven approach to improve upon a previously-described series of capped dipeptide antagonists of CC Chemokine Receptor 2 (CCR2). Modification of the substitution around the isostere was combined w...
- Inhibition of platelet adhesion by peptidomimetics mimicking the interactive beta-hairpin of glycoprotein Ib alpha
[作者:Bernard, E; Buckley, V; Moman, E; Coleman, L; Meade, G; Kenny, D; Devocelle, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3323-3326 , 文章类型: Article,,卷期:2012年22-9]
- beta-Hairpin peptidomimetics mimicking the interaction sites of the platelet receptor glycoprotein (GP)Ib alpha with von Willebrand factor (vWF) were synthesised and evaluated for their ability to increase platelet veloc...
- Novel potent dual inhibitors of CK2 and Pim kinases with antiproliferative activity against cancer cells
[作者:Pierre, F; Regan, CF; Chevrel, MC; Siddiqui-Jain, A; Macalino, D; Streiner, N; Drygin, D; Haddach, M; O'Brien, SE; Rice, WG; Ryckman, DM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3327-3331 , 文章类型: Article,,卷期:2012年22-9]
- A novel family of potent dual inhibitors of CK2 and the Pim kinases was discovered by modifying the scaffolds of tricyclic Pim inhibitors. Several analogs were active at single digit nanomolar IC50 values against CK2 and...
- Penicacids A-C, three new mycophenolic acid derivatives and immunosuppressive activities from the marine-derived fungus Penicillium sp SOF07
[作者:Chen, ZM; Zheng, ZH; Huang, HB; Song, YX; Zhang, XL; Ma, JY; Wang, B; Zhang, CS; Ju, JH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3332-3335 , 文章类型: Article,,卷期:2012年22-9]
- Three new mycophenolic acid derivatives, penicacids A-C (1-3), together with two known analogues, mycophenolic acid (MPA, 4) and 4'-hydroxy-MPA (5), were isolated from a fungus Penicillium sp. SOF07 derived from a South ...
- Synthesis and inhibitory effect of piperine derivates on monoamine oxidase
[作者:Mu, LH; Wang, B; Ren, HY; Liu, P; Guo, DH; Wang, FM; Bai, L; Guo, YS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3343-3348 , 文章类型: Article,,卷期:2012年22-9]
- A series of piperine derivates (1-19) have been designed, synthesized and evaluated in vitro for their monoamine oxidase (MAO) A and B inhibitory activity and selectivity. It is worth noting that most of the small amine ...
- Substituted aminopyrimidine protein kinase B (PknB) inhibitors show activity against Mycobacterium tuberculosis
[作者:Chapman, TM; Bouloc, N; Buxton, RS; Chugh, J; Lougheed, KEA; Osborne, SA; Saxty, B; Smerdon, SJ; Taylor, DL; Whalley, D,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3349-3353 , 文章类型: Article,,卷期:2012年22-9]
- A high-throughput screen against PknB, an essential serine-threonine protein kinase present in Mycobacterium tuberculosis (M. tuberculosis), allowed the identification of an aminoquinazoline inhibitor which was used as a...
- Fused bicycles as arylketone bioisosteres leading to potent, orally active thiadiazole H3 antagonists
[作者:Xiao, D; Palani, A; Sofolarides, M; Aslanian, R; West, RE; Williams, SM; Wu, RL; Hwa, J; Sondey, C; Lachowicz, J; Korfmacher, WA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3354-3357 , 文章类型: Article,,卷期:2012年22-9]
- A structure-activity relationship study was undertaken to address the lack of oral exposure of the H3 antagonist 1, which incorporated an arylketone. Among a number of sub-series, the 4H-pyrido[1,2-a] pyrimidin-4-one ana...
- Blocking HIV-1 entry by a gp120 surface binding inhibitor
[作者:Tsou, LK; Chen, CH; Dutschman, GE; Cheng, YC; Hamilton, AD,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3358-3361 , 文章类型: Article,,卷期:2012年22-9]
- We report the mode of action of a proteomimetic compound that binds to the exterior surface of gp120 and blocks HIV-1 entry into cells. Using a one cycle time-of-addition study and antibody competition binding studies, w...
- Overcoming fluconazole resistance in Candida albicans clinical isolates with tetracyclic indoles
[作者:Youngsaye, W; Dockendorff, C; Vincent, B; Hartland, CL; Bittker, JA; Dandapani, S; Palmer, M; Whitesell, L; Lindquist, S; Schreiber, SL; Munoz, B,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:3362-3365 , 文章类型: Article,,卷期:2012年22-9]
- Continuing efforts to discover novel means of combating fluconazole resistance in Candida albicans have identified an indole derivative that sensitizes strains demonstrating resistance to fluconazole. This tetracycle (3,...
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