- Synthesis and antifungal evaluation of pyrido[1,2-a]indole-1,4-diones and benzo[f]pyrido[1,2-a]indole-6,11-diones
[作者:Ryu, CK; Yoon, JH; Song, AL; Im, HA; Kim, JY; Kim, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:497-499 , 文章类型: Article,,卷期:2012年22-1]
- Pyrido[1,2-a]indole-1,4-diones and benzo[f]pyrido[1,2-a]indole-6,11-diones were synthesized and tested for in vitro antifungal activity against two pathogenic strains of fungi. Among them tested, many compounds showed go...
- Synthesis and antifungal activity of 6,7-bis(arylthio)-quinazoline-5,8-diones and furo[2,3-f]quinazolin-5-ols
[作者:Ryu, CK; Kim, YH; Im, HA; Kim, JY; Yoon, JH; Kim, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:500-503 , 文章类型: Article,,卷期:2012年22-1]
- 6,7-Bis(arylthio)-quinazoline-5,8-dione and furo[2,3-f]quinazolin-5-ol derivatives were synthesized and tested for in vitro antifungal activity against Candida, Aspergillus species, and Cryptococcus neoformans. Among the...
- Identification of oxazolidinediones and thiazolidinediones as potent 17 beta-hydroxysteroid dehydrogenase type 3 inhibitors
[作者:Harada, K; Kubo, H; Tanaka, A; Nishioka, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:504-507 , 文章类型: Article,,卷期:2012年22-1]
- Novel and potent inhibitors of 17 beta-hydroxysteroid dehydrogenase type 3 (17 beta-HSD3) were identified based on oxazolidinedione and thiazolidinedione derivatives, starting from a high-throughput screening hit, 5-(3-b...
- AChE inhibitor: A regio- and stereo-selective 1,3-dipolar cycloaddition for the synthesis of novel substituted 5,6-dimethoxy spiro[5.3 ']-oxindole-spiro-[6.3 '']-2,3-dihydro-1H-inden-1 ''-one-7-(substituted aryl)-tetrahydro-1H-pyrrolo[1,2-c][1,3]thiazole
[作者:Ali, MA; Ismail, R; Choon, TS; Kumar, RS; Osman, H; Arumugam, N; Almansour, AI; Elumalai, K; Singh, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:508-511 , 文章类型: Article,,卷期:2012年22-1]
- Pyrrolothiazolyloxindole analogues share vital pharmacological properties, considered useful in Alzheimer's disease (AD). The aim of this study was synthesis and evaluate pyralothiazolyloxindole analogues if possess acet...
- Antiangiogenic activity of 3,4-seco-cycloartane triterpenes from Thai Gardenia spp. and their semi-synthetic analogs
[作者:Pudhom, K; Nuanyai, T; Matsubara, K; Vilaivan, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:512-517 , 文章类型: Article,,卷期:2012年22-1]
- Twelve naturally occurring 3,4-seco-cycloartane triterpenes (1-12) isolated from Gardenia sootepensis and Gardenia obtusifolia, and eight semi-synthetic derivatives (13-20) were evaluated for their antiangiogenic activit...
- Design, synthesis, and activity evaluation of broad-spectrum small-molecule inhibitors of anti-apoptotic Bcl-2 family proteins: Characteristics of broad-spectrum protein binding and its effects on anti-tumor activity
[作者:Zheng, CH; Yang, H; Zhang, M; Lu, SH; Shi, D; Wang, J; Chen, XH; Ren, XH; Liu, J; Lv, JG; Zhu, J; Zhou, YJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:39-44 , 文章类型: Article,,卷期:2012年22-1]
- On the basis of the comparison of the structure of the Bim BH3: Bcl-x(L) complex and that of the ABT-737: Bcl-x(L) complex, a series of class A compounds were designed. These compounds had the basic skeleton of ABT-737 a...
- Synthesis and SAR of inhibitors of protein kinase CK2: Novel tricyclic quinoline analogs
[作者:Haddach, M; Pierre, F; Regan, CF; Borsan, C; Michaux, J; Stefan, E; Kerdoncuff, P; Schwaebe, MK; Chua, PC; Siddiqui-Jain, A; Macalino, D; Drygin, D; O'Brien, SE; Rice, WG; Ryckman, DM,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:45-48 , 文章类型: Article,,卷期:2012年22-1]
- Protein kinase CK2 is a potential drug target for many diseases including cancer and inflammation disorders. The crystal structure of clinical candidate CX-4945 1 with CK2 revealed an indirect interaction with the protei...
- New substituted C-19-andrographolide analogues with potent cytotoxic activities
[作者:Sirion, U; Kasemsook, S; Suksen, K; Piyachaturawat, P; Suksamrarn, A; Saeeng, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:49-52 , 文章类型: Article,,卷期:2012年22-1]
- Andrographolide, the major diterpenoid lactone from Andrographis paniculata, is toxic against cancer cells. In the present study, we investigated the structure-activity relationships (SARs) of 19 andrographolide analogue...
- The design, synthesis and in vitro immunosuppressive evaluation of novel isobenzofuran derivatives
[作者:Yang, N; Wang, QH; Wang, WQ; Wang, J; Li, F; Tan, SP; Cheng, MS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:53-56 , 文章类型: Article,,卷期:2012年22-1]
- The synthesis and biological evaluation of a series of novel isobenzofuran-based compounds are described. The compounds were evaluated for their immunosuppressive effects of T-cell proliferation and IMPDH type II inhibit...
- Synthesis, docking and in vitro antimalarial evaluation of bifunctional hybrids derived from beta-lactams and 7-chloroquinoline using click chemistry
[作者:Singh, P; Singh, P; Kumar, M; Gut, J; Rosenthal, PJ; Kumar, K; Kumar, V; Mahajan, MP; Bisetty, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:57-61 , 文章类型: Article,,卷期:2012年22-1]
- 1,2,3-Triazole tethered beta-lactam and 7-chloroquinoline bifunctional hybrids were synthesized and evaluated as potential antimalarial agents. Activity against cultured Plasmodium falciparum was dependent on the N-subst...
- Down-regulation of the human VEGF gene expression by perylene monoimide derivatives
[作者:Taka, T; Joonlasak, K; Huang, LM; Lee, TR; Chang, SWT; Tuntiwechapikul, W,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:518-522 , 文章类型: Article,,卷期:2012年22-1]
- The proximal promoter region of the human vascular endothelial growth factor (VEGF) gene contains a guanine-rich strand that can act as a transcriptional silencer by forming an intramolecular G-quadruplex. In this study,...
- (+/-)-2-(N-tert-Butylamino)-30-[I-125]-iodo-4 '-azidopropiophenone: A dopamine transporter and nicotinic acetylcholine receptor photoaffinity ligand based on bupropion (Wellbutrin, Zyban)
[作者:Lapinsky, DJ; Aggarwal, S; Nolan, TL; Surratt, CK; Lever, JR; Acharya, R; Vaughan, RA; Pandhare, A; Blanton, MP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:523-526 , 文章类型: Article,,卷期:2012年22-1]
- Towards addressing the knowledge gap of how bupropion interacts with the dopamine transporter (DAT) and nicotinic acetylcholine receptors (nAChRs), a ligand was synthesized in which the chlorine of bupropion was isosteri...
- Quinolinone-based agonists of S1P(1): Use of a N-scan SAR strategy to optimize in vitro and in vivo activity
[作者:Pennington, LD; Croghan, MD; Sham, KKC; Pickrell, AJ; Harrington, PE; Frohn, MJ; Lanman, BA; Reed, AB; Lee, MR; Xu, H; McElvain, M; Xu, Y; Zhang, XX; Fiorino, M; Horner, M; Morrison, HG; Arnett, HA; Fotsch, C; Tasker, AS; Wong, M; Cee, VJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:527-531 , 文章类型: Article,,卷期:2012年22-1]
- We reveal how a N-scan SAR strategy (systematic substitution of each CH group with a N atom) was employed for quinolinone-based S1P(1) agonist 5 to modulate physicochemical properties and optimize in vitro and in vivo ac...
- Lead optimisation of pyrazoles as novel FPR1 antagonists
[作者:Morley, AD; King, S; Roberts, B; Lever, S; Teobald, B; Fisher, A; Cook, T; Parker, B; Wenlock, M; Phillips, C; Grime, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:532-536 , 文章类型: Article,,卷期:2012年22-1]
- Optimisation of a series of pyrazole inhibitors of the human FPR1 receptor has been achieved. The use of an in vitro media loss assay was utilised to identify sub-series with more robust DMPK profiles. These were subsequ...
- Discovery, design and synthesis of novel potent and selective sphingosine-1-phosphate 4 receptor (S1P(4)-R) agonists
[作者:Guerrero, M; Urbano, M; Zhao, J; Crisp, M; Chase, P; Hodder, P; Schaeffer, MT; Brown, S; Rosen, H; Roberts, E,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:537-542 , 文章类型: Article,,卷期:2012年22-1]
- High affinity and selective small molecule agonists of the S1P(4) receptor (S1P(4)-R) may have significant therapeutic utility in diverse disease areas including autoimmune diseases, viral infections and thrombocytopenia...
- Virtual ligand screening of alpha-glucosidase: Identification of a novel potent noncarbohydrate mimetic inhibitor
[作者:Hakamata, W; Ishikawa, R; Ushijima, Y; Tsukagoshi, T; Tamura, S; Hirano, T; Nishio, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:62-64 , 文章类型: Article,,卷期:2012年22-1]
- 5-Thiazoleacetamide derivatives of AR122 and AR125 were screened as alpha-glucosidase inhibitors by in silico high-throughput screening from commercial drug-like small compound libraries. Inhibition of alpha-glucosidase ...
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