- Immobilization of fluorous oligosaccharide recognized by influenza virus on polytetrafluoroethylene filter
[作者:Tojino, M; Mori, M; Kasuya, MCZ; Hatanaka, K; Kawaguchi, A; Nagata, K; Shirai, T; Mizuno, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1251-1254 , 文章类型: Article,,卷期:2012年22-2]
- The lactoside with PEG-fluorous tag was introduced to BHK-21(C-13) cells to generate a GM3-type oligosaccharide (Sia alpha 2-3Gal beta 1-4Glc). The GM3-type oligosaccharide obtained was easily immobilized by spotting ont...
- Lead Diversification 2: Application to P38, gMTP and lead compounds
[作者:Masood, MA; Bazin, M; Bunnage, ME; Calabrese, A; Cox, M; Fancy, SA; Farrant, E; Pearce, DW; Perez, M; Hitzel, L; Peakman, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1255-1262 , 文章类型: Article,,卷期:2012年22-2]
- Lead Diversification is a new technology platform developed at Pfizer for the functionalization of drug molecules using C-H activation. We describe its application to some drug programs such as P38 and gMTP and the devel...
- Small molecule inhibitors of BRAF in clinical trials
[作者:Zambon, A; Niculescu-Duvaz, I; Niculescu-Duvaz, D; Marais, R; Springer, CJ,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:789-792 , 文章类型: Article,,卷期:2012年22-2]
- Over the last few years, BRAF has emerged as a validated target in melanoma. This review summarises recent advances in the development of BRAF inhibitors, focussing on agents that have been assessed clinically. (C) 2011 ...
- Tricyclic 3,4-dihydropyrimidine-2-thione derivatives as potent TRPA1 antagonists
[作者:Gijsen, HJM; Berthelot, D; De Cleyn, MAJ; Geuens, I; Brone, B; Mercken, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:797-800 , 文章类型: Article,,卷期:2012年22-2]
- The transient receptor potential A1 (TRPA1) channel has been implicated in a number of inflammatory and nociceptive processes, and antagonists of the TRPA1 receptor could offer a potential treatment for conditions such a...
- Synthesis and evaluation of nitric oxide-releasing DDB derivatives as potential Pgp-mediated MDR reversal agents in MCF-7/Adr cells
[作者:Tang, XB; Gu, XK; Ai, H; Wang, GJ; Peng, H; Lai, YS; Zhang, YH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:801-805 , 文章类型: Article,,卷期:2012年22-2]
- Novel furoxan-based nitric oxide (NO)-releasing DDB derivatives (7a-j) were synthesized. Compounds 7i and 7j significantly reversed the resistance of MCF-7/Adr cells to doxorubicin in the combination treatment, and marke...
- Design, synthesis, and in vitro antiproliferative activity of novel Dasatinib derivatives
[作者:Cai, J; Zhang, SN; Zheng, M; Wu, XQ; Chen, JQ; Ji, M,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:806-810 , 文章类型: Article,,卷期:2012年22-2]
- Two series of novel Dasatinib derivatives have been designed and synthesized, with their in vitro cytostatic effect screened on human chronic myeloid leukemia cell line K562 and human myeloid leukemia cell line U937. Som...
- Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates
[作者:Fu, LQ; Liu, X; Ling, CY; Cheng, JJ; Guo, XS; He, HL; Ding, S; Yang, YS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:814-819 , 文章类型: Article,,卷期:2012年22-2]
- We report herein the design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates based on the structure of SB-222734. The antibacterial activities of these newly sy...
- Design and synthesis of 3,5-diarylpiperidin-2,6-diones as anticonvulsant agents
[作者:Babu, M; Pitchumani, K; Ramesh, P,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1263-1266 , 文章类型: Article,,卷期:2012年22-2]
- The present Letter describes a one-pot multi-component method that allows the efficient and mild preparation of 3,5-diphenylpiperidin-2,6-dione and a new series of 3,5-diarylpiperidin-2,6-dione derivatives from ethyl 2-a...
- AMG 837: A potent, orally bioavailable GPR40 agonist
[作者:Houze, JB; Zhu, LS; Sun, Y; Akerman, M; Qiu, W; Zhang, AJ; Sharma, R; Schmitt, M; Wang, YC; Liu, JW; Liu, JIA; Medina, JC; Reagan, JD; Luo, J; Tonn, G; Zhang, J; Lu, JYL; Chen, M; Lopez, E; Nguyen, K; Yang, L; Tang, L; Tian, H; Shuttleworth, SJ; Lin, DCH,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1267-1270 , 文章类型: Article,,卷期:2012年22-2]
- The discovery that certain long chain fatty acids potentiate glucose stimulated insulin secretion through the previously orphan receptor GPR40 sparked interest in GPR40 agonists as potential antidiabetic agents. Optimiza...
- Structure-based virtual screening approach to the discovery of novel PTPMT1 phosphatase inhibitors
[作者:Park, H; Kim, SY; Kyung, A; Yoon, TS; Ryu, SE; Jeong, DG,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1271-1275 , 文章类型: Article,,卷期:2012年22-2]
- Dual-specificity protein protein tyrosine phosphatase localized to mitochondrion 1 (PTPMT1) has recently proved to be a promising therapeutic target for the treatment of type II diabetes. Herein we report the first examp...
- Synthesis and biological evaluations of novel indenoisoquinolines as topoisomerase I inhibitors
[作者:Zhang, XY; Wang, RB; Zhao, L; Lu, N; Wang, JB; You, QD; Li, ZY; Guo, QL,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1276-1281 , 文章类型: Article,,卷期:2012年22-2]
- A series of novel indenoisoquinoline derivatives were synthesized. The anticancer activities of these molecules were tested in human cancer cell lines A549, HepG2, and HCT-116. These compounds were also tested for their ...
- New benzimidazole derivatives as antiplasmodial agents and plasmepsin inhibitors: Synthesis and analysis of structure-activity relationships
[作者:Saify, ZS; Azim, MK; Ahmad, W; Nisa, M; Goldberg, DE; Hussain, SA; Akhtar, S; Akram, A; Arayne, A; Oksman, A; Khan, IA,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1282-1286 , 文章类型: Article,,卷期:2012年22-2]
- The newly synthesized benzimidazole compounds were suggested to be inhibitors of Plasmodium falciparum plasmepsin II and human cathepsin D by virtual screening of an internal library of synthetic compounds. This was conf...
- Synthesis and biological evaluation of alpha, beta unsaturated lactones as potent immunosuppressive agents (vol 21 pg 5726, 2011)
[作者:Lee, SM; Lee, WG; Kim, YC; Ko, H,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:1287-1287 , 文章类型: Correction,,卷期:2012年22-2]
-
- Synthesis, pharmacological evaluation and docking studies of N-(benzo[d]thiazol-2-yl)-2-(piperazin-1-yl)acetamide analogs as COX-2 inhibitors
[作者:Raghavendra, NM; Jyothsna, A; Rao, AV; Subrahmanyam, CVS,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:820-823 , 文章类型: Article,,卷期:2012年22-2]
- The existing NSAIDs having number of toxicities emphasises the need for discovery of new non-toxic anti-inflammatory agents. In this Letter, we present the simple two step chemical synthesis, in vivo pharmacological scre...
|