- Synthesis and biological evaluation of new potent and selective HCV NS5A inhibitors
[作者：Shi, JX; Zhou, LH; Amblard, F; Bobeck, DR; Zhang, HW; Liu, P; Bondada, L; McBrayer, TR; Tharnish, PM; Whitaker, T; Coats, SJ; Schinazi, RF,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3488-3491 , 文章类型： Article，,卷期：2012年22-10]
- NS5A inhibitors are a new class of direct-acting antiviral agents which display very potent anti-HCV activity in vitro and in humans. Rationally designed modifications to the central biphenyl linkage of a known NS5A seri...
- Crystal structures of AKR1C3 containing an N-(aryl)amino-benzoate inhibitor and a bifunctional AKR1C3 inhibitor and androgen receptor antagonist. Therapeutic leads for castrate resistant prostate cancer
[作者：Chen, M; Adeniji, AO; Twenter, BM; Winkler, JD; Christianson, DW; Penning, TM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3492-3497 , 文章类型： Article，,卷期：2012年22-10]
- Castrate resistant prostate cancer (CRPC) is associated with increased androgen receptor (AR) signaling often brought about by elevated intratumoral androgen biosynthesis and AR amplification. Inhibition of androgen bios...
- The central valine concept provides an entry in a new class of non peptide inhibitors of the p53-MDM2 interaction
[作者：Furet, P; Chene, P; De Pover, A; Valat, TS; Lisztwan, JH; Kallen, J; Masuya, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3498-3502 , 文章类型： Article，,卷期：2012年22-10]
- Disrupting the interaction between the p53 tumor suppressor and its regulator MDM2 is a promising therapeutic strategy in anticancer drug research. In our search for non peptide inhibitors of this protein-protein interac...
- Serendipity in discovery of proteasome inhibitors
[作者：Dunn, D; Iqbal, M; Husten, J; Ator, MA; Chatterjee, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3503-3505 , 文章类型： Article，,卷期：2012年22-10]
- Among its various catalytic activities, the 'chymotrypsin-like' activity of the proteasome, a large multicatalytic proteinase complex has emerged as the focus of drug discovery efforts in cancer therapy. Herein, a series...
- Structure-activity relationship in the antitumor activity of 6-, 8- or 6,8-substituted 3-benzylamino-beta-carboline derivatives
[作者：Ikeda, R; Kimura, T; Tsutsumi, T; Tamura, S; Sakai, N; Konakahara, T,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3506-3515 , 文章类型： Article，,卷期：2012年22-10]
- We synthesized 47 kinds of 3-amino- or 3-benzylamino-beta-carboline derivatives with a substituent on the 6-, 8-, or 6,8-carbon atoms and evaluated their antitumor activities for Hela S-3 and Sarcoma 180 cell lines using...
- Long-acting peptidomimetics based DPP-IV inhibitors
[作者：Jadav, P; Bahekar, R; Shah, SR; Patel, D; Joharapurkar, A; Kshirsagar, S; Jain, M; Shaikh, M; Sairam, KVVM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3516-3521 , 文章类型： Article，,卷期：2012年22-10]
- Pyrrolidine based peptidomimetics are reported as potent and selective DPP-IV inhibitors for the treatment of T2DM. Compounds 16c and 16d showed excellent in vitro potency and selectivity towards DPP-IV and the lead comp...
- Novel desosamine-modified 14- and 15-membered macrolides without antibacterial activity
[作者：Jakopovic, IP; Krajacic, MB; Skugor, MM; Stimac, V; Pesi, D; Vujasinovic, I; Alihodzic, S; Paljetak, HC; Kragol, G,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3527-3530 , 文章类型： Article，,卷期：2012年22-10]
- Novel modifications of the desosamine sugar of 14- and 15-membered antibacterial macrolides, in which the desosamine was fused with N-substituted-1,3-oxazolidin-2-ones, were developed in order to completely suppress anti...
- The discovery of 2-fluoro-N-(3-fluoro-4-(5-((4-morpholinobutyl)amino)-1,3,4-oxadiazol-2-yl)phenyl)benzamide, a full agonist of the alpha-7 nicotinic acetylcholine receptor showing efficacy in the novel object recognition model of cognition enhancement
[作者：Skidmore, J; Atcha, Z; Boucherat, E; Castelletti, L; Chen, DW; Coppo, FT; Cutler, L; Dunsdon, RM; Heath, BM; Hutchings, R; Hurst, DN; Javed, S; Martin, S; Maskell, ESL; Norton, D; Pemberton, DJ; Redshaw, S; Rutter, R; Sehmi, SS; Scoccitti, T; Temple, HE; Theobald, P; Ward, RW; Wilson, DM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3531-3534 , 文章类型： Article，,卷期：2012年22-10]
- A series of alpha 7 nicotinic acetylcholine receptor full agonists with a 1,3,4-oxadiazol-2-amine core has been discovered. Early lead 1 was found to have a limited therapeutic index with respect to its potential for car...
- Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds
[作者：Ortar, G; Morera, L; Moriello, AS; Morera, E; Nalli, M; Di Marzo, V; De Petrocellis, L,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3535-3539 , 文章类型： Article，,卷期：2012年22-10]
- A series of thirty-three thymol, p-cymene-3-carboxylic acid, and 3-amino-p-cymene derivatives was synthesized and tested on TRPA1, TRPM8, and TRPV3 channels. Most of them acted as strong modulators of TRPA1, TRPM8, and T...
- Substrate specificity of galactokinase from Streptococcus pneumoniae TIGR4 towards galactose, glucose, and their derivatives
[作者：Zou, Y; Wang, WJ; Cai, L; Chen, LL; Xue, MY; Zhang, XM; Shen, J; Chen, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3540-3543 , 文章类型： Article，,卷期：2012年22-10]
- Galactokinases (GalKs) have attracted significant research attention for their potential applications in the enzymatic synthesis of unique sugar phosphates. The galactokinase (GalKSpe4) cloned from Streptococcus pneumoni...
- Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity
[作者：Voss, ME; Rainka, MP; Fleming, M; Peterson, LH; Belanger, DB; Siddiqui, MA; Hruza, A; Voigt, J; Gray, K; Basso, AD,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3544-3549 , 文章类型： Article，,卷期：2012年22-10]
- The structure-activity relationships of new Aurora A/B kinase inhibitors derived from the previously identified kinase inhibitor 12 are described. Introduction of acetic acid amides onto the pyrazole of compound 12 was p...
- Derivatives of 8-hydroxyquinoline-antibacterial agents that target intra- and extracellular Gram-negative pathogens
[作者：Enquist, PA; Gylfe, A; Hagglund, U; Lindstom, P; Norberg-Scherman, H; Sundin, C; Elofsson, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3550-3553 , 文章类型： Article，,卷期：2012年22-10]
- Small molecule screening identified 5-nitro-7-((4-phenylpiperazine-1-yl-)methyl)quinolin-8-ol INP1750 as a putative inhibitor of type III secretion (T3S) in the Gram-negative pathogen Yersinia pseudotuberculosis. In this...
- Synthesis and acrosin inhibitory activity of methyl 5-substituted-1H-benzo[d]imidazol-2-yl carbamate derivatives
[作者：Liu, XF; Chen, QQ; Zhu, J; Fan, YZ; Ding, LL; Zhao, JT; Han, GQ; Tian, W; Qi, JJ; Zhou, YJ; Lv, JG,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3554-3559 , 文章类型： Article，,卷期：2012年22-10]
- A series of novel methyl 5-substituted 1H-benzo[d]imidazol-2-ylcarbamates were designed, synthesized, and their acrosin inhibitory activities evaluated in vitro. The results of acrosin inhibitory activity showed that all...
- Identification of a series of 1,3,4-oxadiazol-2-amines as potent alpha-7 agonists with efficacy in the novel object recognition model of cognition
[作者：Skidmore, J; Atcha, Z; Boucherat, E; Castelletti, L; Chen, DW; Coppo, FT; Cutler, L; Dunsdon, RM; Heath, BM; Hutchings, R; Hurst, DN; Javed, S; Martin, S; Maskell, ESL; Norton, D; Pemberton, DJ; Redshaw, S; Rutter, R; Sehmi, SS; Scoccitti, T; Temple, HE; Theobald, P; Ward, RW; Wilson, DM,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3560-3563 , 文章类型： Article，,卷期：2012年22-10]
- A series of alpha 7 nicotinic acetylcholine receptor full-agonists with a 1,3,4-oxadiazol-2-amine core has been discovered. Systematic exploration of the structure-activity relationships for both alpha 7 potency and sele...
- A carbosilane dendrimer and a silacyclopentadiene analog carrying peripheral lactoses as drug-delivery systems
[作者：Aizawa, H; Otomo, K; Honsho, N; Shimazaki, T; Villeneuve, M; Matsuoka, K; Hatano, K; Terunuma, D,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：3564-3566 , 文章类型： Article，,卷期：2012年22-10]
- A carbosilane dendrimer (4a) and its silacyclopentadiene analog (4b), both functionalized with lactoses, were tested for their abilities to act as drug-delivery systems. The critical micelle concentrations of 4a and 4b w...
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