- Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)-Hit to Lead studies
[作者：Wan, HH; Huynh, T; Pang, SH; Geng, JP; Vaccaro, W; Poss, MA; Trainor, GL; Lorenzi, MV; Gottardis, M; Jayaraman, L; Purandare, AV,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5063-5066 , 文章类型： Article，,卷期：2009年19-17]
- Hit to Lead optimization and SAR development led to the identification of the potent and selective benzo[d]imidazole inhibitor (17b) of Co-activator Associated Arginine Methyltransferase (CARM1). (C) 2009 Elsevier Ltd. A...
- Design, synthesis and evaluation of novel 5,6-dimethoxy-1-oxo-2,3-dihydro-1H-2-indenyl-3,4-substituted phenyl methanone analogues
[作者：Ali, MA; Yar, MS; Hasan, MZ; Ahsan, MJ; Pandian, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5075-5077 , 文章类型： Article，,卷期：2009年19-17]
- In present investigation, a series of substituted phenyl-5,6-dimethoxy-1-oxo-2,3-dihydro-1H-2-indenylmethanone analogues were synthesized and were tested for their potential for treating AD disease. All the newly synthes...
- N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: Impact of small structural modifications on P-gp recognition and CNS penetration
[作者：Wakenhut, F; Allan, GA; Fish, PV; Fray, MJ; Harrison, AC; McCoy, R; Phillips, SC; Stobie, A; Westbrook, D; Westbrook, SL; Whitlock, GA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5078-5081 , 文章类型： Article，,卷期：2009年19-17]
- The structure-activity relationship and the synthesis of novel N-[(3S)-pyrrolidin-3-yl]benzamides as dual serotonin and noradrenaline monoamine reuptake inhibitors (SNRI) is described. Preferred compound 9 aka PF-184,298...
- Carbonic anhydrase inhibitors; Fluorinated phenyl sulfamates show strong inhibitory activity and selectivity for the inhibition of the tumor-associated isozymes IX and XII over the cytosolic ones I and II
[作者：Winum, JY; Innocenti, A; Vullo, D; Montero, JL; Supuran, CT,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5082-5085 , 文章类型： Article，,卷期：2009年19-17]
- A series of fluorinated-phenylsulfamates have been prepared by sulfamoylation of the corresponding phenols and the inhibition of four physiologically relevant carbonic anhydrase (CA, EC 4.2.1.1) isozymes, the cytosolic C...
- Design, syntheses, and evaluation of Taspase1 inhibitors
[作者：Lee, JT; Chen, DY; Yang, ZM; Ramos, AD; Hsieh, JJD; Bogyo, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5086-5090 , 文章类型： Article，,卷期：2009年19-17]
- Taspase1 is a threonine protease responsible for cleaving MLL (Mixed-Lineage Leukemia) to achieve proper HOX gene expression. Subsequent studies identified additional Taspase1 substrates including Transcription Factor II...
- Atovaquone derivatives as potent cytotoxic and apoptosis inducing agents
[作者：Zhou, J; Duan, L; Chen, HM; Ren, XM; Zhang, Z; Zhou, FT; Liu, JS; Pei, DQ; Ding, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5091-5094 , 文章类型： Article，,卷期：2009年19-17]
- 2-Piperazinyl naphthoquinones (2) and 2-piperidinyl naphthoquinones (3) were designed and synthesized as new cytotoxic and apoptosis inducing agents by utilizing the anti-parasite drug atovaquone as lead compound. Severa...
- Crystal structure, antitumour and antimetastatic activities of disubstituted fused 1,2,4-triazinones
[作者：Sztanke, K; Pasternak, K; Sztanke, M; Kandefer-Szerszen, M; Koziol, AE; Dybala, I,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5095-5100 , 文章类型： Article，,卷期：2009年19-17]
- Molecular structure of 3,8-disubstituted 7,8-dihydroimidazo[2,1-c][1,2,4]triazin-4(6H)-ones (8-14) was confirmed by X-ray crystallography of 14. All the compounds were evaluated for their antitumour and antimetastatic ac...
- Synthesis of sialic acid derivatives having a C = C double bond substituted at the C-5 position and their glycopolymers
[作者：Suzuki, K; Sakamoto, JI; Koyama, T; Yingsakmongkon, S; Suzuki, Y; Hatano, K; Terunuma, D; Matsuoka, K,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5105-5108 , 文章类型： Article，,卷期：2009年19-17]
- Glycomonomers of sialic acid in which the acetamide group at C-5 was converted into two kinds of C = C double bond substituents were prepared and the fully protected glycomonomers were directly polymerized before deprote...
- Design, synthesis and evaluation of 4,5-di-substituted acridone ligands with high G-quadruplex affinity and selectivity, together with low toxicity to normal cells
[作者：Cuenca, F; Moore, MJB; Johnson, K; Guyen, B; De Cian, A; Neidle, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5109-5113 , 文章类型： Article，,卷期：2009年19-17]
- A series of 4,5-di-substituted acridones have been designed and synthesized. Several compounds show high affinity for telomeric G-quadruplex DNA in classical and competition FRET assays, together with low duplex DNA affi...
- Optimization of a series of quinazolinone-derived antagonists of CXCR3
[作者：Liu, JW; Fu, ZC; Li, AR; Johnson, M; Zhu, L; Marcus, A; Danao, J; Sullivan, T; Tonn, G; Collins, T; Medina, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5114-5118 , 文章类型： Article，,卷期：2009年19-17]
- The evaluation of the CXCR3 antagonist AMG 487 in clinic trials was complicated due to the formation of an active metabolite. In this Letter, we will discuss the further optimization of the quinazolinone series that led ...
- Substituted tetrahydroquinolines as potent allosteric inhibitors of reverse transcriptase and its key mutants
[作者：Su, DS; Lim, JJ; Tinney, E; Wan, BL; Young, MB; Anderson, KD; Rudd, D; Munshi, V; Bahnck, C; Felock, PJ; Lu, MQ; Lai, MT; Touch, S; Moyer, G; DiStefano, DJ; Flynn, JA; Liang, YX; Sanchez, R; Prasad, S; Yan, YW; Perlow-Poehnelt, R; Torrent, M; Miller, M; Vacca, JP; Williams, TM; Anthony, NJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5119-5123 , 文章类型： Article，,卷期：2009年19-17]
- Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are key elements of multidrug regimens, called HAART (Highly Active Antiretroviral Therapy), that are used to treat HIV-1 infections. Elucidation of the structure-...
- Synthesis and evaluation of a series of 2,4-diaminopyridine derivatives as potential positron emission tomography tracers for neuropeptide Y Y1 receptors
[作者：Kameda, M; Ando, M; Nakama, C; Kobayashi, K; Kawamoto, H; Ito, S; Suzuki, T; Tani, T; Ozaki, S; Tokita, S; Sato, N,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5124-5127 , 文章类型： Article，,卷期：2009年19-17]
- A series of 2,4-diaminopyridine derivatives was synthesized and evaluated as potential candidates for neuropeptide Y (NPY) Y1 receptor positron emission tomography (PET) tracers. Derivatives bearing substitutions allowin...
- Antiparasitic activities of novel, orally available fumagillin analogs
[作者：Arico-Muendel, C; Centrella, PA; Contonio, BD; Morgan, BA; O'Donovan, G; Paradise, CL; Skinner, SR; Sluboski, B; Svendsen, JL; White, KF; Debnath, A; Gut, J; Wilson, N; McKerrow, JH; DeRisi, JL; Rosenthal, PJ; Chiang, PK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：5128-5131 , 文章类型： Article，,卷期：2009年19-17]
- Fumagillin, an irreversible inhibitor of MetAP2, has been shown to potently inhibit growth of malaria parasites in vitro. Here, we demonstrate activity of fumagillin analogs with an improved pharmacokinetic profile again...
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