- Cell-based optimization of novel benzamides as potential antimalarial leads
[作者：Wu, T; Nagle, A; Sakata, T; Henson, K; Borboa, R; Chen, Z; Kuhen, K; Plouffe, D; Winzeler, E; Adrian, F; Tuntland, T; Chang, J; Simerson, S; Howard, S; Ek, J; Isbell, J; Deng, XM; Gray, NS; Tully, DC; Chatterjee, AK,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6970-6974 , 文章类型： Article，,卷期：2009年19-24]
- Screening our in-house compound collection using a cell based Plasmodium falciparum proliferation assay we discovered a known pan- kinase inhibitor scaffold as a hit. Further optimization of this series led us to a novel...
- Synthesis, stereochemistry and antimicrobial studies of novel oxime ethers of aza/diazabicycles
[作者：Parthiban, P; Aridoss, G; Rathika, P; Ramkumar, V; Kabilan, S,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6981-6985 , 文章类型： Article，,卷期：2009年19-24]
- Two series of bicyclic oxime ethers viz, 2,4-diaryl-3-azabicyclo[3.3.1]nonan-9-one O-benzyloximes 13-24 and 2,4,6,8-tetraaryl-3,7-diazabicyclo[3.3.1]nonan-9-one O-benzyloximes 31-36 were synthesized and stereochemistry w...
- NSAID-derived gamma-secretase modulators. Part III: Membrane anchoring
[作者：Baumann, S; Hottecke, N; Schubenel, R; Baumann, K; Schmidt, B,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6986-6990 , 文章类型： Article，,卷期：2009年19-24]
- Selective lowering of A beta(42) levels with small-molecule substrate targeting c-secretase modulators (sGSMs), such as some non-steroidal anti-inflammatory drugs, is a promising therapeutic approach for Alzheimer's dise...
- Imidazo[1,2-a]pyrazine diaryl ureas: Inhibitors of the receptor tyrosine kinase EphB4
[作者：Mitchell, SA; Danca, MD; Blomgren, PA; Darrow, JW; Currie, KS; Kropf, JE; Lee, SH; Gallion, SL; Xiong, JM; Pippin, DA; DeSimone, RW; Brittelli, DR; Eustice, DC; Bourret, A; Hill-Drzewi, M; Maciejewski, PM; Elkin, LL,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6991-6995 , 文章类型： Article，,卷期：2009年19-24]
- Inhibition of receptor tyrosine kinases (RTKs) such as vascular endothelial growth factor receptors (VEGFRs) and platelet-derived growth factor receptors (PDGFRs) has been validated by recently launched small molecules S...
- Synthesis of 9-anilinoacridine triazines as new class of hybrid antimalarial agents
[作者：Kumar, A; Srivastava, K; Kumar, SR; Puri, SK; Chauhan, PMS,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6996-6999 , 文章类型： Article，,卷期：2009年19-24]
- There is challenge and urgency to synthesize cost-effective chemotherapeutic agents for treatment of malaria after the widespread development of resistance to CQ. In the present study, we synthesized a new series of hybr...
- Synthesis and antimycobacterial evaluation of novel 5,6-dimethoxy-1-oxo-2,5-dihydro-1H-2-indenyl-5,4-substituted phenyl methanone analogues
[作者：Ali, MA; Samy, JG; Manogaran, E; Sellappan, V; Hasan, MZ; Ahsan, MJ; Pandian, S; ShaharYar, M,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7000-7002 , 文章类型： Article，,卷期：2009年19-24]
- In present investigation, a series of substituted phenyl-5,6-dimethoxy-1-oxo-2,5-dihydro-1H-2-indenylmethanone analogues were synthesized and were evaluated for antimycobacterial activity against Mycobacterium tuberculos...
- Evaluation and optimization of antifibrotic activity of cinnamoyl anthranilates
[作者：Zammit, SC; Cox, AJ; Gow, RM; Zhang, Y; Gilbert, RE; Krum, H; Kelly, DJ; Williams, SJ,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：7003-7006 , 文章类型： Article，,卷期：2009年19-24]
- Tranilast is an anti-inflammatory drug in use for asthma and atopic dermatitis. In studies over the last decade it has been revealed that tranilast can reduce fibrosis occurring in the kidney during diabetes, thereby del...
- Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: Discovery of highly potent and selective analogs with improved human microsomal stability
[作者：Richard, DJ; Verheijen, JC; Curran, K; Kaplan, J; Toral-Barza, L; Hollander, I; Lucas, J; Yu, K; Zask, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6830-6835 , 文章类型： Article，,卷期：2009年19-24]
- A series of highly potent and selective pyrazolopyrimidine mTOR inhibitors which contain water-solubilizing groups attached to the 6-arylureidophenyl moiety have been prepared. Such derivatives displayed superior potency...
- N-3-Arylmalonamides: A new series of thieno[3,2-b]pyridine based inhibitors of c-Met and VEGFR2 tyrosine kinases
[作者：Saavedra, O; Claridge, S; Zhan, L; Raeppel, F; Granger, MC; Raeppel, S; Mannion, M; Gaudette, F; Zhou, N; Isakovic, L; Bernstein, N; Deziel, R; Nguyen, H; Beaulieu, N; Beaulieu, C; Dupont, I; Wang, J; Macleod, AR; Besterman, JM; Vaisburg, A,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6836-6839 , 文章类型： Article，,卷期：2009年19-24]
- A family of thieno[3,2-b]pyridine based small molecule inhibitors of c-Met and VEGFR2 were designed based on lead structure 2. These compounds were shown to have IC50 values in the low nanomolar range in vitro and were e...
- Tetrahydroquinoline derivatives as CRTH2 antagonists
[作者：Liu, JW; Wang, YC; Sun, Y; Marshall, D; Miao, SC; Tonn, G; Anders, P; Tocker, J; Tang, HL; Medina, J,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6840-6844 , 文章类型： Article，,卷期：2009年19-24]
- A series of tetrahydroquinoline-derived inhibitors of the CRTH2 receptor was discovered by a high throughput screen. Optimization of these compounds for potency and pharmacokinetic properties led to the discovery of pote...
- Fragment-based discovery of selective inhibitors of the Mycobacterium tuberculosis protein tyrosine phosphatase PtpA
[作者：Rawls, KA; Lang, PT; Takeuchi, J; Imamura, S; Baguley, TD; Grundner, C; Alber, T; Ellman, JA,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6851-6854 , 文章类型： Article，,卷期：2009年19-24]
- The development of low mu M inhibitors of the Mycobacterium tuberculosis phosphatase PtpA is reported. The most potent of these inhibitors (K-i = 1.4 +/- 0.3 mu M) was found to be selective when tested against a panel of...
- Synthesis and biological evaluation of salicylic acid and N-acetyl-2-carboxybenzenesulfonamide regioisomers possessing a N-difluoromethyl-1,2-dihydropyrid-2-one pharmacophore: Dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity
[作者：Chowdhury, MA; Abdellatif, KRA; Dong, Y; Das, D; Yu, G; Velazquez, CA; Suresh, MR; Knaus, EE,期刊：Bioorganic & Medicinal Chemistry Letters, 页码：6855-6861 , 文章类型： Article，,卷期：2009年19-24]
- A novel class of salicylic acid and N-acetyl-2-carboxybenzenesulfonamide regioisomers possessing a N-difluoromethyl-1,2-dihydropyrid-2-one pharmacophore attached to its C-4 or C-5 position was designed for evaluation as ...
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