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Bioorganic & Medicinal Chemistry Letters
Papers 23428
1 page of 2,343 pages (23.4k results)
Published on Jul 1, 2019in Bioorganic & Medicinal Chemistry Letters 2.45
Anna K. Puszko4
Estimated H-index: 4
(University of Warsaw),
Piotr Sosnowski (PAN: Polish Academy of Sciences)+ 4 AuthorsAleksandra Misicka19
Estimated H-index: 19
(University of Warsaw)
Abstract NRP-1 is an important co-receptor of vascular endothelial growth factor receptor-2 (VEGFR-2). Many reports suggested that NRP-1 might also serve as a separate receptor for VEGF-A 165 causing stimulation of tumour growth and metastasis. Therefore, compounds interfering with VEGF-A 165 /NRP-1 complex triggered interest in the design of new molecules, including peptides, as anti-angiogenic and anti-tumour drugs. Here, we report the synthesis, affinity and stability evaluation of the urea-p...
Xavier Fradera8
Estimated H-index: 8
(MSD: Merck & Co.),
Joey L. Methot9
Estimated H-index: 9
(MSD: Merck & Co.)
+ -3 AuthorsYudith Garcia2
Estimated H-index: 2
(MSD: Merck & Co.)
Abstract PI3Kδ mediates key immune cell signaling pathways and is a target of interest for multiple indications in immunology and oncology. Here we report a structure-based scaffold-hopping strategy for the design of chemically diverse PI3Kδ inhibitors. Using this strategy, we identified several scaffolds that can be combined to generate new PI3Kδ inhibitors with high potency and isoform selectivity. In particular, an oxindole-based scaffold was found to impart exquisite selectivity when combine...
Jingxin Qiao (Sichuan University), Guifeng Lin1
Estimated H-index: 1
(Sichuan University)
+ -3 AuthorsSheng-Yong Yang26
Estimated H-index: 26
(Sichuan University)
Abstract Inhibitors of the Hippo signaling pathway have been demonstrated to have a potential clinical application in cases such as tissue repair and organ regeneration. However, there is a lack of potent Hippo pathway inhibitors at present. Herein we report the discovery of a series of 1,8-disubstituted-[1,2,3]triazolo[4,5-c]quinoline derivatives as a new class of Hippo pathway inhibitors by utilizing a cell line-based screening model (A549-CTGF). Structure-activity relationship (SAR) of these ...
Arun K. Ghosh53
Estimated H-index: 53
(Purdue University),
Jacqueline N. Williams1
Estimated H-index: 1
(Purdue University)
+ -3 AuthorsHiroaki Mitsuya69
Estimated H-index: 69
(Kumamoto University)
Abstract We describe the design, synthesis, and biological evaluation of novel HIV-1 protease inhibitors containing a squaramide-derived scaffold as the P2 ligand in combination with a (R)-hydroxyethylamine sulfonamide isostere. Inhibitor 3h with an N-methyl-3-(R)-aminotetrahydrofuranyl squaramide P2-ligand displayed an HIV-1 protease inhibitory Ki value of 0.51 nM. An energy minimized model of 3h revealed the major molecular interactions between HIV-1 protease active site and the tetrahydrofura...
Published on Jul 1, 2019in Bioorganic & Medicinal Chemistry Letters 2.45
Ahmed M. Abdelaziz1
Estimated H-index: 1
(UniSA: University of South Australia),
Sunita K. C. Basnet6
Estimated H-index: 6
(UniSA: University of South Australia)
+ 6 AuthorsShudong Wang24
Estimated H-index: 24
(UniSA: University of South Australia)
Abstract Post-translational modulation of eIF4E through phosphorylation by Mnks is highly integral to the pathogenesis of different cancers. Therefore, inhibition of Mnks offers a strategy for cancer treatment. Herein, a series of 2' H -spiro[cyclohexane-1,3'-imidazo[1,5- a ]pyridine]-1',5'-dione derivatives is presented as Mnk inhibitors. Some of them showed sub-micromolar to low nanomolar inhibitory activities against Mnk1/2 with a high level of selectivity for both kinases over CDKs. Biochemi...
Published on Jul 1, 2019in Bioorganic & Medicinal Chemistry Letters 2.45
Peng-Jen Chen (TU: Temple University), Michelle Taylor14
Estimated H-index: 14
(University of North Texas Health Science Center)
+ 9 AuthorsRobert R. Luedtke28
Estimated H-index: 28
(University of North Texas Health Science Center)
Abstract As part of our on-going effort to explore the role of dopamine receptors in drug addiction and identify potential novel therapies for this condition, we have a identified a series of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamide D 3 ligands. Members of this class are highly selective for D 3 versus D 2 , and we have identified two compounds ( 13g and 13r ) whose rat in vivo IV pharmacokinetic properties that indicate that they are suitable for assessment in in vivo eff...
Published on Jul 1, 2019in Bioorganic & Medicinal Chemistry Letters 2.45
Hui Li (SCAU: South China Agricultural University), Lizhu Chen (Southern Medical University)+ 5 AuthorsGaopeng Song3
Estimated H-index: 3
(SCAU: South China Agricultural University)
Abstract The glycoprotein hemagglutinin of influenza virus plays a key role in the initial stage of virus infection, making it a potential target for novel influenza viruses entry inhibitors. Two “privileged fragments”, 2-(piperidin-1-yl)ethan-1-amine and 2-(1,3-oxazinan-3-yl)ethan-1-amine were integrated into 3- O -β-chacotriosyl ursolic acid producing new derivatives 5 and 6 with improved activity against IAVs in vitro . Mechanistically, compound 6 was effective in inhibiting infection of H1-,...
Feyisola P. Olatunji (WSU: Washington State University), Brittany N. Kesic (WSU: Washington State University)+ -3 AuthorsClifford E. Berkman23
Estimated H-index: 23
(WSU: Washington State University)
Abstract L-Dopa has continued to be a mainstay in the symptomatic treatment of Parkinson’s disease (PD). However, extensive peripheral metabolism, a short systemic circulation half-life and development of motor complications called dyskinesia prevents its long-term utilization as a PD therapeutic. Herein, we report a series of phosphoramidate derivatives of L-Dopa and controlled release of L-Dopa at pH 7.4 and 3. The kinetic data for the release of L-Dopa support our hypothesis that a proximal c...