Bioorganic & Medicinal Chemistry
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#1Szu Lee (TMU: Taipei Medical University)
#2Shih-Wei Wang (MMC: Mackay Medical College)H-Index: 32
Last. Hsueh Yun Lee (TMU: Taipei Medical University)H-Index: 17
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A series of phenylurea hydroxamic acids incorporating pharmacophores of inhibitors of HDAC inhibitors and VEGFR-2 has been designed. Most of the compounds show antiproliferative activity comparable to that of Vorinostat and Sorafenib, and better EPC inhibitory activity. Enzymatic assays and Western blotting results indicated that compound 14 not only inhibits HDAC but also has slight VEGFR-2 inhibitory activity. A docking study revealed that the polar hydroxamic acid retains the interaction with...
#1Valeria Romanucci (University of Naples Federico II)H-Index: 14
#2Maddalena Giordano (University of Naples Federico II)H-Index: 6
Last. Giovanni Di Fabio (University of Naples Federico II)H-Index: 20
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Abstract null null Prodrugs are ingenious derivatives of therapeutic agents designed to improve the pharmacokinetic profile of the drug. Here, we report an efficient and regioselective solid phase approach for obtaining new prodrugs of 9″-silybins conjugated with 3′-ribonucleotide units (uridine and adenosine) as pro-moieties. Uridine and adenosine conjugates were obtained in good yields (41–50%), beginning with silibinin and its diastereomers (silybin A and silybin B), using a NovaSyn® support ...
#1Zhen Zhang (JNU: Jinan University)
#2Yongjin Wang (JNU: Jinan University)H-Index: 1
Last. Ke Ding (JNU: Jinan University)H-Index: 51
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Abstract null null An aromatic trifluoromethyl ketone moiety was characterized as a new warhead for covalently reversible kinase inhibitor design to target the non-catalytic cysteine residue. Potent and selective covalently reversible inhibitors of FGFR4 kinase were successfully designed and synthesized by utilizing this new warhead. The binding mode of a representative inhibitor was fully characterized by using multiple technologies including MALDI-TOF mass spectrometry, dialysis assay and X-ra...
#1Anna Kryshchyshyn-Dylevych (LNMU: Danylo Halytsky Lviv National Medical University)H-Index: 2
#2Lidia RadkoH-Index: 8
Last. Roman Lesyk (LNMU: Danylo Halytsky Lviv National Medical University)H-Index: 32
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Abstract null null A series of novel indole-azolidinone hybrids has been synthesized via Knoevenagel reaction of 5-fluoro-3-formyl-1H-indole-2-carboxylic acid methyl ester and some azolidinones differing in heteroatoms in positions 1, 2 and 4. Their anticancer activity in vitro was screened towards MCF-7 (breast cancer), HCT116 (colon cancer), HepG2 (hepatoma), HeLa (cervical cancer), A549 (lung cancer), WM793 (melanoma) and THP-1 (leukemia) cell lines, and a highly active 5-fluoro-3-(4-oxo-2-th...
#1Markus Falkenstein (HHU: Heinrich Heine University Düsseldorf)H-Index: 1
#2David Reiner-Link (HHU: Heinrich Heine University Düsseldorf)H-Index: 3
Last. Holger Stark (HHU: Heinrich Heine University Düsseldorf)H-Index: 56
view all 6 authors...
Abstract null null Alzheimeŕs disease (AD) is the most prominent neurodegenerative disorder with high medical need. Protein-protein-interactions (PPI) interactions have a critical role in AD where β-amyloid structures (Aβ) build toxic oligomers. Design of disease modifying multi target directed ligand (MTDL) has been performed, which disable PPI on the one hand and on the other hand, act as procognitive antagonists at the histamine H3 receptor (H3R). The synthetized compounds are structurally ba...
#1Yuki Hitora (Kumamoto University)H-Index: 3
#2Rika Maeda (Kumamoto University)
Last. Sachiko Tsukamoto (Kumamoto University)H-Index: 42
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Abstract null null Natural products that inhibit cell cycle progression show promise as anticancer agents and chemical probes. In our research on biologically active natural products that affect cell cycle progression of HeLa/fluorescent ubiquitination-based cell cycle indicator (Fucci)2 cells, the extract of the marine sponge Neopetrosia chaliniformis was revealed to inhibit cell proliferation. Purification of the extract afforded four new pyridine alkaloids, neopetrosidines A–D (1–4). Their st...
#1Basilius Sauter (University of Basel)H-Index: 5
#2Lukas A. Schneider (University of Basel)H-Index: 2
Last. Dennis Gillingham (University of Basel)H-Index: 19
view all 4 authors...
Abstract null null DNA encoded libraries have become an essential hit-finding tool in early drug discovery. Recent advances in synthetic methods for DNA encoded libraries have expanded the available chemical space, but precisely how each type of chemistry affects the DNA is unstudied. Available assays to quantify the damage are limited to write efficiency, where the ability to ligate DNA onto a working encoded library strand is measured, or qPCR is performed to measure the amplifiability of the ...
#1Ganyuan XiaoH-Index: 2
#2Magnus S. AlpheyH-Index: 22
Last. James H. NaismithH-Index: 79
view all 11 authors...
Funding: This work was supported by grants from The Scottish Universities Life Science Alliance (L.P., Ph.D. studentship), a China Scholarship Council-University of St Andrews PhD Fellowship (GX). JHN is funded by the Wellcome Trust (100209/Z/12/Z).
#1Agnieszka Sulima (NIDA: National Institute on Drug Abuse)H-Index: 12
#2Fatemeh Akhlaghi (URI: University of Rhode Island)H-Index: 30
Last. Kenner C. Rice (NIDA: National Institute on Drug Abuse)H-Index: 94
view all 4 authors...
Abstract null null Preclinical and human studies have indicated involvement of the ghrelin system in alcohol-related behaviors illuminating the possibility of using ghrelin receptor blockers as a pharmacological intervention for alcohol use disorder (AUD). Preliminary data from a recently conducted phase 1b human study with a ghrelin receptor inverse agonist, PF-5190457 (2-(2-methylimidazo[2,1-b][1,3thiazol-6-yl)-1-{2-(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]...
#1Kazuya Kobayashi (Kyoto Pharmaceutical University)H-Index: 13
#2Takuya Otani (Kyoto Pharmaceutical University)H-Index: 1
Last. Naoka Shindo (Kyoto Pharmaceutical University)H-Index: 1
view all 16 authors...
Abstract null null An aromatic substituent has been introduced into a known hydroxyethylamine (HEA)-type BACE1 inhibitor containing the superior substrate sequence to enhance inhibitory activity. The HEA-type isosteres bearing different hydroxyl group and methyl group configurations were prepared through a branched synthesis approach using intra- and inter-molecular epoxide opening reactions. The effect of their configuration was evaluated, showing that an R-configuration improved the inhibitory...
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