Bioorganic & Medicinal Chemistry Letters
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2.82
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#2Liangxing Wu (Incyte)H-Index: 4
Last. Wenqing Yao (Incyte)H-Index: 17
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Abstract null null Activin receptor-like kinase 2 (ALK2) has been implicated as a key target in multiple rare diseases. Herein, we describe the design of a novel bicyclic lactam series of potent and selective ALK2 inhibitors. This manuscript details an improvement in potency of two orders of magnitude from the initial bicyclic structure as well as a two-fold improvement in cellular potency from the original monocyclic inhibitor. Furthermore, we provide a detailed strategy for progressing this pr...
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#1Sanjay Bhattarai (KU: University of Kansas)H-Index: 5
#2Lei Liu (BWH: Brigham and Women's Hospital)H-Index: 9
Last. Michael S. Wolfe (KU: University of Kansas)H-Index: 5
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Abstract null null A series of analogs based on a prototype aryl aminothiazole γ-secretase modulator (GSM) were synthesized and tested for their effects on the profile of 37-to-42-residue amyloid β-peptides (Aβ), generated through processive proteolysis of precursor protein substrate by γ-secretase. Certain substitutions on the terminal aryl D ring resulted in an altered profile of Aβ production compared to that seen with the parent molecule. Small structural changes led to concentration-depende...
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#1Xuelian Zhao (HNUST: Hunan University of Science and Technology)
#2Xuehui Zhan (CSUT: Changsha University of Science and Technology)
Last. Wenlin Xie (HNUST: Hunan University of Science and Technology)H-Index: 6
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Abstract null null A series of (Z)-3-(2-(1,3,4-thiadiazol-2-yl)hydrazono)-1-substituted indolin-2-ones derivatives (3a-3m) were designed and synthesized. All newly synthesized compounds were evaluated for their a-glucosidase inhibitory activity with resveratrol as positive control in vitro. Except for 3i and 3j, all of the compounds showed a potent inhibitory activity against a-glucosidase with IC50 values in the range of 3.12 ± 1.25 to 45.95 ± 1.26 μM and the purity of these compounds was great...
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#1Ruixu Mu (CAMS&PUMC: Chinese Academy of Medical Sciences & Peking Union Medical College)
#2Yongting Zhou (CAMS&PUMC: Chinese Academy of Medical Sciences & Peking Union Medical College)H-Index: 1
Last. Lei Zhu (CAMS&PUMC: Chinese Academy of Medical Sciences & Peking Union Medical College)H-Index: 9
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Abstract null null Inflammation and immunity are closely related to the occurrence and development of a variety of immune diseases. Although IL-1β has been identified as a key cytokine in many immune diseases, safe and specific small molecular IL-1β releasement inhibitors are still scarce and urgently required in clinic. The investigation prospect of triazoleis limited by its complicated pharmacological effect which exhibited inferior effects on IL-1β and TNF-α. Herein, 36 novel derivatives were...
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#1Masahiko Oshige (Gunma University)H-Index: 6
#2Koki Kano (Gunma University)H-Index: 1
Last. Ichiro Matsuo (Gunma University)H-Index: 27
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Abstract null null Sulfoquynovosylacyl propanediol (SQAP; 1) has been developed as a radiosensitizer (anti-cancer agent) for solid tumors, but it was easily cleaved in vivo and had a problem of short residence time. We synthesized a novel compound of a SQAP derivative (3-octadecanoxypropyl 6-deoxy-6-sulfo-α- d -glucopyranoside: ODSG; 2) to solve these problems not easily cleaved by lipase. ODSG (2) cytotoxicity was investigated in vitro, resulting in low toxicity like SQAP (1).
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Abstract null null Epidermal growth factor receptor (EGFR) inhibitors have clinical utility in the treatment of non-small cell lung cancer (NSCLC) patients. Despite encouraging clinical efficacy with these agents, many patients develop resistance due to sensitizing (or activating) mutations ultimately leading to disease progression. In the majority of the cases, this resistance is due to the T790M mutation and frequently coexisting L858R. In addition, EGFR wild type receptor inhibition can lead ...
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Abstract null null The preliminary results on the development of a viable methodology for the further functionalization of 4-hydroxythiazole derivatives to afford target TRPM8 antagonists are reported. The combined Sonogashira coupling / annulation reactions of the ethyl 2-(3-fluorophenyl)-4-tifluoromethylsulfonyloxy-1,3-thiazole-5-carboxylate have been applied to the synthesis of analogues of the selective blocker of TRPM8 DFL23448. Among all the synthetised derivatives, the most promising comp...
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#1Koji Matsuoka (Saitama University)H-Index: 27
#2Takayuki Kaneshima (Saitama University)
Last. Ken Hatano (Saitama University)H-Index: 17
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Abstract null null A water-soluble glycomonomer having a sialyl α2 → 3 lactose (SLac) moiety was prepared from a known imidate derivative of the SLac and an acrylamide alcohol by means of Schmidt’s protocol followed by transesterification. Polymerization of the monomer proceeded in water as the solvent in the presence of ammonium persulfate (APS)—tetramethylethylenediamine (TEMED). Since acryl amide (AAm) was used as a regulator for the arrangement of sugar density, three kinds of glycopolymers ...
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#1Xupeng Huang (CAMS&PUMC: Chinese Academy of Medical Sciences & Peking Union Medical College)H-Index: 1
#2Hao Chen (CAMS&PUMC: Chinese Academy of Medical Sciences & Peking Union Medical College)H-Index: 2
Last. Zhiqiang Feng (CAMS&PUMC: Chinese Academy of Medical Sciences & Peking Union Medical College)H-Index: 11
view all 6 authors...
Abstract null null Blocking the programmed cell death protein 1 (PD-1) and programmed death-ligand.1 (PD-L1) interaction has emerged as one of the most promising treatments for cancer immunotherapy. A novel series of compounds bearing a benzo[d]isoxazole scaffold was developed as PD-1/PD-L1 inhibitors, among them, compound P20 exhibited the most potent inhibitory activity, with an IC50 value of 26.8 nM. The preliminary structure-activity relationship was also investigated. The docking analysis o...
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#1Li-Ping Guan (ZJOU: Zhejiang Ocean University)H-Index: 10
#2Peng Dingxin (ZJOU: Zhejiang Ocean University)H-Index: 2
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Abstract null null The marine environment is a rich resource for discovering functional materials, and seaweed is recognized for its potential use in biology and medicine. Liquiritigenin has been isolated and identified from Sargassum pallidum. To find new anti-Alzheimer’s activity, we designed and synthesized thirty-two 7-prenyloxy-2,3-dihydroflavanone derivatives (3a-3p) and 5-hydroxy-7-prenyloxy-2,3-dihydro-flavanone derivatives (4a-4p) as cholinesterases inhibitors based on liquiritigenin as...
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