European Journal of Medicinal Chemistry_文献综述【化源网】 -


New lipophilic isoniazid derivatives and their 1,3,4-oxadiazole analogues: Synthesis, antimycobacterial activity and investigation of their mechanism of action 10.1016/j.ejmech.2018.04.017 2018-04-10 The development of novel drugs is essential for the treatment of tuberculosis and other mycobacterial infections in future. A series of N-alkyl-2-isonicotinoylhydrazine-1-carboxamides was synthesized from isoniazid (INH) and then cyclized to N-alkyl-5-(pyridi...
Discovery of new benzensulfonamide derivatives as tripedal STAT3 inhibitors 10.1016/j.ejmech.2018.03.053 2018-04-04 Persistent activated STAT3 has a striking correlation with cancer development and inhibition of STAT3 signaling pathway is a novel therapeutic way for human cancers. Among STAT family, STAT1 and STAT3 play opposite roles in tumorigenesis. However, the discove...
2-Benzylpiperazine: A new scaffold for potent human carbonic anhydrase inhibitors. Synthesis, enzyme inhibition, enantioselectivity, computational and crystallographic studies and in vivo activity for a new class of intraocular pressure lowering agents 10.1016/j.ejmech.2018.04.002 2018-04-03 Two series of 2-benzylpiperazines have been prepared and tested for the inhibition of physiologically relevant isoforms of human carbonic anhydrases (hCA, EC 4.2.1.1). The new compounds carry on one nitrogen atom of the piperazine ring a sulfamoylbenzamide gr...
Anti-leishmanial click modifiable thiosemicarbazones: Design, synthesis, biological evaluation and in silico studies 10.1016/j.ejmech.2018.04.003 2018-04-03 Leishmaniasis is a devastating tropical disease with limited therapeutic options. Depending on recently reported active anti-leishmanial compounds, we designed and synthesized a series of click modifiable 1,2,3-triazole and thiosemicarbazone hybrids. Most of ...
Design and synthesis of BPR1K653 derivatives targeting the back pocket of Aurora kinases for selective isoform inhibition 10.1016/j.ejmech.2018.03.064 2018-04-03 Twenty five novel chemical analogs of the previously reported Aurora kinase inhibitor BPR1K653 (1-(4-(2-((5-chloro-6-phenylfuro[2,3-d]pyrimidin-4-yl)amino)ethyl)phenyl)- 3-(2-((dimethylamino)methyl)phenyl)urea) have been designed, synthesized, and evaluated b...
Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation 10.1016/j.ejmech.2018.04.006 2018-04-03 A series of diverse small molecules have been designed and synthesized through structure-based drug design by taking advantage of fragment merging and elaboration approaches. Compounds ZL0420 (28) and ZL0454 (35) were identified as potent and selective BRD4 i...
Indolyl-isoxazolidines attenuates LPS-stimulated pro-inflammatory cytokines and increases survival in a mouse model of sepsis: Identification of potent lead 10.1016/j.ejmech.2018.04.004 2018-04-03 A library of indolyl-isoxazolidines (6–9) has been synthesized by regio- and stereoselective microwave irradiated 1,3-dipolar cycloadditions of C-(3-indolyl)-N-phenylnitrone (2′) with variedly substituted dipolarophiles (3′-5′) and screened for their anti-inf...
Discovery of 6-chloro-2-(propylthio)-8,9-dihydro-7H-purines containing a carboxamide moiety as potential selective anti-lung cancer agents 10.1016/j.ejmech.2018.03.084 2018-04-03 A new series of 6-chloro-2-(propylthio)-8,9-dihydro-7H-purine-8-caboxamide derivatives were designed, synthesized, and further evaluated for their antiproliferative activities on four human cancer cell lines (A549, MGC803, PC-3 and TE-1). The structure-activi...
Therapeutic journery of nitrogen mustard as alkylating anticancer agents: Historic to future perspectives 10.1016/j.ejmech.2018.04.001 2018-04-03 Cancer is considered as one of the most serious health problems today. The discovery of nitrogen mustard as an alkylating agent in 1942, opened a new era in the cancer chemotherapy. This valuable class of alkylating agent exerts its biological activity by bin...
Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation 10.1016/j.ejmech.2018.03.082 2018-04-03 Sarsasapogenin, an active ingredient in Rhizoma anemarrhenae, is a promising bioactive lead compound in the treatment of Alzheimer's disease. To search for more efficient anti-Alzheimer agents, a series of novel sarsasapogenin-triazolyl hybrids were designed,...

New lipophilic isoniazid derivatives and their 1,3,4-oxadiazole analogues: Synthesis, antimycobacterial activity and investigation of their mechanism of action

10.1016/j.ejmech.2018.04.017

2018-04-10

The development of novel drugs is essential for the treatment of tuberculosis and other mycobacterial infections in future. A series of N-alkyl-2-isonicotinoylhydrazine-1-carboxamides was synthesized from isoniazid (INH) and then cyclized to N-alkyl-5-(pyridi...

Discovery of new benzensulfonamide derivatives as tripedal STAT3 inhibitors

10.1016/j.ejmech.2018.03.053

2018-04-04

Persistent activated STAT3 has a striking correlation with cancer development and inhibition of STAT3 signaling pathway is a novel therapeutic way for human cancers. Among STAT family, STAT1 and STAT3 play opposite roles in tumorigenesis. However, the discove...

2-Benzylpiperazine: A new scaffold for potent human carbonic anhydrase inhibitors. Synthesis, enzyme inhibition, enantioselectivity, computational and crystallographic studies and in vivo activity for a new class of intraocular pressure lowering agents

10.1016/j.ejmech.2018.04.002

2018-04-03

Two series of 2-benzylpiperazines have been prepared and tested for the inhibition of physiologically relevant isoforms of human carbonic anhydrases (hCA, EC 4.2.1.1). The new compounds carry on one nitrogen atom of the piperazine ring a sulfamoylbenzamide gr...

Anti-leishmanial click modifiable thiosemicarbazones: Design, synthesis, biological evaluation and in silico studies

10.1016/j.ejmech.2018.04.003

2018-04-03

Leishmaniasis is a devastating tropical disease with limited therapeutic options. Depending on recently reported active anti-leishmanial compounds, we designed and synthesized a series of click modifiable 1,2,3-triazole and thiosemicarbazone hybrids. Most of ...

Design and synthesis of BPR1K653 derivatives targeting the back pocket of Aurora kinases for selective isoform inhibition

10.1016/j.ejmech.2018.03.064

2018-04-03

Twenty five novel chemical analogs of the previously reported Aurora kinase inhibitor BPR1K653 (1-(4-(2-((5-chloro-6-phenylfuro[2,3-d]pyrimidin-4-yl)amino)ethyl)phenyl)- 3-(2-((dimethylamino)methyl)phenyl)urea) have been designed, synthesized, and evaluated b...

Discovery of potent and selective BRD4 inhibitors capable of blocking TLR3-induced acute airway inflammation

10.1016/j.ejmech.2018.04.006

2018-04-03

A series of diverse small molecules have been designed and synthesized through structure-based drug design by taking advantage of fragment merging and elaboration approaches. Compounds ZL0420 (28) and ZL0454 (35) were identified as potent and selective BRD4 i...

Indolyl-isoxazolidines attenuates LPS-stimulated pro-inflammatory cytokines and increases survival in a mouse model of sepsis: Identification of potent lead

10.1016/j.ejmech.2018.04.004

2018-04-03

A library of indolyl-isoxazolidines (6–9) has been synthesized by regio- and stereoselective microwave irradiated 1,3-dipolar cycloadditions of C-(3-indolyl)-N-phenylnitrone (2′) with variedly substituted dipolarophiles (3′-5′) and screened for their anti-inf...

Discovery of 6-chloro-2-(propylthio)-8,9-dihydro-7H-purines containing a carboxamide moiety as potential selective anti-lung cancer agents

10.1016/j.ejmech.2018.03.084

2018-04-03

A new series of 6-chloro-2-(propylthio)-8,9-dihydro-7H-purine-8-caboxamide derivatives were designed, synthesized, and further evaluated for their antiproliferative activities on four human cancer cell lines (A549, MGC803, PC-3 and TE-1). The structure-activi...

Therapeutic journery of nitrogen mustard as alkylating anticancer agents: Historic to future perspectives

10.1016/j.ejmech.2018.04.001

2018-04-03

Cancer is considered as one of the most serious health problems today. The discovery of nitrogen mustard as an alkylating agent in 1942, opened a new era in the cancer chemotherapy. This valuable class of alkylating agent exerts its biological activity by bin...

Novel sarsasapogenin-triazolyl hybrids as potential anti-Alzheimer's agents: Design, synthesis and biological evaluation

10.1016/j.ejmech.2018.03.082

2018-04-03

Sarsasapogenin, an active ingredient in Rhizoma anemarrhenae, is a promising bioactive lead compound in the treatment of Alzheimer's disease. To search for more efficient anti-Alzheimer agents, a series of novel sarsasapogenin-triazolyl hybrids were designed,...