European Journal of Medicinal Chemistry
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#1Angela Di Capua (UNISI: University of Siena)H-Index: 9
#2Annalisa Reale (UNISI: University of Siena)H-Index: 3
Last. Carla Ghelardini (UniFI: University of Florence)H-Index: 41
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Abstract A series of 4-phenyl-6H-imidazo[1,5-a]thieno[3,2-f][1,4]diazepine-7-carboxylate esters were synthesized and tested as central benzodiazepine receptor (CBR) ligands by the ability to displace [3H]flumazenil from rat cortical membranes. All the compounds showed high affinity with IC50 values ranging from 5.19 to 16.22 nM. In particular, compounds 12b (IC50 = 8.66 nM) and 12d (IC50 = 5.19 nM) appeared as the most effective ligands being their affinity values significantly lower than that o...
#1Perihan A. Elzahhar (Alexandria University)H-Index: 2
#2Shrouk M. Abd El Wahab (Damanhour University)
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Abstract Cancer is a multifactorial disorder involving multiplicity of interrelated signaling pathways and molecular targets. To that end, a multi-target design strategy was adopted to develop some 1,2,3-triazoles hybridized with some pharmacophoric anticancer fragments, as first-in-class simultaneous inhibitors of COX-2, 15-LOX and tumor associated carbonic anhydrase enzymes. Results revealed that compounds 5a, 5d, 8b and 8c were potent inhibitors of COX-2 and 15-LOX enzymes. COX-2 inhibitory a...
#1Reza Ahmadi (Mazandaran University of Medical Sciences)
#2Mohammad Ali Ebrahimzadeh (Mazandaran University of Medical Sciences)H-Index: 29
Abstract Resveratrol is a natural polyphenolic stilbene isolated from various plants, foods and beverages with a broad spectrum of biological and pharmacological properties through modulating diverse targets and signaling pathways. Particularly, it has attracted a great deal of attention as a promising and multitarget anticancer agent due to its potential use in chemoprevention and chemotherapy of various tumors. However, unfavorable pharmacokinetics/pharmacodynamics profile such as poor bioavai...
#1Apeng Wang (Peking Union Medical College)H-Index: 5
#2Chao Ma (Peking Union Medical College)H-Index: 2
Last. Yu LuH-Index: 11
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Abstract A series of new benzothiazinone derivatives containing a symmetric 2-benzyl-2,7-diazaspiro[3.5]nonane moiety, based on the structure of LK02 discovered in our lab, were designed and synthesized. With one exception 3, all of them show excellent in vitro activity against both drug-sensitive and clinically isolated multidrug-resistant Mycobacterium tuberculosis (MTB) strains (MIC:
Abstract The development of new small molecules from known structural motifs through molecular hybridization is one of the trends in drug discovery. In this connection, we have combined the two pharmacophoric units (pyrimidine and thioindole) in a single entity via molecular hybridization strategy along with introduction of urea functionality at C2 position of pyrimidine to increase the efficiency of H-bonding interactions. Among the synthesized conjugates 12a-aa, compound 12k was found to exhib...
Abstract Most of the anti-inflammatory drugs in clinical practice are becoming outdated owing to their potential side and adverse effects. These are found to be highly unsafe for long term use. Thus, since last few years, new anti-inflammatory agents are being developed and number of them are in advanced stages of clinical trials. Heterocyclic molecules have gained great attention of chemists due to their similarity to different biological precursors. In the current review, we have highlighted t...
#1Junyu Xu (CPU: China Pharmaceutical University)H-Index: 4
#2Xinren Wang (CPU: China Pharmaceutical University)
Last. Fei Jiang (CPU: China Pharmaceutical University)H-Index: 1
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Abstract Specific inhibition of CDK9 is considered a promising strategy for developing effective anticancer therapeutics. However, most of the reported CDK9 inhibitors are still at an early stage of development and lack selectivity against other CDKs. Herein, we discovered coumarin derivative 30i as a potent CDK9 inhibitor with high selectivity (8300-fold over CDK7). Binding mode analysis illustrated that the substituent coumarin moiety is a critical group for CDK9 selectivity by occupying a fle...
#1Zhixian Shi (CPU: China Pharmaceutical University)H-Index: 1
#2Na Li (CPU: China Pharmaceutical University)H-Index: 1
Last. Jianbo Sun (CPU: China Pharmaceutical University)H-Index: 11
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Abstract A series of phenylsulfonyfuroxan-based NO-releasing scopoletin derivatives were designed and synthesized in the study. All target compounds showed significantly improved antiproliferative activity against four cancer cell lines (MDA-MB-231, MCF-7, HepG2 and A459) and lower cytotoxicity toward normal liver LO2 cells. Derivative 47 concentration-dependently inhibited the colony formation of MDA-MB-231 cells. NO-releasing assessment indicated that the intracellular NO level was almost posi...
#1Jyoti Sharma (UAB: University of Alabama at Birmingham)H-Index: 1
#2Kim M. Keeling (UAB: University of Alabama at Birmingham)H-Index: 25
Last. Steven M. Rowe (UAB: University of Alabama at Birmingham)H-Index: 44
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Abstract Cystic fibrosis (CF) is a monogenic autosomal recessive disorder. The clinical manifestations of the disease are caused by ∼2,000 mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) protein. It is unlikely that any one approach will be efficient in correcting all defects. The recent approvals of ivacaftor, lumacaftor/ivacaftor and elexacaftor/tezacaftor/ivacaftor represent the genesis of a new era of precision combination medicine for the CF patient population. I...
#1Natalia Sanz del Olmo (University of Alcalá)H-Index: 3
#2Ana M. Bajo (University of Alcalá)H-Index: 15
Last. F. Javier de la Mata (University of Alcalá)H-Index: 20
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Abstract In searching for efficient and selective antitumour drugs, a new family of carbosilane metallodendrimers functionalized with [Ru(η5-C5H5)(PTA)Cl] (PTA = 1,3,5-triaza-7-phosphatricyclo-[] decane) is reported. Experiments of the biophysical characterization showed an ability to interact with biological membranes, as well as with proteins (e.g. human serum albumin) without affecting their usual biological activity. These metallodendrimers possessed potent and selective anticancer ac...
Top fields of study
Chemical synthesis
Organic chemistry