BIOMAT Database Logo BIOMAT Database Logo

Synthesis of chalcone-imide derivatives and investigation of their anticancer and antimicrobial activities, carbonic anhydrase and acetylcholinesterase enzymes inhibition profiles. 2018

Umit Muhammet Kocyigit, and Yakup Budak, and Meliha Burcu Gürdere, and Fatih Ertürk, and Belkız Yencilek, and Parham Taslimi, and İlhami Gülçin, and Mustafa Ceylan
a Vocational School of Health Services , Cumhuriyet University , Sivas , Turkey.

The new 1-(4-(3-(aryl)acryloyl)phenyl)-1H-pyrrole-2,5-diones (5a-g) were prepared from 4'-aminchalcones (3a-g) and screened for biological activities. All compounds (3a-g and 5a-g), except 3d and 3e displayed good cytotoxic activities with IC50 values in the range of 7.06-67.46 μM. IC50 value of 5-fluorouracil (5-FU) was 90.36 μM. Moreover, most of compounds 5a-g showed high antibacterial activity with 8-20 mm of inhibition zone (19-25 mm of Sulbactam-Cefoperazone (SCF)). In addition, they showed good inhibitory action against acetylcholinesterase (AChE), and human carbonic anhydrase I, and II (hCA I and hCA II) isoforms. Also, these compounds demonstrated effective inhibition profiles with Ki values of 426.47-699.58 nM against hCA I, 214.92-532.21 nM against hCA II, and 70.470-229.42 nM against AChE. On the other hand, acetazolamide, clinically used drug, showed a Ki value of 977.77 ± 227.4 nM against CA I, and 904.47 ± 106.3 nM against CA II, respectively. Also, tacrine inhibited AChE showed a Ki value of 446.56 ± 58.33 nM.

UI MeSH Term Description Entries
D007094 Imides Organic compounds containing two acyl groups bound to NITROGEN. Imide
D007700 Kinetics The rate dynamics in chemical or physical systems.
D002176 Candida albicans A unicellular budding fungus which is the principal pathogenic species causing CANDIDIASIS (moniliasis). Candida albicans var. stellatoidea,Candida stellatoidea,Dematium albicans,Monilia albicans,Myceloblastanon albicans,Mycotorula albicans,Parasaccharomyces albicans,Procandida albicans,Procandida stellatoidea,Saccharomyces albicans,Syringospora albicans
D002257 Carbonic Anhydrase Inhibitors A class of compounds that reduces the secretion of H+ ions by the proximal kidney tubule through inhibition of CARBONIC ANHYDRASES. Carbonate Dehydratase Inhibitor,Carbonate Dehydratase Inhibitors,Carbonic Anhydrase Inhibitor,Carboxyanhydrase Inhibitor,Carboxyanhydrase Inhibitors,Anhydrase Inhibitor, Carbonic,Dehydratase Inhibitor, Carbonate,Inhibitor, Carbonate Dehydratase,Inhibitor, Carbonic Anhydrase,Inhibitor, Carboxyanhydrase,Inhibitors, Carbonate Dehydratase,Inhibitors, Carbonic Anhydrase,Inhibitors, Carboxyanhydrase
D002277 Carcinoma A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for "cancer." Carcinoma, Anaplastic,Carcinoma, Spindle-Cell,Carcinoma, Undifferentiated,Carcinomatosis,Epithelial Neoplasms, Malignant,Epithelioma,Epithelial Tumors, Malignant,Malignant Epithelial Neoplasms,Neoplasms, Malignant Epithelial,Anaplastic Carcinoma,Anaplastic Carcinomas,Carcinoma, Spindle Cell,Carcinomas,Carcinomatoses,Epithelial Neoplasm, Malignant,Epithelial Tumor, Malignant,Epitheliomas,Malignant Epithelial Neoplasm,Malignant Epithelial Tumor,Malignant Epithelial Tumors,Neoplasm, Malignant Epithelial,Spindle-Cell Carcinoma,Spindle-Cell Carcinomas,Tumor, Malignant Epithelial,Undifferentiated Carcinoma,Undifferentiated Carcinomas
D002800 Cholinesterase Inhibitors Drugs that inhibit cholinesterases. The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract and urinary bladder, the eye, and skeletal muscles; they are also used for their effects on the heart and the central nervous system. Acetylcholinesterase Inhibitor,Acetylcholinesterase Inhibitors,Anti-Cholinesterase,Anticholinesterase,Anticholinesterase Agent,Anticholinesterase Agents,Anticholinesterase Drug,Cholinesterase Inhibitor,Anti-Cholinesterases,Anticholinesterase Drugs,Anticholinesterases,Cholinesterase Inhibitors, Irreversible,Cholinesterase Inhibitors, Reversible,Agent, Anticholinesterase,Agents, Anticholinesterase,Anti Cholinesterase,Anti Cholinesterases,Drug, Anticholinesterase,Drugs, Anticholinesterase,Inhibitor, Acetylcholinesterase,Inhibitor, Cholinesterase,Inhibitors, Acetylcholinesterase,Inhibitors, Cholinesterase,Inhibitors, Irreversible Cholinesterase,Inhibitors, Reversible Cholinesterase,Irreversible Cholinesterase Inhibitors,Reversible Cholinesterase Inhibitors
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D006090 Gram-Negative Bacteria Bacteria which lose crystal violet stain but are stained pink when treated by Gram's method. Gram Negative Bacteria
D006094 Gram-Positive Bacteria Bacteria which retain the crystal violet stain when treated by Gram's method. Gram Positive Bacteria
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man

Related Publications

Umit Muhammet Kocyigit, and Yakup Budak, and Meliha Burcu Gürdere, and Fatih Ertürk, and Belkız Yencilek, and Parham Taslimi, and İlhami Gülçin, and Mustafa Ceylan
Evaluation of antimicrobial, antibiofilm and carbonic anhydrase inhibition profiles of 1,3-bis-chalcone derivatives.
April 2019, Journal of biochemical and molecular toxicology,
Umit Muhammet Kocyigit, and Yakup Budak, and Meliha Burcu Gürdere, and Fatih Ertürk, and Belkız Yencilek, and Parham Taslimi, and İlhami Gülçin, and Mustafa Ceylan
The synthesis of some β-lactams and investigation of their metal-chelating activity, carbonic anhydrase and acetylcholinesterase inhibition profiles.
January 2016, Journal of enzyme inhibition and medicinal chemistry,
Umit Muhammet Kocyigit, and Yakup Budak, and Meliha Burcu Gürdere, and Fatih Ertürk, and Belkız Yencilek, and Parham Taslimi, and İlhami Gülçin, and Mustafa Ceylan
Synthesis of novel bis-sulfone derivatives and their inhibition properties on some metabolic enzymes including carbonic anhydrase, acetylcholinesterase, and butyrylcholinesterase.
November 2019, Journal of biochemical and molecular toxicology,
Umit Muhammet Kocyigit, and Yakup Budak, and Meliha Burcu Gürdere, and Fatih Ertürk, and Belkız Yencilek, and Parham Taslimi, and İlhami Gülçin, and Mustafa Ceylan
Synthesis of some novel pyridine compounds containing bis-1,2,4-triazole/thiosemicarbazide moiety and investigation of their antioxidant properties, carbonic anhydrase, and acetylcholinesterase enzymes inhibition profiles.
January 2018, Journal of biochemical and molecular toxicology,
Umit Muhammet Kocyigit, and Yakup Budak, and Meliha Burcu Gürdere, and Fatih Ertürk, and Belkız Yencilek, and Parham Taslimi, and İlhami Gülçin, and Mustafa Ceylan
Synthesis of chalcone derivatives on steroidal framework and their anticancer activities.
November 2007, Steroids,
Umit Muhammet Kocyigit, and Yakup Budak, and Meliha Burcu Gürdere, and Fatih Ertürk, and Belkız Yencilek, and Parham Taslimi, and İlhami Gülçin, and Mustafa Ceylan
The first synthesis of 4-phenylbutenone derivative bromophenols including natural products and their inhibition profiles for carbonic anhydrase, acetylcholinesterase and butyrylcholinesterase enzymes.
June 2017, Bioorganic chemistry,
Umit Muhammet Kocyigit, and Yakup Budak, and Meliha Burcu Gürdere, and Fatih Ertürk, and Belkız Yencilek, and Parham Taslimi, and İlhami Gülçin, and Mustafa Ceylan
Synthesis of 2-amino-3-cyanopyridine derivatives and investigation of their carbonic anhydrase inhibition effects.
December 2017, Journal of biochemical and molecular toxicology,
Umit Muhammet Kocyigit, and Yakup Budak, and Meliha Burcu Gürdere, and Fatih Ertürk, and Belkız Yencilek, and Parham Taslimi, and İlhami Gülçin, and Mustafa Ceylan
Synthesis and characterization of novel substituted thiophene derivatives and discovery of their carbonic anhydrase and acetylcholinesterase inhibition effects.
March 2019, Journal of biochemical and molecular toxicology,
Umit Muhammet Kocyigit, and Yakup Budak, and Meliha Burcu Gürdere, and Fatih Ertürk, and Belkız Yencilek, and Parham Taslimi, and İlhami Gülçin, and Mustafa Ceylan
Synthesis of new cyclic thioureas and evaluation of their metal-chelating activity, acetylcholinesterase, butyrylcholinesterase, and carbonic anhydrase inhibition profiles.
July 2017, Journal of biochemical and molecular toxicology,
Umit Muhammet Kocyigit, and Yakup Budak, and Meliha Burcu Gürdere, and Fatih Ertürk, and Belkız Yencilek, and Parham Taslimi, and İlhami Gülçin, and Mustafa Ceylan
Schiff bases and their amines: Synthesis and discovery of carbonic anhydrase and acetylcholinesterase enzymes inhibitors.
September 2018, Archiv der Pharmazie,
Copied contents to your clipboard!