36983-36-5Relevant academic research and scientific papers
Hybrid organoruthenium(II) complexes with thiophene-β-diketo-benzazole ligands: Synthesis, optical properties, CT-DNA interactions and anticancer activity
Alfaifi, Mohammad Y.,El-Sayed, W. N.,Elbehairi, Serag Eldin I.,Elshaarawy, Reda F. M.,Gad, Emad M.,Ismail, Lamia A.
, (2021)
Two new hybrid half‐sandwiched Ru(II) arene complexes of a general formula [η6-(p-cymene)Ru(L)Cl] (4a,b) {where L = 1-(Benzazol-2-yl)-3-(thiophen-2-yl) propane-1,3-dione} were synthesized and characterized. Spectral and elemental analysis revealed that these complexes have tetrahedral piano stool‐like geometry with a coordination environment composed of two O atoms of ligand, chloride ion, and electron cloud of p‐cymene moiety. The CT-DNA–Ru(II) complexes interactions were evaluated based on absorption and emission titration experiments. The results have shown intercalative modes of interaction between DNA and complexes, with a preferable binding to complex 4b. Based on the in vitro cytotoxicity MTT assay, the complexes exhibit significant inhibitory activity against human breast and lung cancer cells (MCF-7, A549), with lower micromolar IC50 values in comparison to that of clinical drug (cisplatin). In contrast, neither complex shows activity against the normal cell lines (Hela), suggesting that the new hybrid thiophene-β-diketo-benzazole organoruthenium(II) complexes may offer promising safe anticancer agents.
Comprehensive study on potent and selective carbonic anhydrase inhibitors: Synthesis, bioactivities and molecular modelling studies of 4-(3-(2-arylidenehydrazine-1-carbonyl)-5-(thiophen-2-yl)-1H-pyrazole-1-yl) benzenesulfonamides
Yamali, Cem,Sakagami, Hiroshi,Uesawa, Yoshihiro,Kurosaki, Kota,Satoh, Keitaro,Masuda, Yoshiko,Yokose, Satoshi,Ece, Abdulilah,Bua, Silvia,Angeli, Andrea,Supuran, Claudiu T.,Gul, Halise Inci
, (2021)
In this research, rational design, synthesis, carbonic anhydrases (CAs) inhibitory effects, and cytotoxicities of the 4-(3-(2-arylidenehydrazine-1-carbonyl)-5-(thiophen-2-yl)-1H-pyrazole-1-yl)benzenesulfonamides 1–20 were reported. Compound 18 (Ki = 7.0 nM) was approximately 127 times more selective cancer-associated hCA IX inhibitor over hCA I, while compound 17 (Ki = 10.6 nM) was 47 times more selective inhibitor of hCA XI over hCA II compared to the acetazolamide. Compounds 11 (CC50 = 5.2 μM) and 20 (CC50 = 1.6 μM) showed comparative tumor-specificity (TS= > 38.5; >128.2) with doxorubicin (TS > 43.0) towards HSC-2 cancer cell line. Western blot analysis demonstrated that 11 induced slightly apoptosis whereas 20 did not induce detectable apoptosis. A preliminary analysis showed that some correlation of tumor-specificity of 1–20 with the chemical descriptors that reflect hydrophobic volume, dipole moment, lowest hydrophilic energy, and topological structure. Molecular docking simulations were applied to the synthesized ligands to elucidate the predicted binding mode and selectivity profiles towards hCA I, hCA II, and hCA IX.
Synthesis, characterization, thermal analysis and biological study of new thiophene derivative containing o-aminobenzoic acid ligand and its mn(ii), cu(ii) and co(ii) metal complexes
Al-Hazmi, Ghaferah H.,Al-Humaidi, Jehan Y.,Altalhi, Tariq A.,Refat, Moamen S.
, p. 129 - 140 (2021/06/03)
New ligand containing 2-(2,4-dioxo-4-thiophen-2-yl-butyrylamino)-benzoic acid (HL) merged moiety was synthesized and characterized by FT-IR, elemental analyses, mass spectra and 1H-NMR spectral. In the present study, the attempts were carried to form comp
Synthesis, Characterization, Enzyme Inhibitory Activity, and Molecular Docking Analysis of a New Series of Thiophene-Based Heterocyclic Compounds
Bursal, E.,Cetin, A.,Murahari, M.,Türkan, F.
, p. 598 - 604 (2021/06/02)
Abstract: 1-Phenyl-3-(thiophen-2-yl)-1H-pyrazole-5-carboxamide derivatives were designed and evaluated for their in vitro enzyme inhibitory activities against acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and glutathione S-transferase (GST).
ISOXAZOLE CARBOXAMIDE COMPOUNDS AND USES THEREOF
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Page/Page column 39, (2020/04/25)
A compound of Formula (I) or or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating hearing loss or balance disorder: Formula (I) wherein R1 and Y are as defined herein.
Synthesis, biological evaluation and in silico modelling studies of 1,3,5-trisubstituted pyrazoles carrying benzenesulfonamide as potential anticancer agents and selective cancer-associated hCA IX isoenzyme inhibitors
Yamali, Cem,Gul, Halise Inci,Ece, Abdulilah,Bua, Silvia,Angeli, Andrea,Sakagami, Hiroshi,Sahin, Ertan,Supuran, Claudiu T.
, (2019/09/10)
Inhibition of carbonic anhydrases (CAs, EC 4.2.1.1) has clinical importance for the treatment of several diseases. They participate in crucial regulatory mechanisms for balancing intracellular and extracellular pH of the cells. Among CA isoforms, selectiv
INHIBITORS OF SHORT-CHAIN DEHYDROGENASE ACTIVITY FOR PROMOTING NEUROGENESIS AND INHIBITING NERVE CELL DEATH
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Paragraph 00268, (2018/02/27)
A method of promoting neuroprotection in a subject from axonal degeneration, neuronal cell death, and/or glia cell damage after injury, augmenting neuronal signaling underlying learning and memory, stimulating neuronal regeneration after injury, and/or treating a disease, disorder, and/or condition of the nervous system in a subject in need thereof includes administering to the subject a therapeutically effective amount of a 15-PGDH inhibitor.
The First Example of Azole-Fused Cyclic Anhydride Reacting in the Castagnoli-Cushman Way
Moreau, Ella,Dar'In, Dmitry,Krasavin, Mikhail
supporting information, p. 890 - 893 (2018/03/06)
Pyrazole-fused cyclic anhydrides have been employed for the first time as the Castagnoli-Cushman reaction partners to produce hitherto unknown 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5- a ]pyrazine-7-carboxylates in remarkably convenient and speedy fashion. At
ISOXAZOLE CARBOXAMIDE COMPOUNDS AND USES THEREOF
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Paragraph 0133-0134, (2018/10/19)
A compound of Formula (I)) or or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating hearing loss or balance disorder: wherein R1 through R3, and L are as defined herein.
INHIBITORS OF SHORT-CHAIN DEHYDROGENASE ACTIVITY FOR TREATING FIBROSIS
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Paragraph 00279, (2016/09/26)
A method of treating or preventing a fibrotic disease, disorder or condition includes administering to a subject in need of treatment a 15-PGDH inhibitor.
