A5102992786- Synthesis and biological activity
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis of heterocyclic compounds
- Synthesis and Biological Evaluation
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Quinazolinone synthesis and applications
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Click Chemistry and Applications
- Synthesis and Reactivity of Heterocycles
- Multicomponent Synthesis of Heterocycles
- Cancer therapeutics and mechanisms
- Phenothiazines and Benzothiazines Synthesis and Activities
- Computational Drug Discovery Methods
- Synthesis of Organic Compounds
- Melanoma and MAPK Pathways
- Synthesis and Reactions of Organic Compounds
- Asthma and respiratory diseases
- Ferrocene Chemistry and Applications
- Crystallography and molecular interactions
- Bioactive Compounds and Antitumor Agents
- Chemical Synthesis and Analysis
- Lung Cancer Treatments and Mutations
- Lung Cancer Research Studies
- Synthesis and Characterization of Pyrroles
Minia University
2015-2024
Florida Institute of Technology
2016
In this investigation, novel 4-((quinolin-4-yl)amino)-thia-azaspiro[4.4/5]alkan-3-ones were synthesized via interactions between 4-(2-cyclodenehydrazinyl)quinolin-2(1H)-one and thioglycolic acid catalyzed by acid. We prepared a new family of spiro-thiazolidinone derivatives in one-step reaction with excellent yields (67-79%). The various NMR, mass spectra, elemental analyses verified the structures all newly obtained compounds. antiproliferative effects 6a-e, 7a, 7b against four cancer cells...
2,3,4-trisubstituted thiazoles
A series of new pyrazolylquinolin-2-ones were designed and synthesised. The structures the compounds validated by IR, NMR, elemental analysis. evaluated as antiproliferative agents targeting EGFR BRAF V600E .
( E )‐4‐Aryl‐2‐[2‐(1‐substituted ethylidene)hydrazinyl]thiazoles and Z )‐3‐substituted‐4‐aryl‐2‐[( )‐(1‐phenylethylidene)hydrazono]‐2,3‐dihydrothiazoles were synthesized by the reaction of (substituted ethylidene)hydrazinecarbothioamides with ω‐bromoacetophenones. The characterization this new class compounds was performed using different spectroscopic tools. structure )‐3‐benzyl‐4‐(4‐bromophenyl)‐2‐[( )‐(1‐phenylethylidene)hydrazono]‐2,3‐dihydrothiazole 6e unambiguously confirmed...
The reaction of 4-azido-quinolin-2(1H)-ones 1a-e with the active methylene compounds pentane-2,4-dione (2a), 1,3-diphenylpropane-1,3-dione (2b), and K2CO3 was investigated in this study. This approach afforded 4-(1,2,3-triazol-1-yl)quinolin-2(1H)-ones 3a-j high yields purity. All newly synthesized products' structures were identified. Compounds tested for antiproliferative activity against a panel four cancer cell lines. In comparison to reference erlotinib (GI50 = 33), 3f-j most potent...
A series of new quinoline-based derivatives was designed and synthesised. The structures the compounds were validated by IR, NMR, elemental analysis. evaluated as antiproliferative agents targeting EGFR, HER2.
New pyridazinethiones and 1,2,4-triazolo [4,3-b]pyridazinethiones have been obtained during the reaction of thiosemicarbazide its 1,4-disubstituted derivatives with 2,3-diphenylcyclopropenone.The this cyclopropenone two equivalents afforded corresponding 1,2,4-triazolo[4,3-b]pyridazinethiones.However, Nsubstituted hydrazino thiosemicarbazides occurs stoichiometric amounts starting materials to produce pyridazinethiones.The mechanism, in both cases, was described as a formal [3+3]-cycloaddition.
A series of novel 1,2,3-triazoles hybridized with two quinolin-2-ones, was designed and synthesized through click reactions. The structures the compounds were elucidated by NMR, IR, mass spectra in addition to elemental analysis. assessed for their antiapoptotic activity testis, as testicular torsion is main cause male infertility. This effect studied light decreasing tissue damage induced I/R testis rats using N-acetylcysteine (NAC) an reference. Compounds 6a-c most active hybrids...
A mild and versatile method based on Cu-catalyzed [2+3] cycloaddition (Huisgen-Meldal-Sharpless reaction) was developed to tether 3,3'-((4-(prop-2-yn-1-yloxy)phenyl)methylene)bis(4-hydroxyquinolin-2(1H)-ones) with 4-azido-2-quinolones in good yields. This methodology allowed attaching three quinolone molecules via a triazole linker the proposed mechanism. The products are interesting precursors for their anti-proliferative activity. Compound 8g most active one, achieving IC50 = 1.2 ± 0.2 µM...
Although, recent reviews demonstrated intensively on the reactivity of dimethyl acetylenedicarboxylate (DMAD) in organic synthesis, its reactions have still get importance addition that field. Moreover, and due to huge amount published literatures dealing with DMAD, we are trying give more focus important missed light updated publications. DMAD is an compound formula (C 6 H O 4 ), it a diester which ester groups conjugated triple bond. As such, highly electrophilic widely employed as...
Abstract magnified image New 1,2,4‐triazepine‐3‐thiones have been obtained during the respective reactions of N ‐substituted‐hydrazino carbothioamides with dimethyl acetylenedicarboxylate and dibenzoyl acetylene under prolonged reflux in acetic acid and/or DMF. However, reaction starting materials DMF microwave irradiation afforded same products higher yields within a few minutes.
The reaction of (substituted ethylidene)hydrazinecarbothioamides 4a, 4b, 4c, 4d, 4e, 4f, 4g with dimethyl ethynedicarboxylate (DMAD, 2) gave [(substituted ethylidene)hydrazono)-4-oxothiazolidine-5-ylidene]acetates 7a, 7b, 7c, 7d, 7e, 7f, 7g (71–88 %). structure the new compounds was established by infrared spectroscopy, mass spectrometry, and NMR spectroscopy.
Abstract The review summarizes published data on the behavior and reactions of acylthiosemicarbazides their derivatives, which lead to formation heterocyclic systems, including methods preparation in addition synthesis pyrrole, thiazole, thiadiazole, thiadiazolidine, triazole derivatives as well fused compounds. J. Heterocyclic Chem., (2012).
1‐Substituted 3‐[3‐(methyl/phenyl)‐1 H ‐pyrazol‐5‐yl]thioureas react with the triple bond of dimethyl acetylenedicarboxylate forming ( Z )‐methyl 2‐[( )‐3‐substituted‐2‐(3‐(methyl/phenyl‐1 ‐pyrazol‐5‐ylimino)‐4‐oxothiazolidin‐5‐ylidene)acetates. Rational for these conversations are presented.
New classes of 3N-substituted-2-[(3-methyl-1H-pyrazole-5-yl)-imino]-5,6-diphenyl-2H-1,3-thiazin-4(3H)-ones have been synthesized, via one pot reactions between pyrazolylthioureas, 2,3-diphenylcyclopropenone and 2,3-dichloro-5,6-dicyano-1,4-benzoquinone. The structures the products confirmed by different spectroscopic analyses. A rationale for formation is presented.
Our investigation includes the synthesis of new naphthalene-bis-triazole-bis-quinolin-2(1H)-ones 4a–e and 7a–e via Cu-catalyzed [3 + 2] cycloadditions 4-azidoquinolin-2(1H)-ones 3a–e with 1,5-/or 1,8-bis(prop-2-yn-1-yloxy)naphthalene (2) or (6). All structures obtained products have been confirmed different spectroscopic analyses. Additionally, a mild versatile method based on copper-catalyzed cycloaddition (Meldal–Sharpless reaction) was developed to tether quinolinones O-atoms 1,5-...
( Z )‐Methyl 2‐[3‐(arylideneamino)‐2‐(arylidenehydrazono)‐4‐oxothiazolidin‐5‐ylidene]acetate prepared during the reaction between thiocarbonohydrazides and dimethyl acetylene dicarboxylate. Rational for there conversations involving nucleophilic addition on C/C triple bond of acetylenedicarboxylate are presented.