Article
Chemistry, Medicinal
Jiri Rehulka, Ivanna Subtelna, Anna Kryshchyshyn-Dylevych, Alina Cherniienko, Aleksandra Ivanova, Mariia Matveieva, Pavel Polishchuk, Sona Gurska, Marian Hajduch, Oleh Zagrijtschuk, Petr Dzubak, Roman Lesyk
Summary: This study identified hit-compounds with anticancer activity against different cancer cell lines, inhibiting the growth of daunorubicin and paclitaxel-resistant cell lines. The hit compounds induced apoptosis and cellular proliferation in treated cells, and they showed mitotic arrest by interacting with tubulin and inhibiting its polymerization.
ARCHIV DER PHARMAZIE
(2022)
Article
Chemistry, Organic
Hairui Du, Tao Qin, Heye Zhou, Bin Liu
Summary: A ligand and base-free copper-catalyzed method has been developed for the synthesis of O-arylated pyrazolin-5ones from readily available reagents. This methodology exhibits broad substrate scope and tolerance towards a wide range of functional groups. Control experiments demonstrated that specific diaryliodonium salts notably enhance reactivity in the O-arylation process of pyrazolin-5-ones.
TETRAHEDRON LETTERS
(2023)
Article
Chemistry, Organic
Meng-Hao Yi, Hai-Shan Jin, Ru-Bing Wang, Li-Ming Zhao
Summary: An efficient copper-catalyzed cascade annulation of o-hydroxyphenyl propargylamines and pyrazolin-5-ones is described, leading to the rapid assembly of a series of valuable pyrano[2,3-c]pyrazoles with good yields across a wide range of substrates in a simple fashion. The mechanistic elucidation is well supported by control experiment and literature precedents.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Review
Polymer Science
Alya M. Al-Etaibi, Morsy Ahmed El-Apasery
Summary: This study synthesized new dyes using microwave technology and demonstrated their superior efficiency compared to traditional methods. Additionally, using ultrasonic technology, the study achieved higher color depth in dyeing polyester fabrics at lower temperatures. The study also highlighted the biological activity and fastness properties of the synthesized dyes.
Article
Chemistry, Physical
Abdel Majid A. Adam, Tariq A. Altalhi, Hosam A. Saad, Moamen S. Refat, Mohamed S. Hegab
Summary: This study investigated the charge-transfer chemistry of pyrazole derivative FP with five p-acceptors, demonstrating the formation of stable CT complexes through an n -> pi* transition. Strong statistically significant correlations were found between various spectroscopic parameters.
JOURNAL OF MOLECULAR LIQUIDS
(2021)
Article
Chemistry, Organic
Cheng-Yong Wang, Jiang-Xi Yu, Bang Liu, Fu-Xing Zhang, Zhi-Qiang Wang, Qin-Yu Hu, Zhi-Feng Xu, Jin-Heng Li
Summary: We report a DTBP-mediated oxidative [4 + 2]/[3 + 2] annulation between 2-alkynylbenzaldehydes and terminal arylalkenes enabled by aldehyde C(sp(2))-H functionalization for the synthesis of a range of benzo[a]fluoren-5-ones. This method offers high step-economy, simple operation under metal-/solvent-free conditions, and excellent functional group tolerance. It provides a useful new strategy for constructing complex benzo[a]fluoren-5-one scaffolds compared to existing protocols using alkene reaction partners.
ORGANIC CHEMISTRY FRONTIERS
(2022)
Article
Chemistry, Medicinal
Ivanna Subtelna, Anna Kryshchyshyn-Dylevych, Ruochen Jia, Maryan Lelyukh, Anna Ringler, Stefan Kubicek, Oleh Zagrijtschuk, Robert Kralovics, Roman Lesyk
Summary: Research suggests that 5-arylidyne-2-(4-hydroxyphenyl)aminothiazol-4(5H)-ones may have anticancer properties, with compounds like (5Z)-5-(2-methoxybenzylidene) demonstrating high antileukemic activity at submicromolar concentrations comparable to or lower than chlorambucil.
ARCHIV DER PHARMAZIE
(2021)
Article
Spectroscopy
Tatyana N. Moshkina, Emiliya Nosova, Galina N. Lipunova, Marina S. Valova, Elizaveta F. Petrusevich, Robert Zalesny, Borys Osmialowski, Valery N. Charushin
Summary: 2-(2-Hydroxyphenyl)-3H-quinazolin-4-ones with diverse substituents on the phenol ring and their six-membered difluoroboron complexes were synthesized through a few-stage approach. The photophysical properties of these compounds were studied in two solvents and in the solid state, revealing the impact of substituents and substitution points on the photophysical properties of the dyes. In a THF/water mixture, all ligands showed enhanced emission with increasing water fraction due to aggregation-induced emission.
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY
(2021)
Article
Chemistry, Organic
Xiurong Hu, Haichang Guo, Huajiang Jiang, Renhua Zheng, Yaqin Zhou, Lei Wang
Summary: This study presents a direct, aerobic and visible light photocatalytic approach for synthesizing 4-thiocyanated 5-hydroxy-1H-pyrazoles through the cross-coupling of pyrazolin-5-ones with ammonium thiocyanate. The reaction proceeds under redox-neutral and metal-free conditions, and a series of 4-thiocyanated 5-hydroxy-1H-pyrazoles are obtained easily and efficiently in good to high yields using low-toxicity and inexpensive ammonium thiocyanate as the thiocyanate source.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2023)
Article
Chemistry, Physical
Yong-Liang Ban, Long You, Tao Wang, Li-Zhu Wu, Qiang Liu
Summary: A metallaphotoredox catalysis protocol has been developed for the efficient dearomatization of indoles using readily available N-quinolyl benzamides under environmentally benign conditions. The reaction allows regioselective functionalization of indoles and provides a mild and economical approach to produce a diverse array of products. Preliminary mechanistic studies suggest a single-electron transfer process is involved, with a catalytically competent organometallic Co(bzac)(3) identified.
Article
Optics
Mateusz Chorobinski, Paulina Smialek, Marta Gordel-Wojcik, Elizaveta F. Petrusevich, Eugeniusz Zych, Damian Plazuk, Lukasz Skowronski, Beata Jedrzejewska
Summary: The photophysical and optical properties of 4-(4'-(diphenylamino)benzylidene)-2-phenyloxazol-5(4H)-ones with different peripheral substituents were investigated in various environments. The nature of the substituent on the phenyl ring and the solvent mixture influenced these properties. The brightest emission was observed in solid state for the dye with a phenyl group or no substituent in the para position, while the dye with a cyano functional group showed the strongest emission in chloroform. The spectroscopic behavior of the dyes depended on the solvent mixture.
JOURNAL OF LUMINESCENCE
(2023)
Article
Chemistry, Organic
Mohammad Nikpassand, Zahra Pourkarim
Summary: NiFe2O4@SiO2nPr@glucose was used as a catalyst to synthesize novel 5-pyrazolin-1,2,4-triazazolidine-3-ones (thiones) with high yields in short reaction times. The catalyst showed consistent activity for six cycles, and the synthesized compounds were confirmed by various spectroscopic methods. This eco-friendly and reusable catalyst offers advantages such as high yield, green chemistry principles, and waste reduction.
CURRENT ORGANIC SYNTHESIS
(2021)
Article
Chemistry, Organic
Anatolii Sokolov, Maria A. Sycheva, Dilara A. Farkhutdinova, Ivan N. Myasnyanko, Andrey A. Mikhaylov, Nadezhda S. Baleeva, Anastasia Bochenkova, Mikhail S. Baranov
Summary: This study finds that pyridineacetic acids can undergo dimerization under the action of activating agents, resulting in the formation of 2-hydroxy-3-(pyridin-2-yl)-4H-quinolizin-4-ones. Introducing a difluoroboryl bridge into these derivatives leads to the development of novel highly fluorescent compounds.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Kai-Zhong Fu, Xu-Xin Chen, Ya-Shi Zhao, Yuan-Qing Gu, Guo-Kai Liu
Summary: The CF2H moiety has significant potential in drug design and incorporating it into biologically active molecules is an efficient strategy for finding lead compounds and drug candidates. Quinoxalin-2-one is of great interest to pharmaceutical chemists and frequently occurs in natural products and bioactive compounds. This study presents a practical and efficient method for synthesizing 3-CF2H-quinoxalin-2-ones, which could facilitate the search for potential lead compounds and drug candidates.
Article
Chemistry, Organic
Marta Romaniszyn, Leslaw Sieron, Lukasz Albrecht
Summary: This study demonstrates the use of organocatalytic Brønsted base activation to generate 2π-components for the diastereoselective [8 + 2]-cycloaddition reaction involving 8,8-dicyanoheptafulvene. The use of dienolates leads to the formation of biologically relevant polycyclic products bearing a γ-butyrolactone structural motif, thus expanding the synthetic potential of Brønsted base activated higher-order cycloadditions.
JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Organic
Ghada E. Abd El-Ghani, Magdy A. El-Sayed, El-Sayed El-Desoky
Summary: This study focused on synthesizing novel heterocyclic scaffolds with quinoline moiety and exploring their antimicrobial properties. The synthesized compounds showed promising antimicrobial and antifungal activities, with certain derivatives exhibiting superior efficacy compared to standard antibiotics and antifungals.
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2022)
Article
Chemistry, Organic
Samir Bondock, Omeer Albormani, Ahmed M. Fouda
Summary: This study describes the convenient synthesis of new 5-heteroaryl-thiazoles through reactions of thiazolylenaminone with various compounds and their evaluation for antitumor activity. Among the synthesized thiazoles, compounds 6, 19, and 23a showed potent antitumor profiles without evidence of human toxicity.
POLYCYCLIC AROMATIC COMPOUNDS
(2023)
Article
Chemistry, Multidisciplinary
Samir Bondock, Omeer Albormani, Ahmed M. Fouda
Summary: Novel pyrazoline derivatives bearing thiazole and thiophene moieties were synthesized and evaluated for their anticancer activity. Compounds 8, 14a, and 14f exhibited the highest activity against various cancer cell lines.
RUSSIAN JOURNAL OF GENERAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Mohammad M. Al-Sanea, Tamer M. Nasr, Samir Bondock, Aya Y. Gawish, Nada M. Mohamed
Summary: Bis-thiazole derivatives were synthesized based on the Pim1 pharmacophore model and showed strong inhibitory effects on Pim1 activity. Derivatives 3b and 8b exhibited the best Pim1 inhibition with IC50 values of 0.32 and 0.24 μM, respectively, compared to staurosporine (IC50 = 0.36 μM). They also effectively arrested the cell cycle at G0/G1 and S phases, as demonstrated by the significant accumulation of cells in these phases. In vivo cytotoxic evaluation confirmed their potent antitumor activity, with 8b showing additional up-regulation of caspase-3 and down-regulation of VEGF and TNF alpha immune expression.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Sanaa M. Emam, Samir Bondock, Ahmed A. M. Aldaloa
Summary: A new thiosemicarbazone ligand containing an allyl group and a 5-pyrazolone derivative was synthesized. The ligand reacted with chloride and nitrate salts of Co(II), Cu(II), Pd(II), and Ni(II), Cu(II) ions, resulting in the formation of different chelates with variable chemical formulas. Structural characterization of the ligand and its chelates was established using various spectroscopic and analytical techniques. The chelates exhibited square pyramidal structures, except for those of Co(II) and Pd(II) ions, and copper(II) chelates showed the highest anticancer activity against hepatocellular carcinoma cells (Hep G-2) in biological studies.
RESULTS IN CHEMISTRY
(2023)
Review
Chemistry, Multidisciplinary
Ahmed Abu-Rayyan, Imtiaz Ahmad, Nawal H. Bahtiti, Tahir Muhmood, Samir Bondock, Mohammed Abohashrh, Habiba Faheem, Nimra Tehreem, Aliya Yasmeen, Shiza Waseem, Tayabba Arif, Amal H. Al-Bagawi, Moaz M. Abdou
Summary: The review focuses on optical chemosensors for formaldehyde detection, specifically organic probes, which are cost-effective, portable, and have high detection limits. It discusses various organic functionalities and reaction mechanisms, as well as photophysical phenomena. The review also addresses gas-based and liquid formaldehyde detection and provides recommendations for future research.
Article
Chemistry, Multidisciplinary
Samir Bondock, Tallah Albarqi, Tamer Nasr, Nada M. Mohamed, Moaz M. Abdou
Summary: New thiadiazole sulfonamide derivatives were designed as human carbonic anhydrase inhibitors (hCAIs) to develop robust and novel anticancer agents. The target compounds were synthesized using a two-step procedure starting from 5-acetyl-3-N-(4-sulfamoylphenyl)-2-imino-1,3,4-thiadiazoline and a tail modification approach. Cytotoxic evaluation revealed the potent activity of the synthesized compounds against various cancer cell lines, and molecular docking and ADME evaluation provided insights into their mechanism of action.
ARABIAN JOURNAL OF CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Mahmoud M. Shaban, N. M. El Basiony, A. Bahgat Radwan, Emad E. El-Katori, Ahmed Abu-Rayyan, Nawal H. Bahtiti, Moaz M. Abdou
Summary: The inhibitory effect of two synthesized pyrazole derivatives (3 and 4) on metallic and microbial corrosion was investigated. The compounds demonstrated the ability to prevent corrosion of C-steel in 1 M HCl with increasing concentration. They acted as mixed-type inhibitors and followed the Langmuir isotherm adsorption model. The research also highlighted the antimicrobial performance of the compounds against sulfate-reducing bacteria.
Article
Chemistry, Multidisciplinary
Samir Bondock, Tallah Albarqi, Mohamed Abboud, Tamer Nasr, Nada M. Mohamed, Moaz M. Abdou
Summary: A novel series of thiazole hybrids targeting hCAIX were synthesized and evaluated for their cytotoxicity. The compounds showed enhanced cytotoxicity against different cancer cell lines, with some derivatives exhibiting significant improvements. Molecular docking and dynamic simulation studies provided insights into the binding of the compounds with the target enzyme and their potential mechanism of action.
Article
Chemistry, Multidisciplinary
Samir Bondock, Tallah Albarqi, Ibrahim A. Shaaban, Moaz M. Abdou
Summary: In this study, novel differently substituted unsymmetrical azine-modified thiadiazole sulfonamide derivatives were designed and prepared using the combi-targeting approach for potential anticancer therapy. The E/Z configuration and chemical shifts of the synthesized compounds were determined through spectroscopic analysis and quantum mechanical calculations, which were consistent with experimental data, suggesting their existence in solution. The biological activities of the synthesized compounds were predicted using molecular reactivity descriptors and ADMT/drug-likeness properties.
Article
Chemistry, Multidisciplinary
Samir Bondock, Tallah Albarqi, Moaz M. Abdou, Nada M. Mohamed
Summary: Vascular endothelial growth factor VEGFR-2 has been identified as a potential target for anticancer agents. In this study, ten benzenesulfonamide-1,3,4-thiadiazole hybrids were synthesized and two compounds, 8c and 8e, exhibited potent inhibition against HepG-2 cells. Molecular docking and molecular dynamics simulations confirmed their binding to VEGFR-2.
NEW JOURNAL OF CHEMISTRY
(2023)
Review
Chemistry, Multidisciplinary
Moaz M. Abdou, Ahmed Abu-Rayyan, Ahmed G. Bedir, S. Abdel-Fattah, A. M. A. Omar, Abdullah A. Ahmed, El-Sayed El-Desoky, Eslam A. Ghaith
Summary: This review emphasizes recent advances in synthetic routes of 3-(bromoacetyl)coumarin derivatives and their versatility as building blocks in the preparation of polyfunctionalized heterocyclic systems and industrially significant scaffolds. It also highlights the attractiveness of 3-(bromoacetyl)coumarins as starting points for a wide range of five and six-membered heterocyclic systems. Additionally, the review covers the wide-ranging applications of these moieties in analytical chemistry, fluorescent sensors, and biological settings.
Article
Polymer Science
Mohamed Abboud, Samir Bondock, Adel A. El-Zahhar, Majed M. Alghamdi, Sherif M. A. S. Keshk
Summary: This study presents a new eco-friendly flame-retardant nanocomposite combining dialdehyde cellulose (DAC) and amino-functionalized mesoporous silica MCM-41 (N-M41), showing improved fire performance. The mechanism of reduced flammability of this nanocomposite has been proposed based on experimental data.
JOURNAL OF APPLIED POLYMER SCIENCE
(2021)
