Article
Biochemistry & Molecular Biology
Manel Ben Hassen, Dhouha Msalbi, Badr Jismy, Fares Elghali, Sami Aifa, Hassan Allouchi, Mohamed Abarbri, Fakher Chabchoub
Summary: A series of new [1,2,4]triazolo[4,3-a]pyrimidine derivatives were synthesized using a one-pot three-component synthesis. The structures of the compounds were confirmed by various analyses. The compounds were evaluated for their antitumor activity and displayed promising results against cancer cell lines.
Article
Chemistry, Applied
Yue Sun, Sihao Ling, Yubo Duan, Jingxian Li, Zhengkai Chen, Xiao-Feng Wu
Summary: A metal-free approach for constructing 5-trifluoromethyl-1,4-dihydro-1,2,4-triazines has been developed using base-mediated [3+3] cycloaddition. This protocol offers readily available starting materials, mild reaction conditions, a broad substrate scope, high efficiency, good synthetic prospect, and scalability.
ADVANCED SYNTHESIS & CATALYSIS
(2023)
Article
Biochemistry & Molecular Biology
Fatma A. M. Mohamed, Hesham A. M. Gomaa, O. M. Hendawy, Asmaa T. Ali, Hatem S. Farghaly, Ahmed M. Gouda, Ahmed H. Abdelazeem, Mostafa H. Abdelrahman, Laurent Trembleau, Bahaa G. M. Youssif
Summary: The new series of EGFR inhibitors showed promising antiproliferative activity against cancer cell lines, with para-substituted phenethyl derivatives displaying superior activity. Some compounds also exhibited potential EGFR inhibitory activity, modulation of apoptosis-related proteins, and cell cycle arrest effects.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Dongwei Kang, Francesc X. Ruiz, Yanying Sun, Da Feng, Lanlan Jing, Zhao Wang, Tao Zhang, Shenghua Gao, Lin Sun, Erik De Clercq, Christophe Pannecouque, Eddy Arnold, Peng Zhan, Xinyong Liu
Summary: The study focused on a novel anti-HIV-1 drug, 16c, which showed improved potency against NNRTI-resistance mutations through structural modifications. The co-crystal structure of 16c revealed the key role of water networks in binding and resilience against resistance mutations, suggesting further development strategies for the compound. Additionally, 16c demonstrated favorable pharmacokinetic and safety properties, indicating its potential as a promising anti-HIV-1 drug candidate.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Stephen Lo, Euphemia Leung, Bruno Fedrizzi, David Barker
Summary: Quercetin is a flavonoid found in plants with various biological activities. In this study, 5-O-acyl derivatives of quercetin showed improved antiproliferative activity and retained radical scavenging activity against cancer cell lines and radical species.
Article
Chemistry, Multidisciplinary
Qiuyue Zhang, Xuexuan Wu, Hengheng Zhang, Qiuyu Wu, Min Fu, Liwen Hua, Xinyue Zhu, Yuqi Guo, Lianshan Zhang, Qidong You, Lei Wang
Summary: The normal phosphorylation state of proteins is crucial for their function. Hyperphosphorylation of oncoproteins, such as ASK1, can lead to diseases, including gastric cancer. In this study, researchers designed a phosphatase recruitment chimera (PHORC) called DDO3711 to specifically accelerate the dephosphorylation of p-ASK1T838 using a proximity-mediated effect. DDO3711 effectively reduced the level of p-ASK1T838 in vitro and in vivo, showing promising antiproliferative activity against MKN45 cells. This study highlights the potential of PHORCs in regulating abnormal phosphorylation of oncoproteins.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Biochemistry & Molecular Biology
Francisco V. Gaspar, Soraya Marques Ribeiro, Julio C. F. Barcellos, Samuel Monteiro, Jorge L. O. Domingos, Maria Claudia dos Santos Luciano, Carlos R. K. Paier, Claudia Pessoa, Paulo R. R. Costa
Summary: 5-carba-pterocarpans, isosteres of natural pterocarpans, were synthesized and evaluated for potential anti-proliferative activity in various cancer cell lineages, showing promising results for further development as novel antiproliferative agents.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Physical
Shubham Jaiswal, Shivendra Kumar Pandey, Tarun Minocha, S. Chandra, M. K. Bharty, S. K. Yadav, D. Kushwaha, R. J. Butcher
Summary: The global burden of cervical cancer is increasing, and the compound Pypao has been synthesized and characterized. The crystal structure of Pypao is stabilized through intermolecular hydrogen bonding interactions. The binding potential of Pypao to oncoproteins E6, E6AP, and E7 of HPV has been examined through molecular docking study. The anticancer activity of Pypao has been investigated against SiHa cells through various assays.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Physical
Subham G. Patel, Paras J. Patel, Dipti B. Upadhyay, Adrian Puerta, Apoorva Malik, Nagesh K. Kandukuri, Rakesh K. Sharma, Jose M. Padron, Hitendra M. Patel
Summary: In this study, a green approach for the synthesis of spirochromeno[2,3-d]pyrimidines was established using an environmentally friendly polymer catalyst and microwave-assisted multicomponent reaction. The synthesized compounds showed outstanding green credentials with higher yield and no need for purification. The most potent compound, 4j, exhibited excellent antiproliferative activity against six solid human tumor cell lines.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Eva Bokor, Attila Ferenczi, Mahir Hashimov, Eva Juhasz-Toth, Zsofia Gotz, Alshimaa Ibrahim Zaki, Laszlo Somsak
Summary: In this paper, the first synthesis of 3-glycopyranosyl-1,2,4-triazines is accomplished, which were previously unknown. Several related compounds were also synthesized by different reaction pathways.
Article
Chemistry, Organic
Siuli Das, Rakesh Mondal, Amit Kumar Guin, Nanda D. Paul
Summary: This study reports ligand-centered redox controlled Zn(II)-catalyzed multicomponent approaches for synthesizing pyrimidines and triazines. The well-defined Zn(II)-catalyst (1a) with redox-active ligand L-1a enables the preparation of substituted pyrimidines and triazines via dehydrogenative alcohol functionalization reactions, with good tolerance towards a wide range of substrates. The active participation of ligand-centered redox events allows the Zn(II)-complex 1a to efficiently act as a catalyst for synthesizing these N-heterocycles, with electron transfer processes occurring at the azo-aromatic ligand during the catalytic reaction.
ORGANIC & BIOMOLECULAR CHEMISTRY
(2022)
Article
Chemistry, Physical
Marcin Stolarczyk, Agnieszka Matera-Witkiewicz, Aleksandra Wolska, Magdalena Krupinska, Aleksandra Mikolajczyk, Anna Pyra, Iwona Bryndal
Summary: Pyrimidine is considered a promising unit for new drug research due to its diverse bioactivities. In this study, a series of derivatives of 5-hydroxymethylpyrimidine were obtained and evaluated for their cytotoxic properties against normal and cancer cell lines. The results showed that derivatives with aliphatic amino groups at the 4-position were less toxic to normal cells compared to those with benzylsulfanyl groups, and compounds with bulky constituents exhibited moderate anticancer properties.
Article
Chemistry, Physical
Bakr F. Abdel-Wahab, Benson M. Kariuki, Hanan A. Mohamed, Mohamed S. Bekheit, Hanem M. Awad, Gamal A. El-Hiti
Summary: The synthesis of heterocycles containing 1,2,3-triazole and pyrazole moieties has been explored for their potential applications in the agrochemical and pharmaceutical fields. These heterocycles have shown promising anti-proliferation properties against cancer cells. In this study, several new 1H-1,2,3-triazole derivatives were successfully synthesized using simple procedures, and their activity against different types of cancer cells and normal cells was evaluated.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Edua Kovacs, Hazhmat Ali, Renata Minorics, Peter Traj, Vivien Resch, Gabor Paragi, Bella Bruszel, Istvan Zupko, Erzsebet Mernyak
Summary: Novel 13 alpha-estrone derivatives were synthesized through direct arylation of the phenolic hydroxy function. The antiproliferative activities of the synthesized compounds against human cancer cell lines were investigated, and the quinoline derivative showed substantial activity with low IC50 values. Disturbance of tubulin polymerization was confirmed, and computational calculations revealed significant interactions of the quinoline derivative with the taxoid binding site of tubulin.
Article
Chemistry, Medicinal
Lamya H. H. Al-Wahaibi, Essmat M. M. El-Sheref, Mohamed M. M. Hammouda, Bahaa G. M. Youssif
Summary: Novel 4-((quinolin-4-yl)amino)-thia-azaspiro[4.4/5]alkan-3-ones were synthesized via a one-step reaction between 4-(2-cyclodenehydrazinyl)quinolin-2(1H)-one and thioglycolic acid catalyzed by thioglycolic acid. The newly obtained compounds were characterized by NMR, mass spectra, and elemental analyses. Among them, compounds 6b, 6e, and 7b showed the most potent antiproliferative effects.