Article
Biochemistry & Molecular Biology
Yu Wang, Yajing Liu, Tingjie Ge, Jiechun Tang, Shihui Wang, Zhanfeng Gao, Jiaxu Chen, Jundong Xu, Ping Gong, Yanfang Zhao, Jiuyu Liu, Yunlei Hou
Summary: In this study, novel semicarbazone derivatives were designed and synthesized to be potent and selective PI3K alpha inhibitors. Compound A10 showed extraordinary selectivity and inhibition activity against PI3K alpha, and demonstrated significant anticancer effects in both cell and animal models.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Lukasz Tomorowicz, Beata Zolnowska, Krzysztof Szafranski, Jaroslaw Chojnacki, Ryszard Konopinski, Ewa A. Grzybowska, Jaroslaw Slawniski, Anna Kawiak
Summary: In the search for new compounds with antitumor activity, new potential anticancer agents were designed as molecular hybrids containing the structures of a triazine ring and a sulfonamide fragment. The obtained compounds showed cytotoxic activity against tumor cell lines and induced cell cycle arrest and apoptosis. The study also revealed the key role of certain substituents for the cytotoxic activity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Renkai Li, Winston Wing-Shum Mak, Jingjing Li, Chengwen Zheng, Polly Ho-Ting Shiu, Sai-Wang Seto, Simon Ming-Yuen Lee, George Pak-Heng Leung
Summary: This study identified compound 3c as a selective and irreversible non-competitive inhibitor of ENT1 and ENT2, which is a derivative of FPMINT. The structure-activity relationship analysis revealed the importance of the position of benzene moiety and the addition of halogen substitutes for the inhibitory effects. These findings contribute to the development of more potent and selective drugs.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Materials Science, Multidisciplinary
Tianheng Chen, Hao Yu, Xianfei Wen, Caleb Redding, Tibor Jacob Hajagos, Hongxiang Zhao, Jason P. Hayward, Chuluo Yang, Qibing Pei
Summary: A highly efficient TADF dye was reported for PSD applications, which can achieve high scintillation light yield and PSD figures of merit in plastic scintillators. Introducing a secondary dye further increased the efficiency of excitation energy utilization in achieving high light yield.
ADVANCED OPTICAL MATERIALS
(2021)
Article
Chemistry, Organic
Jaroslaw Sukiennik, Katarzyna Kasperowicz-Frankowska, Malgorzata Szczesio, Justyna Fraczyk, Beata Kolesinska, Zbigniew J. Kaminski
Summary: Quinine reacts with CDMT in a multistage process, leading to the attachment of two triazinyl substituents to the quinoline molecule, confirmed by various analytical techniques.
Article
Biochemistry & Molecular Biology
Takayuki Ohnuma, Tomoki Taku, Takeshi Nagatani, Atsushi Horii, Shun Imaoka, Tomonari Tanaka
Summary: The chemo-enzymatic synthesis of lacto-N-biose I (LNB) catalyzed by beta-1,3-galactosidase from Bacillus circulans (BgaC) was achieved using 4,6-dimethoxy-1,3,5-triazin-2-yl beta-galactopyranoside (DMT-beta-Gal) and GlcNAc as substrates. BgaC transferred the Gal moiety to the acceptor to produce LNB, with the maximum yield obtained at a ratio of 1:30 for acceptor to donor substrates.
BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Tiruhi Gomktsyan, Angelina Khachatryan, Diana Avakyan, Lernik Hunanyan, Roza Shainova, Armen Karapetyan, Emma Ghazaryan, Asya Vorskanyan, Margarita Dovlatyan, Yana Gharibyan, Aleksandr Yengoyan, Vergush Pivazyan
Summary: This study employed an eco-friendly ultrasound-assisted synthesis method to produce a series of novel compounds, and conducted in silico studies to predict their biological activities. Additionally, physicochemical and pharmacokinetic properties were calculated, providing valuable reference for the application of these compounds.
GREEN PROCESSING AND SYNTHESIS
(2023)
Article
Chemistry, Inorganic & Nuclear
Tian Wen-Yu, Chu Jin-Feng
Summary: Three azide bridged complexes were synthesized using different metal ions connecting modes. Additionally, a copper(II) complex was successfully prepared, and all complexes were characterized and analyzed for their properties.
CHINESE JOURNAL OF STRUCTURAL CHEMISTRY
(2021)
Article
Multidisciplinary Sciences
Hitler Louis, Obieze C. Enudi, Joseph O. Odey, Izubundu B. Onyebuenyi, Azuaga T. Igbalagh, Tomsmith O. Unimuke, Tabe N. Ntui
Summary: In this study, a cyanurated H-acid (CHA) azo dye was synthesized and characterized, and its molecular orbital excitation properties were investigated using density functional theory and spectroscopic analysis. The low energy gap obtained from molecular orbital analysis indicates the feasibility of HOMO-LUMO transitions, making CHA suitable for electronic and optic applications. The study of excitations revealed different types of local and charge transfer interactions, contributing to the stabilization of the compound. This study is valuable for understanding the molecular properties of azo dyes and for the synthesis of new compounds in the future.
SN APPLIED SCIENCES
(2021)
Article
Chemistry, Medicinal
Hao-Yue Xiang, Xiang Wang, Yan-Hong Chen, Xi Zhang, Cun Tan, Yi Wang, Yi Su, Zhi-Wei Gao, Xiao-Yan Chen, Bing Xiong, Zhao-Bing Gao, Yi Chen, Jian Ding, Ling-Hua Meng, Chun-Hao Yang
Summary: The PI3Ks pathway is commonly dysregulated in human cancers, making it a promising target for anti-cancer drugs. Compound 37 (CYH33) was identified as a selective PI3Ka inhibitor with potential anti-cancer properties, inhibiting phosphorylation of AKT to modulate the PI3K/AKT/mTOR pathway in human cancer cells. Evaluation in vivo against SKOV-3 xenograft models demonstrated dose-dependent antitumor efficacy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Inorganic & Nuclear
Xiaowen Xu, Anne K. Seiffert, Ruben Lenaerts, Kanykei Ryskulova, Somdeb Jana, Kristof Van Hecke, Valentin Victor Jerca, Richard Hoogenboom
Summary: The study demonstrated a straightforward synthesis route to prepare bis-tridentate 4,6-bis((1H-1,2,3-triazol-4-yl)-pyridin-2-yl)-2-phenylpyrimidine ligands and their self-assembly into [2 x 2] grid-like metal complexes through double CuAAC click chemistry. Additionally, four macromolecular ligands were synthesized for the construction of star-shaped supramolecular polymers, showing successful formation confirmed by UV-vis titration measurements and MALDI-TOF mass spectrometry. The chemical structure of the polymer was found to significantly influence the [2 x 2] grid formation, with PEG ligands successful but not the PEtOx ligands.
DALTON TRANSACTIONS
(2021)
Article
Biochemistry & Molecular Biology
Olga V. Mikolaichuk, Elena A. . Popova, Alexandra V. Protas, Olga S. Shemchuk, Lubov V. Vasina, Yulia N. Pavlyukova, Artem A. Potanin, Oleg E. Molchanov, Dmitrii N. Maistrenko, Konstantin N. Semenov, Vladimir V. Sharoyko
Summary: This study investigated the stability, compatibility, antioxidant properties, and cytotoxicity of a tetrazole-containing derivative of 1,3,5-triazine. The derivative showed stability in neutral and alkaline conditions, but undergoes hydrolysis in acidic environments. It exhibited good hemocompatibility and antioxidant properties, but did not exhibit antiradical activity. Furthermore, it demonstrated cytotoxic effects on various cancer cell lines, potentially through HIF pathway inhibition.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2022)
Article
Chemistry, Organic
Muhammad Syafiq Bin Shahari, Ahmad Junaid, Edward R. T. Tiekink, Anton Dolzhenko
Summary: A new method for the fast synthesis of diverse 4-aryl-6-cycloamino-1,3,5-triazin-2-amines was developed using microwave irradiation in a one-pot manner. The targeted compounds showed potent antileukemic activity, indicating the potential biological activity of this method.
SYNTHESIS-STUTTGART
(2021)
Article
Chemistry, Multidisciplinary
Nian Rao, Yuyu Ding, Lan Yang, Yue Zhou, Yi Le, Longjia Yan, Li Liu
Summary: 1,3,5-Triazine derivatives have a wide range of biological and pharmaceutical activities. In this study, a specific triazine derivative was synthesized and characterized, and its crystal structure and biological activity were investigated.
MOLECULAR CRYSTALS AND LIQUID CRYSTALS
(2023)
Article
Chemistry, Multidisciplinary
Yunseung Kuk, Kang Min Ok
Summary: New enantiomorphic Pb-based metal-organic coordination polymers with high water and chemical stabilities have been synthesized, showing selective adsorption of anionic organic dyes. The complexes exhibit second-harmonic generation signals and the effect of pH and particle size on adsorption has been discussed in detail.
MATERIALS CHEMISTRY FRONTIERS
(2021)
