Styrylquinoline derivatives are demonstrated to be HIV-1 integrase inhibitors. On the basis of our previous CoMFA analysis of a series of styrylquinoline derivatives, N-[(2-substituted-styryl)-5-chloro-8-hydroxyquinolin-7-yl]-benzenesulfonamide derivatives were designed and synthesized,and their possible HIV IN inhibitory activity was evaluated.
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http://dx.doi.org/10.3390/molecules15031903 | DOI Listing |
Sci Rep
November 2024
A. Chelkowski Institute of Physics, University of Silesia in Katowice, 75 Pulku Piechoty 1a, Chorzow, 41- 500, Poland.
In the present study, a detailed analysis of the effect of a substitution at the C4 position of the quinoline ring by styryl or furanylvinyl substituents on the structure-antitumour activity relationship was conducted. After analysing a library of derivatives from the styrylquinoline and furanylvinylquinoline groups, we selected the most active (IC below 100 nM) derivative 13, which contained the strongly electron-withdrawing nitro group in the furan substituent. The mechanism of action of this compound was studied on cell lines that differed in their p53 protein status.
View Article and Find Full Text PDFJ Biomol Struct Dyn
February 2025
Department of Basic Sciences, Faculty of Engineering, Architecture and Design, Bartin University, Bartin, Turkey.
Two novel quinoline-anthracene conjugates comprising styrylquinoline and anthracene moieties linked by triazole bridges were designed and synthesized in good yields. These molecules were determined for some metabolic enzymes activities. Results indicated that the synthetic molecules exhibited powerful inhibitory actions against all aims as compared to the control molecules.
View Article and Find Full Text PDFHeliyon
November 2022
Mechanic, Materials and complex structures Laboratory, Department of Physics, Faculty of Science, University of Yaoundé I, P.O. Box 812, Yaoundé, Cameroon.
Hartree-Fock (HF) and Density Functional Theory (DFT) studies were conducted to assess the impact of potassium doping on the thermodynamic, optoelectronic, electronic and nonlinear optical properties and on the reactivity of photochromic polymers containing styrylquinoline fragments. Doping was carried out on the virgin monomer (M1) and on the derivative monomer (M2) with the nitro group NO. Three doped monomers were investigated including, the monomer M3 obtained from M1 by substituting the H atom with a potassium, the monomer M4 by substituting two H atoms and the monomer M5 obtained from M2 by substituting the H atom.
View Article and Find Full Text PDFMolecules
October 2022
Medical and Experimental Mycology Group, CIB-UPB-UdeA-UDES, Medellin 050034, Colombia.
Seven styrylquinolines were synthesized in this study. Two of these styrylquinolines are new and were elucidated by spectroscopic analysis. The chemopreventive potential of these compounds was evaluated against SW480 human colon adenocarcinoma cells, its metastatic derivative SW620, and normal cells (HaCaT).
View Article and Find Full Text PDFACS Med Chem Lett
October 2022
Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan.
Synucleinopathies are characterized by the deposition of α-synuclein (α-syn) aggregates before the onset of clinical symptoms. Therefore, imaging of α-syn may contribute to early diagnosis of these diseases and has attracted much attention in recent years. However, no clinically useful probes have been reported.
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