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3 results on '"reduced cytotoxicity"'

1. Design, synthesis, and biological evaluation of piperidinyl‐substituted [1,2,4]triazolo[1,5‐a]pyrimidine derivatives as potential anti‐HIV‐1 agents with reduced cytotoxicity

Author

Boshi Huang, Ye Tian, Peng Zhan, Dirk Daelemans, Dongwei Kang, Erik De Clercq, Christophe Pannecouque, and Xinyong Liu

Subjects
Etravirine, Chemistry, Medicinal, anti-HIV-1 potency, 01 natural sciences, Biochemistry, chemistry.chemical_compound, Drug Discovery, Pharmacology & Pharmacy, DRUG, Cytotoxicity, Biological evaluation, Chemistry, reduced cytotoxicity, HIV Reverse Transcriptase, Molecular Docking Simulation, Reverse Transcriptase Inhibitors, Molecular Medicine, Life Sciences & Biomedicine, medicine.drug, Biochemistry & Molecular Biology, Pyrimidine, Anti-HIV Agents, Cell Survival, Stereochemistry, Cell Line, Structure-Activity Relationship, reverse transcriptase, medicine, Humans, Potency, OPTIMIZATION, EC50, Pharmacology, Science & Technology, Binding Sites, 010405 organic chemistry, Organic Chemistry, BEARING BRIDGEHEAD NITROGEN, molecular docking, Triazoles, DIARYLPYRIMIDINES, Reverse transcriptase, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, Pyrimidines, 4]Triazolo[1, Design synthesis, DISCOVERY, Drug Design, 5-a]pyrimidines, HIV-1, POTENCY, [1, HIV-1 NNRTIS, INHIBITORS
Abstract

Taking the previously reported compound BH-7d as the lead, we designed and synthesized a series of piperidinyl-substituted [1,2,4]triazolo[1,5-a]pyrimidines, and their anti-HIV activities as well as cytotoxicities were evaluated. Several compounds exhibited moderate anti-HIV (IIIB) potency, among which 2b was the most active one (EC50 = 4.29 μM). Structure-activity relationships derived from the antiretroviral results were analyzed. Additionally, most compounds demonstrated reduced cytotoxicity (CC50 > 200 μM) compared with those of BH-7d and etravirine. Molecular docking study further revealed the binding conformation of 2b in the binding pocket of HIV-1 reverse transcriptase. ispartof: CHEMICAL BIOLOGY & DRUG DESIGN vol:97 issue:1 pages:67-76 ispartof: location:England status: published

Published
2020

2. Galvanic Displacement Synthesis of Monodisperse Janus‐ and Satellite‐Like Plasmonic–Magnetic Ag–Fe@Fe3O4 Heterostructures with Reduced Cytotoxicity

Author

Yanglong Hou, Tianyu Tang, Ziyu Yang, Xiaoxiao Huang, Xintai Su, Huilin Zhang, Yanmin Ju, Ya Ding, Xin Chu, and Kai Zhu

Subjects
Materials science, General Chemical Engineering, Dispersity, General Physics and Astronomy, Medicine (miscellaneous), Nanoparticle, 02 engineering and technology, 010402 general chemistry, 01 natural sciences, Biochemistry, Genetics and Molecular Biology (miscellaneous), Silver nanoparticle, Ag–Fe@Fe3O4, Galvanic cell, General Materials Science, galvanic displacement, Plasmon, 5th Anniversary Article, Full Paper, General Engineering, Heterojunction, Full Papers, reduced cytotoxicity, 021001 nanoscience & nanotechnology, 0104 chemical sciences, Anode, Amorphous solid, Chemical engineering, magnetic properties, 0210 nano-technology
Abstract

The unique physicochemical properties of silver nanoparticles offer a large potential for biomedical application, however, the serious biotoxicity restricts their usage. Herein, nanogalvanic couple Ag–Fe@Fe3O4 heterostructures (AFHs) are designed to prevent Ag+ release from the cathodic Ag by sacrificial anodic Fe, which can reduce the cytotoxicity of Ag. AFHs are synthesized with modified galvanic displacement strategy in nonaqueous solution. To eliminate the restriction of lattice mismatch between Fe and Ag, amorphous Fe@Fe3O4 nanoparticles (NPs) are selected as seeds, meanwhile, reductive Fe can reduce Ag precursor directly even at as low as 20 °C without additional reductant. The thickness of the Fe3O4 shell can influence the amorphous properties of AFHs, and a series of Janus‐ and satellite‐like AFHs are synthesized. A “cut‐off thickness” effect is proposed based on the abnormal phenomenon that with the increase of reaction temperature, the diameter of Ag in AFHs decreases. Because of the interphase interaction and the coupling effect of Ag and Fe@Fe3O4, the AFHs exhibit unique optical and magnetic properties. This strategy for synthesis of monodisperse heterostructures can be extended for other metals, such as Au and Cu.

Published
2018

3. Nanoparticles: Galvanic Displacement Synthesis of Monodisperse Janus- and Satellite-Like Plasmonic-Magnetic Ag-Fe@Fe3 O4 Heterostructures with Reduced Cytotoxicity (Adv. Sci. 8/2018)

Author

Kai Zhu, Tianyu Tang, Yanglong Hou, Huilin Zhang, Ziyu Yang, Xin Chu, Xiaoxiao Huang, Xintai Su, Yanmin Ju, and Ya Ding

Subjects
Materials science, biology, business.industry, General Chemical Engineering, Dispersity, General Engineering, Frontispiece, General Physics and Astronomy, Medicine (miscellaneous), Nanoparticle, Heterojunction, reduced cytotoxicity, biology.organism_classification, Biochemistry, Genetics and Molecular Biology (miscellaneous), Ag–Fe@Fe3O4, Galvanic cell, Optoelectronics, General Materials Science, Satellite (biology), Displacement (orthopedic surgery), magnetic properties, Janus, business, galvanic displacement, Plasmon
Abstract

Lattice mismatch is a key obstacle for synthesizing heterostructures with desired constituents. In article number https://doi.org/10.1002/advs.201800271, Xintai Su, Yanglong Hou, and co‐workers develop a facile method to synthesize Janus‐ and satellite‐like Ag‐Fe@Fe3O4 heterostructures, which as a galvanic couple can reduce the cytotoxicity of Ag while maintaining controlled magnetic and optical properties.

Published
2018

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