Two 4-imidazolylflavans were synthesized and their relative stereochemistry was established by 1H and 13C NMR data. These compounds were tested for their activity to inhibit aromatase. It was observed that the introduction of an imidazolyl group at carbon 4 on flavan nucleus led to potent molecules.
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http://dx.doi.org/10.1016/s0960-894x(02)00565-6 | DOI Listing |
JBI Evid Synth
January 2025
School of Nursing and Midwifery, University of Newcastle, Newcastle, New South Wales, Australia.
Objective: The objective of this review was to synthesize the available evidence on the experiences of African women who migrated to a developed country and encountered intimate partner violence (IPV).
Introduction: IPV is a significant public health issue, and migrant women living in developed countries are particularly vulnerable to IPV, experiencing disproportionately higher rates of IPV. Understanding the experiences of these women can inform health policy and decision-making in clinical practice to minimize IPV.
Acta Pharm Sin B
December 2024
Key Laboratory of Drug Metabolism and Pharmacokinetics, Research Unit of PK-PD Based Bioactive Components and Pharmacodynamic Target Discovery of Natural Medicine of Chinese Academy of Medical Sciences, China Pharmaceutical University, Nanjing 210009, China.
Hydrogen sulfide (HS) is a gas signaling molecule with versatile bioactivities; however, its exploitation for disease treatment appears challenging. This study describes the design and characterization of a novel type of HS donor-drug conjugate (DDC) based on the thio-ProTide scaffold, an evolution of the ProTide strategy successfully used in drug discovery. The new HS DDCs achieved hepatic co-delivery of HS and an anti-fibrotic drug candidate named hydronidone, which synergistically attenuated liver injury and resulted in more sufficient intracellular drug exposure.
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December 2024
School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou 310024, China.
The fat mass and obesity-associated protein (FTO) is an RNA demethylase required for catalytic demethylation of -methyladenosine (mA); it is highly expressed and functions as an oncogene in acute myeloid leukemia (AML). Currently, the overarching objective of targeting FTO is to precisely inhibit the catalytic activity. Meanwhile, whether FTO degradation also exerts antileukemic effects remains unknown.
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January 2025
Department of Chemistry, Faculty of Science, University of Maragheh P.O Box 55181-83111 Maragheh Iran.
In this study, we present the design, synthesis, and utilization of a covalent triazine framework (CTF) formed by the condensation of , , -tris(4-(aminomethyl)benzyl)-1,3,5-triazine-2,4,6-triamine and 2,4,6-tris(4-formylphenoxy)-1,3,5-triazine on which silica is immobilized (TPT-TAT/silica) as an innovative catalyst for porphyrins synthesis. Under solvothermal conditions, the condensation of triamine and trialdehyde precursors led to the formation of a covalent triazine framework (CTF) with a high nitrogen content. The resulting CTF is characterized by its extensive porosity and elevated nitrogen levels, which are critical for the creation of catalytic active sites.
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January 2025
Department of Therapeutic Chemistry, Pharmaceutical and Drug Industries Research Institute, National Research Centre Dokki Giza 12622 Egypt
A novel molecular design based on a quinazolinone scaffold was developed the attachment of aryl alkanesulfonates to the quinazolinone core through a thioacetohydrazide azomethine linker, leading to a new series of quinazolinone-alkanesulfonates 5a-r. The antimicrobial properties of the newly synthesized quinazolinone derivatives 5a-r were investigated to examine their bactericidal and fungicidal activities against bacterial pathogens like , (Gram-positive), , , (Gram-negative), in addition to (unicellular fungal). The tested compounds demonstrated reasonable bactericidal activities compared to standard drugs.
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