Fragment Hopping-Based Design of Novel Biphenyl-DAPY Derivatives as Potent Non-Nucleoside Reverse Transcriptase Inhibitors Featuring Significantly Improved Anti-Resistance Efficacy

Article Chemistry, Medicinal

Design and Synthesis of Novel HIV-1 NNRTIs with Bicyclic Cores and with Improved Physicochemical Properties

Ladislav Prener et al.

Summary: Novel bicyclic NNRTIs with improved solubility and high antiviral activity against HIV-1 were designed and prepared. The binding modes of these compounds to reverse transcriptase were also studied by X-ray crystallography.

JOURNAL OF MEDICINAL CHEMISTRY (2023)

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Article Biology

ZBTB18 inhibits SREBP-dependent lipid synthesis by halting CTBPs and LSD1 activity in glioblastoma

Roberto Ferrarese et al.

Summary: Enhanced fatty acid synthesis is a prominent feature of glioblastoma. This study reveals a novel interaction between the co-activator/co-repressor CTBP and the tumor suppressor ZBTB18, which regulates the expression of SREBP genes. The researchers also identify CTBP1/2 and LSD1 as co-activators of SREBP genes and show that the functional activity of the CTBP-LSD1 complex is altered by ZBTB18. This study sheds light on a new epigenetic mechanism involved in fatty acid synthesis and its potential as a target for glioblastoma treatment.

LIFE SCIENCE ALLIANCE (2022)

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Article Chemistry, Multidisciplinary

Palladium-catalyzed sulfonylative coupling of benzyl(allyl) carbonates with arylsulfonyl hydrazides

Bozhen Gong et al.

Summary: An efficient palladium-catalyzed sulfonylative coupling reaction has been developed for the synthesis of benzyl(allyl) sulfones from sulfonyl hydrazides and carbonates. The methodology utilizes easily accessible chemical feedstocks and enables the synthesis of various benzyl(allyl) sulfones under mild conditions without the need for additional base catalyst.

GREEN SYNTHESIS AND CATALYSIS (2022)

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Review Biochemistry & Molecular Biology

Trends and strategies to combat viral infections: A review on FDA approved antiviral drugs

Dharma Rao Tompa et al.

Summary: Infections caused by microscopic viruses can lead to chronic illnesses like HIV/AIDS, flu, etc. Developing new and superior antiviral drugs is crucial, but the drugs can be toxic to human cells and viruses can develop resistance. Combination drugs targeting viral replication are common, but innovative strategies are needed to combat emerging viruses like Ebola and coronaviruses.

INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES (2021)

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Article Chemistry, Medicinal

Lead Optimization: Synthesis and Biological Evaluation of PBT-1 Derivatives as Novel Antitumor Agents

Lan Xie et al.

Summary: Phenanthrene-based tylophorine-1 (PBT-1) and its derivatives showed significant antiproliferative activities in cellular assays, especially compounds with a 7-hydroxy group on the phenanthrene B-ring and a pendant piperidine E-ring. One compound, 9h, displayed over 4-fold higher potency against triple-negative breast cancer cells compared to estrogen-responsible breast cancer cells. The new active compounds induced cell cycle accumulation in the late S and G2/M phase, without affecting microtubule formation or cell morphology, indicating their potential as novel antitumor agents.

ACS MEDICINAL CHEMISTRY LETTERS (2021)

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Article Biochemistry & Molecular Biology

Chemical space exploration of novel naphthyl-carboxamide-diarylpyrimidine derivatives with potent anti-HIV-1 activity

Yali Sang et al.

Summary: Fifteen naphthyl-carboxamide-DAPYs were generated to explore chemical space in reverse transcriptase (RT) binding site via lead optimization strategy. They displayed high inhibitory activity against wildtype (WT) and rilpivirine-associated resistant mutant E138K viruses, with compound a1 showing exceptionally inhibitory effects. Molecular docking analysis elucidated the biological activity and offered a structural insight for follow-up research.

BIOORGANIC CHEMISTRY (2021)

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Review Pharmacology & Pharmacy