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The effect of diphenylethane side-chain substituents on dibenzocyclohexadiene formation and their inhibition of α-synuclein aggregation in vitro

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 78 ()

The naturally-occurring di-catechol lignan nordihydroguaiaretic acid (NDGA) and an analog without methyl groups on the butyl linker both undergo intra......

Discovery and structure-activity relationship study of 2-piperazinyl-benzo- thiazole derivatives as potent and selective PPARδ agonists

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 82 ()

Peroxisome proliferator-activated receptor d (PPARd) is considered to be a target for treating metabolic syndrome, whereas there is no PPARd agonist i......

2-Substituted 1,5-benzothiazepine-based HDAC inhibitors exert anticancer activities on human solid and acute myeloid leukemia cell lines

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 93 ()

Herein, we report the development of a new series of histone deacetylase inhibitors (HDACi) containing a 2-substituted 1,5-benzothiazepine scaffold. F......

Discovery of a potent, orally available tricyclic derivative as a novel BRD4 inhibitor for melanoma

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 93 ()

The epigenetic regulation of the protein bromodomain-containing protein 4 (BRD4) has emerged as a compelling target for cancer treatment. In this stud......

Structure-based lead optimization to improve potency and selectivity of a novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid series of heparanase-1 inhibitor

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 93 ()

Heparanase-1 (HPSE1) is an endo-& beta;-D-glucuronidase that is the only mammalian enzyme known to cleave heparan sulfate (HS) of heparan sulfate ......

Development of decoy oligonucleotide-warheaded chimeric molecules targeting STAT3

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 95 ()

Proteolysis-targeting chimera (PROTAC) technology is a disruptive innovation in the drug development community, and over 20 PROTAC molecules are curre......

Harnessing polyhydroxylated pyrrolidines as a stabilizer of acid alpha-glucosidase (GAA) to enhance the efficacy of enzyme replacement therapy in Pompe disease

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 78 ()

To discover small molecules as acid alpha-glucosidase (GAA) stabilizers for potential benefits of the exogenous enzyme treatment toward Pompe disease ......

Synthesis of a photocleavable bola-phosphatidylcholine

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 93 ()

Phosphatidylinositol transfer proteins (PITPs) are ubiquitous in eukaryotes and are involved in the regulation of phospholipid metabolism, membrane tr......

Synthesis and biophysical properties of tetravalent PEG-conjugated antisense oligonucleotide

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 78 ()

This study was aimed at developing a novel platform for tetravalent conjugation of 4-arm polyethylene glycol (PEG) with an antisense oligonucleotide (......

Pyrrolidinedione-thiazolidinone hybrid molecules with potent cytotoxic effect in squamous cell carcinoma SCC-15 cells

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 92 ()

The hybrid heterocyclic molecules are perspective materials in the development of anticancer drugs. Here, the pyrrolidinedione-thiazolidinone hybrid m......

Synthesis, anti-inflammatory activity, inverse molecular docking, and acid dissociation constants of new naphthoquinone-thiazole hybrids

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 95 ()

Chronic Inflammation is associated with various types of diseases that involves pro-inflammatory cytokines like IL-6 and TNF-alpha. High costs and ser......

Influence of N-arylsulfonamido D-valine N-substituents on the selectivity and potency of matrix metalloproteinase inhibitors

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 90 ()

To develop matrix metalloproteinase inhibitors (MMPIs) for both therapy and medicinal imaging by fluorescence-based techniques or positron-emission to......

Synthesis of novobiocin derivatives and evaluation of their antigonococcal activity and pharmacokinetics

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 92 ()

Gonorrhea has become a serious problem because the number of infected people is increasing and the multi-drug resistance of the causative bacteria, Ne......

Selective modifications of lactose and N-acetyllactosamine with sulfate and aromatic bulky groups unveil unique structural insights in galectin-1-ligand recognition

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 94 ()

Galectins, a family of endogenous glycan-binding proteins, play crucial roles in a broad range of physiological and pathological processes. Galectin-1......

Synthesis and Staphylococcus aureus biofilm inhibitory activity of indolenine-substituted pyrazole and pyrimido[1,2-b]indazole derivatives

期刊: BIOORGANIC & MEDICINAL CHEMISTRY, 2023; 95 ()

Staphylococcus aureus is a highly adaptable opportunistic pathogen that can form biofilms and generate persister cells, leading to life-threatening in......

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