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Design, synthesis, molecular docking, and biological activity of pyrazolo[3,4-b]pyridines as promising lead candidates against Mycobacterium tuberculosis
Pyrazolo[3,4-b]pyridine is a medicinally privileged structure. We have achieved a new and facile synthesis of a combinator...
Medicinal Chemistry Research
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A concise review on anti-breast cancer effectiveness of s-triazines through EGFR kinase inhibition
Today, one of the most common malignancies in women is breast cancer. Despite the large number of commercially available a...
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Unveiling the potential of prodrug and drug-conjugate strategies in treatment of diabetes mellitus and its complications
The 2021 statistics from the International Diabetes Federation reveals that approximately 537 million adults between the a...
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Synthesis of adamantane-monoterpene conjugates with 1,3,4-thiadiazol-2(3H)-imine linker and evaluation of their inhibitory activity against TDP1
Tyrosyl-DNA phosphodiesterase 1 (TDP1) is a DNA repair enzyme that can reduce the efficacy of some anticancer drugs target...
Medicinal Chemistry Research
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Self-assembled amphiphilic bipyridine and bisquinoline cisplatin analogues: synthesis and anticancer properties
We report the synthesis and characterisation of two amphiphilic cisplatin analogues derived from bipyridine and bisquinoli...
Medicinal Chemistry Research
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Increased rigidity and bioisosteric replacement in the design, synthesis and preliminary evaluation of novel, functionalized 3,3-dialkyl-γ-butyrolactones as sigma-2 ligands
The sigma-2 (σ2) receptor has been linked to several diseases and conditions including cancer, neuropathic drug addic...
Medicinal Chemistry Research
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Identification of α-mangostin as a potent inhibitor of β-lactamase OXA-48
The production of carbapenemases is a significant mechanism contributing to carbapenem resistance in Enterobacteriaceae. A...
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Synthesis and pharmacological evaluation of novel coumarin based triazolyl glycoconjugates as potential antibacterial and anti-proliferative agents
A library of novel coumarin-based triazolyl glycoconjugates is prepared and screened for in vitro antibacterial activity a...
Medicinal Chemistry Research
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Rehmannia glutinosa polysaccharides: a review on structure-activity relationship and biological activity
Rehmannia glutinosa has been used historically and is now listed in the 2020 Chinese Pharmacopoeia as a traditional Chines...
Medicinal Chemistry Research
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Bioactivities and the structural modification of Parthenolide: a review
Parthenolide, a sesquiterpene lactone derived from Feverfew (Tanacetum parthenium) buds, has attracted significant attenti...
Medicinal Chemistry Research
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Research progress on the mechanism of anti-myocardial infarction effect and clinical application of effective components of Salvia miltiorrhiza
Salvia miltiorrhiza, a plant in the Labiatae family, is a traditional Chinese herb. The small molecular components in S. m...
Medicinal Chemistry Research
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Indazole derivatives as selective inhibitors of butyrylcholinesterase with effective blood-brain-barrier permeability profile
Alzheimer’s disease (AD) is a chronic disease that is multifactorial. Its underlying cause and mechanisms are yet to...
Medicinal Chemistry Research
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Polyketides from Neohelicosporium griseum: structure assignment and bioactivity investigation
In the pursuit of discovering new active metabolites from helicosporous hyphomycetes, rice fermentation products of Neohel...
Medicinal Chemistry Research
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Exploring the latest breakthroughs in rhodesain inhibitors for African trypanosomiasis
Human African Trypanosomiasis is a serious public health concern, and new chemical therapeutic agents need to be developed...
Medicinal Chemistry Research
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Discovery of novel fatty acid amide hydrolase (FAAH) inhibitors as anti-Alzheimer’s agents through pharmacophore-based virtual screening, molecular docking and experimental validation
Alzheimer’s disease (AD) is the most prevalent form of neurodegenerative condition distinguished by the deposition o...
Medicinal Chemistry Research
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FTase inhibitors and cancer: prospects for use in targeted therapies
Farnesyltransferase (FTase) is a key enzyme that catalyzes the farnesylation of Ras protein. It is used to bind RAS protei...
Medicinal Chemistry Research
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Kaempferia diterpenoids and flavonoids: an overview on phytochemistry, biosynthesis, synthesis, pharmacology, and pharmacokinetics
Kaempferia species have contained various crucial ethnobotanical features, and are being used as traditional folk medicine...
Medicinal Chemistry Research
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One-pot synthesis and in vitro bioactivity of novel 4-aminopyrazolo[3,4-b]pyridine derivatives as potential antimicrobial compounds
The present paper describes an efficient synthesis of a series of 4-aminopyrazolo[3,4-b]pyridine derivatives 11a–i i...
Medicinal Chemistry Research
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Characterization of novel angiotensin-I converting enzyme inhibitory peptides derived from Taiwan red quinoa (Chenopodium formosanum Koidz.) seed proteins using two sequential bioassay-guided fractionations
Taiwan red quinoa (Chenopodium formosanum Koidz.) is a pseudo-cereal crop native to Taiwan with a rich protein content tha...
Medicinal Chemistry Research
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Enantioselectivity of pinene against Leishmania amazonensis
Pinene is a major monoterpene described in various plant essential oils. It has two isomers, α- and β-pinene, th...
Medicinal Chemistry Research
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Design and synthesis of novel cycloalkanecarboxamide parabanic acid hybrids as anticonvulsants
Aiming to develop novel anticonvulsant agents a new series of novel cycloalkanecarboxamide parabanic acid hybrids series 8...
Medicinal Chemistry Research
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Correction: Structural and stereochemical determinants for hGAT3 inhibition: development of novel conformationally constrained and substituted analogs of (S)-isoserine
Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which...
Medicinal Chemistry Research
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Screening of small molecule compounds targeting hnRNPA2 protein
Heterogeneous nuclear ribonucleoprotein A2, as an RNA binding protein, participates in the processing and metabolism of RN...
Medicinal Chemistry Research
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Discovery of potent maternal embryonic leucine zipper kinase (MELK) inhibitors of novel chemotypes using structure-based pharmacophores
Maternal embryonic leucine zipper kinase (MELK) is a serine-threonine kinase. Several studies have revealed its role as a ...
Medicinal Chemistry Research
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Design, synthesis, and in silico studies of novel di-(2-aryl hydrozonopropanal) arene derivatives as potent anticancer for targeting A2AR and LRP6 in HCT116 cell
Colorectal cancer (CRC) is a frequent malignancy with a poor prognosis and a high fatality rate, unlike other malignancies...
Medicinal Chemistry Research
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Design, synthesis and antimicrobial activities of 1,2,3-triazole hybrids with amine-ester functionality
Due to the notable therapeutic importance of 1,4-disubstituted-1,2,3-triazoles linked with amine and ester groups, a serie...
Medicinal Chemistry Research
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Novel aloe emodin–hydroxyethyl piperazine hybrid dihydrochloride induces oral cancer CAL-27 cells apoptosis through ROS production, DNA damage and mitochondrial pathways
Oral cancer severely affects the quality of life of patients, and the primary treatment is surgery, due to a lack of speci...
Medicinal Chemistry Research
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Synthesis of 6,6-Dimethyl-3-azabicyclo [3.1.0]hexane via Ru (II)-catalyzed intramolecular cyclopropanation
6,6-Dimethyl-3-azabicyclo[3.1.0]hexane (6,6-DMABH) is a crucial component in several antiviral medications, such as bocepr...
Medicinal Chemistry Research
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The trimethoxyphenyl (TMP) functional group: a versatile pharmacophore
The Trimethoxyphenyl (TMP) group serves as a pharmacophore in numerous potent agents exhibiting diverse bioactivity effect...
Medicinal Chemistry Research
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1,2,3-triazole derivatives as antiviral agents
In the last years, the emergence and spread of viral infections have been described with increased frequency and becomes a...
Medicinal Chemistry Research
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