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Identification of potential RapJ hits as sporulation pathway inducer candidates in Bacillus coagulans via structure-based virtual screening and molecular dynamics simulation studies.
J Mol Model
July 2023
Department of Pharmaceutical Biotechnology, School of Pharmacy, Shiraz University of Medical Sciences, Shiraz, Iran.
Background: The bacterium Bacillus coagulans has attracted interest because of its ability to produce spores and advantageous probiotic traits, such as facilitating food digestion in the intestine, managing some disorders, and controlling the symbiotic microbiota. Spore-forming probiotic bacteria are especially important in the probiotic industry compared to non-spore-forming bacteria due to their stability during production and high resistance to adverse factors such as stomach acid. When spore-forming bacteria are exposed to environmental stresses, they enter the sporulation pathway to survive.
View Article and Find Full Text PDFEsterase-responsive and size-optimized prodrug nanoparticles for effective intracranial drug delivery and glioblastoma treatment.
Nanomedicine
August 2022
Department of Neurosurgery, Renmin Hospital of Wuhan University, Wuhan, Hubei 430060, China; Central Laboratory, Renmin Hospital of Wuhan University, Wuhan, Hubei 430060, China. Electronic address:
Glioblastoma multiforme (GBM) is the intracranial malignancy with the highest rates of morbidity and mortality. Chemotherapy is often ineffective against GBM due to the presence of the blood-brain barrier (BBB); however, the application of nanotechnology is expected to overcome this limitation. Poly(lactic-co-glycolic acid) (PLGA) is a degradable and nontoxic functional polymer with good biocompatibility that is widely used in the pharmaceutical industry.
View Article and Find Full Text PDFIdentification and characterization of , , and reactive metabolites of tandutinib using liquid chromatography ion trap mass spectrometry.
Anal Methods
January 2021
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh, 11451, Saudi Arabia.
Tandutinib (TND) is a novel, oral small molecule designed for treating acute myeloid leukemia (AML) by inhibiting type III receptor tyrosine kinases. This study reports the use of in silico, in vivo, and in vitro methods to investigate the metabolism and possible metabolic bioactivation of TND. First, in silico metabolism of TND was assessed using the WhichP450™ module of the StarDrop® software to determine labile sites of metabolism in the TND chemical structure.
View Article and Find Full Text PDFDiscovery of 4-piperazinyl-2-aminopyrimidine derivatives as dual inhibitors of JAK2 and FLT3.
Eur J Med Chem
November 2019
Key Laboratory of Structure-Based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang, 110016, PR China. Electronic address:
Article Synopsis
- The study explores a hybridization strategy for developing multi-target inhibitors in drug design, focusing on combining the pharmacophores of momelotinib and tandutinib.
- A series of derivatives were created and tested for their ability to inhibit JAK2 and FLT3 enzymes, with several compounds also evaluated for their effectiveness against specific cancer cell lines.
- Compound 14j emerged as the most potent dual inhibitor, effectively inducing apoptosis and halting the cell cycle in the G/S phase, demonstrating strong potential in cancer treatment.
Synthesis of Novel Thieno[2,3-d]pyrimidine Derivatives and Evaluation of Their Cytotoxicity and EGFR Inhibitory Activity.
Anticancer Agents Med Chem
June 2019
Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
Background: 4-Substitutedaminoquinazoline scaffolds were reported to possess potent cytotoxic and EGFR inhibitory activity such as gefitinib (Iressa), erlotinib (Tarceva) and tandutinib.
Objective: Synthesis of novel 4-substitutedaminothieno[2,3-d]pyrimidine derivatives as bioisosters of 4-substitutedaminoquinazoline derivatives with potential cytotoxic and EGFR inhibitory activity.
Methods: Novel 4-substitutedaminothieno[2,3-d]pyrimidine derivatives 4a-i and 5a-c were synthesized via reacting corresponding 4-chlorothieno[2,3-d]pyrimidine derivatives 3a-c with N-methylpiperazine, morpholine, N-phenylpiperazine or 1,3-propanediamine.
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