Results 41 to 50 of about 73,935 (281)

Novel Aminopyrimidine-2,4-diones, 2-Thiopyrimidine-4-ones, and 6-Arylpteridines as Dual-Target Inhibitors of BRD4/PLK1: Design, Synthesis, Cytotoxicity, and Computational Studies

open access: yesPharmaceuticals, 2023
Structural-based drug design and solvent-free synthesis were combined to obtain three novel series of 5-arylethylidene-aminopyrimidine-2,4-diones (4, 5a–c, 6a,b), 5-arylethylidene-amino-2-thiopyrimidine-4-ones (7,8), and 6-arylpteridines (9,10) as dual ...
Samar El-Kalyoubi   +4 more
doaj   +1 more source

IMPDH inhibition enhances cytarabine efficacy in SAMHD1‐expressing leukaemia cells via guanine nucleotide depletion

open access: yesMolecular Oncology, EarlyView.
Cytarabine is a key therapy for acute myeloid leukaemia (AML), but its efficacy is limited by the dNTPase SAMHD1, which hydrolyses its active metabolite. Screening nucleotide biosynthesis inhibitors revealed that IMPDH inhibitors selectively sensitise SAMHD1‐proficient AML cells to cytarabine.
Miriam Yagüe‐Capilla   +9 more
wiley   +1 more source

Modification of Purine and Pyrimidine Nucleosides by Direct C-H Bond Activation

open access: yesMolecules, 2015
Transition metal-catalyzed modifications of the activated heterocyclic bases of nucleosides as well as DNA or RNA fragments employing traditional cross-coupling methods have been well-established in nucleic acid chemistry.
Yong Liang, Stanislaw F. Wnuk
doaj   +1 more source

Unusual Nucleophilic Addition of Grignard Reagents in the Synthesis of 4-Amino-pyrimidines [PDF]

open access: yes, 2018
Pyrimidines have always received considerable attention because of their importance in synthesis and elucidation of biochemical roles, in particular that of vitamin B1.
Hughes, David L.   +3 more
core   +3 more sources

Dihydroorotate dehydrogenase (DHODH) regulates trophoblast syncytialization through organelle stress–induced cellular senescence

open access: yesFEBS Open Bio, EarlyView.
The inhibition of mitochondrial dihydroorotate dehydrogenase (DHODH) impairs syncytialization and induces cellular senescence via mitochondrial and endoplasmic reticulum stress in human trophoblast stem cells, elevating sFlt1/PlGF levels, a hallmark of placental dysfunction in hypertensive disorders of pregnancy.
Kanoko Yoshida   +6 more
wiley   +1 more source

Nitrogen doping of carbon nanoelectrodes for enhanced control of DNA translocation dynamics

open access: yes, 2017
Controlling the dynamics of DNA translocation is a central issue in the emerging nanopore-based DNA sequencing. To address the potential of heteroatom doping of carbon nanostructures to achieve this goal, herein we carry out atomistic molecular dynamics ...
Cho, Art E.   +3 more
core   +9 more sources

Aging Is a Key Driver for Adult Acute Myeloid Leukemia

open access: yesAging and Cancer, EarlyView.
Acute myeloid leukemia (AML) is a classical age‐related hematologic malignancy, and a key driver of AML is aging, which profoundly regulates intrinsic factors such as genomic instability, epigenetic reprogramming, and metabolic dysregulation, and alters bone marrow microenvironment.
Rong Yin, Haojian Zhang
wiley   +1 more source

CHEMICAL CONSTITUENTS DERIVED FROM THE CANARIES MARINE SPONGE Myxilla sp.

open access: yesQuímica Nova
Stigmasterols, ceramides, including ceramide-1-phosphates and pyrimidines were identified in an ethanol extract of the marine sponge Myxilla sp. The compounds were identified by MS and 1D- and 2D-NMR techniques.
Pere Ferriol Bunyola   +5 more
doaj   +1 more source

Design and Synthesis of New 4-(3,4,5-Trimethoxyphenyl)Thiazole–Pyrimidine Derivatives as Potential Antiproliferative Agents

open access: yesMedicina, 2023
A new series of 3,4,5-trimethoxyphenyl thiazole pyrimidines has been synthesized and biologically evaluated for its in vitro anticancer activity. Compounds 4a, 4b, and 4h with substituted piperazine showed the best antiproliferative activity.
Ashraf K. El-Damasy   +7 more
doaj   +1 more source

Recognition of abasic sites and single base bulges in DNA by a metalloinsertor [PDF]

open access: yes, 2009
Abasic sites and single base bulges are thermodynamically destabilizing DNA defects that can lead to cancerous transformations if left unrepaired by the cell.
Barton, Jacqueline K.   +2 more
core   +1 more source

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