Results 41 to 50 of about 48,430 (295)

Design, Synthesis, Pharmacodynamic and In Silico Pharmacokinetic Evaluation of Some Novel Biginelli-Derived Pyrimidines and Fused Pyrimidines as Calcium Channel Blockers

Molecules, 2022
Some new pyrimidine derivatives comprising arylsulfonylhydrazino, ethoxycarbonylhydrazino, thiocarbamoylhydrazino and substituted hydrazone and thiosemicarbazide functionalities were prepared from Biginelli-derived pyrimidine precursors.
Ahmed M. Farghaly, Ola H. Rizk, Inas Darwish, Manal Hamza, Mezna Saleh Altowyan, Assem Barakat, Mohamed Teleb   +6 more
doaj   +1 more source

Characterization of Amide Bond Conformers for a Novel Heterocyclic Template of N-acylhydrazone Derivatives

Molecules, 2013
Herein we describe NMR experiments and structural modifications of 4-methyl-2-phenylpyrimidine-N-acylhydrazone compounds (aryl-NAH) in order to discover if duplication of some signals in their 1H- and 13C-NMR spectra was related to a mixture of imine ...
Alexandra Basilio Lopes, Eduardo Miguez, Arthur Eugen Kümmerle, Victor Marcos Rumjanek, Carlos Alberto Manssour Fraga, Eliezer J. Barreiro   +5 more
doaj   +1 more source

Development of Piperazine- and Oxazine-Linked Pyrimidines as p65 Subunit Binders of NF–κB in Human Breast Cancer Cells

Biomedicines, 2023
Nuclear factor kappa B (NF–κB) is a potential therapeutic target in breast cancer. In the current study, a new class of oxazine– and piperazine–linked pyrimidines was developed as inhibitors of NF–κB, overcoming the complexity of the oxazine structure ...
Akshay Ravish, Bhanuprakash C. Narasimhachar, Zhang Xi, Divakar Vishwanath, Arunkumar Mohan, Santosh L. Gaonkar, Paduvalahippe Gowdegowda Chandrashekara, Kwang Seok Ahn, Vijay Pandey, Peter E. Lobie, Basappa Basappa   +10 more
doaj   +1 more source

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

Molecular 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, Christopher Dirks, Caroline Eiden, Sonja K. Fesenmayer, Femke M. Hormann, Yolande Klootsema, Ingrid Lilienthal, Si Min Zhang, Nikolas Herold, Sean G. Rudd   +9 more
wiley   +1 more source

Preparation and Diagnosis of Pyrimidines Derivatives by Conventional And Microwave Ways. [PDF]

مجلة جامعة الانبار للعلوم الصرفة, 2017
This work includes synthesis and characterization of new derivatives of pyrimidine (R. or Ar. -1, 2, 3, 4-tetrahydropyrimidin-5-yl) ethan-1-one), via the reaction of acetyl acetone with different aldehydes and guanidine hydrochloride.
Waleed F. AL-Hiti, Samea J. Khammase, Bushra T. Mahdi   +2 more
doaj   +1 more source

Refinement of amino‐acid conformation vs. difference density maps in time‐resolved serial femtosecond crystallography data analysis

FEBS Open Bio, EarlyView.
The dFoCC pipeline starts with observed DED and resting‐state coordinates, which are then used to generate a library of triggered states. Correlation analysis of the calculated DED features of each candidate vs observed DED permits quantitative evaluation of candidate structural quality.
Meng Iao Fong, Yuhei Hosokawa, Lars Oliver Essen, Manuel Maestre‐Reyna   +3 more
wiley   +1 more source

Hybrid Molecules with Purine and Pyrimidine Derivatives for Antitumor Therapy: News, Perspectives, and Future Directions

Molecules
Cancer is a leading cause of death globally, claiming millions of lives each year. Despite the availability of numerous anticancer drugs, the need for new treatment options remains essential. Many current therapies come with significant toxicity, lead to
Simona Iacob (Ciobotaru), Claudia-Simona Stefan, Aurel Nechita, Madalina-Nicoleta Matei, Elena-Lacramioara Lisa, Dana Tutunaru, Iuliu Fulga, Ana Fulga, Alina-Georgiana Cristea (Hohota), Oana-Maria Dragostin   +9 more
doaj   +1 more source

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

Pharmaceuticals, 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, Samiha A. El-Sebaey, Sherin M. Elfeky, Hanan A. AL-Ghulikah, Mona S. El-Zoghbi   +4 more
doaj   +1 more source

Time‐restricted feeding prior to Mycobacterium tuberculosis infection reduces tissue CD4+ T cells with limited impact on bacterial clearance

FEBS Open Bio, EarlyView.
Time‐restricted feeding (TRF) in mice increased liver fatty acid oxidation and decreased fatty acid biosynthesis. These alterations persisted when TRF was discontinued and the host was infected with Mycobacterium tuberculosis. Pre‐exposure to TRF did not alter tissue (lung and spleen) mycobacterial burden but significantly reduced CD3+ T cells in lungs
Ashish Gupta, Nidhi Yadav, Subhasmita Das, R. Rajendra Kumar Reddy, Nupur Sharma, Amol Ratnakar Suryawanshi, Jaswinder Singh Maras, Ranjan Kumar Nanda   +7 more
wiley   +1 more source

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

Molecules, 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