Results 61 to 70 of about 319,341 (367)

Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

Molecules, 2020
A series of 34 new pyrimido[2,1-c][1,2,4]triazine-3,4-diones were synthesized and fully characterized using IR, NMR, MS, and microanalytical analysis. In vitro investigation of 12 compounds of this series revealed promising antimicrobial activity of the ...
Islam H. El Azab, Nadia A.A. Elkanzi
doaj   +1 more source

Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors

Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
A new series of 5-trifluoromethylpyrimidine derivatives were designed and synthesised as EGFR inhibitors. Three tumour cells A549, MCF-7, PC-3 and EGFR kinase were employed to evaluate their biological activities.
Yaqing Zuo, Rongrong Li, Yan Zhang, Guochen Bao, Yi Le, Longjia Yan   +5 more
doaj   +1 more source

Tertiary alkylamines as nucleophiles in substitution reactions at heteroaromatic halide during the synthesis of the highly potent pirinixic acid derivative 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid (YS-121) [PDF]

, 2011
YS-121 [2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid] is the result of target-oriented structural derivatization of pirinixic acid.
Gabler, Matthias, Schubert-Zsilavecz, Manfred   +1 more
core   +2 more sources

CPS1 maintains pyrimidine pools and DNA synthesis in KRAS/LKB1-mutant lung cancer cells

Nature, 2017
Metabolic reprogramming by oncogenic signals promotes cancer initiation and progression. The oncogene KRAS and tumour suppressor STK11, which encodes the kinase LKB1, regulate metabolism and are frequently mutated in non-small-cell lung cancer (NSCLC ...
Jiyeon Kim, Zeping Hu, L. Cai, Kailong Li, Eunhee Choi, B. Faubert, Divya Bezwada, J. Rodriguez-Canales, P. Villalobos, Yu-Fen Lin, Min Ni, K. Huffman, L. Girard, L. Byers, K. Unsal-Kaçmaz, C. G. Peña, J. Heymach, E. Wauters, J. Vansteenkiste, D. Castrillon, Benjamin P. C. Chen, I. Wistuba, D. Lambrechts, Jian Xu, J. Minna, R. Deberardinis   +25 more
semanticscholar   +1 more source

Multiple ETS family transcription factors bind mutant p53 via distinct interaction regions

FEBS Letters, EarlyView.
Mutant p53 gain‐of‐function is thought to be mediated by interaction with other transcription factors. We identify multiple ETS transcription factors that can bind mutant p53 and found that this interaction can be promoted by a PXXPP motif. ETS proteins that strongly bound mutant p53 were upregulated in ovarian cancer compared to ETS proteins that ...
Stephanie A. Metcalf, Nicholas F. Downing, Kaitlyn M. Mills, Samuel C. Metcalfe, Alexander E. Kritzer, Lindsey D. Mayo, Peter C. Hollenhorst   +6 more
wiley   +1 more source

Novel Selective and Potent EGFR Inhibitor that Overcomes T790M-Mediated Resistance in Non-Small Cell Lung Cancer

Molecules, 2016
Treating patients suffering from EGFR mutant non-small cell lung cancer (NSCLC) with first-generation EGFR tyrosine kinase inhibitors (EGFR TKI) provides excellent response rates.
Yanxia Li, Zhendong Song, Yue Jin, Zeyao Tang, Jian Kang, Xiaodong Ma   +5 more
doaj   +1 more source

Mechanisms of base selection by human single-stranded selective monofunctional uracil-DNA glycosylase [PDF]

, 2009
hSMUG1 (human single-stranded selective monofunctional uracil-DNA glyscosylase) is one of three glycosylases encoded within a small region of human chromosome 12. Those three glycosylases, UNG (uracil-DNA glycosylase), TDG (thymine-DNA glyscosylase), and
Agus Darwanto, Akbari, Alcantara, Barrett, Bennett, Bethod, Boorstein, Bryantsev, Cerny, Clough, Cui, Cybulski, Daniel K. Rogstad, Di Noia, Di Noia, Dunning, Fujimoto, Gait, Guerniou, Hansch, Haushalter, Hobza, Jacob A. Theruvathu, James L. Sowers, Jang, Kavli, Kelly, Kendall, Krokan, Krokan, La Francois, Lawrence C. Sowers, Liu, Marten, Masaoka, Matsubara, Matsubara, Matsudaira, Mendes, Morgan, Neddermann, Nilsen, Nilsen, Pearl, Perezjorda, Privat, Rao, Rogstad, SantaLucia, Sibghat-Ullah, Slupphaug, Sousa, Sowers, Sowers, Sugiyama, Tannor, Tod Pascal, Waters, Wibley, William Goddard, Zhao, Zhao, Zhao, Zielenkiewicz   +63 more
core   +3 more sources

Patient‐specific pharmacogenomics demonstrates xCT as predictive therapeutic target in colon cancer with possible implications in tumor connectivity

Molecular Oncology, EarlyView.
This study integrates transcriptomic profiling of matched tumor and healthy tissues from 32 colorectal cancer patients with functional validation in patient‐derived organoids, revealing dysregulated metabolic programs driven by overexpressed xCT (SLC7A11) and SLC3A2, identifying an oncogenic cystine/glutamate transporter signature linked to ...
Marco Strecker, Keren Zohar, Martin Böttcher, Thomas Wartmann, Henry Freudenstein, Maximilian Doelling, Mihailo Andric, Wenjie Shi, Or Kakhlon, Katrin Hippe, Beatrix Jahnke, Dimitrios Mougiakakos, Franziska Baenke, Daniel Stange, Roland S. Croner, Michal Linial, Ulf D. Kahlert   +16 more
wiley   +1 more source

1-Methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine

IUCrData, 2017
In the crystal, molecules of the title compound, C12H10N4, stack in a head-to-tail manner along the b direction through π–π stacking interactions between both portions of the pyrazolopyrimidine ring system.
Mohamed El Hafi, Mohammed Boulhaoua, Abdelhanine Essaghouani, Youssef Ramli, El Mokhtar Essassi, Joel T. Mague   +5 more
doaj   +1 more source

Chemical investigation of light induced DNA bipyrimidine damage and repair [PDF]

, 2011
In all organisms, genetic information is stored in DNA and RNA. Both of these macromolecules are damaged by many exogenous and endogenous events, with UV irradiation being one of the major sources of damage.
Carell, Thomas, Heil, Korbinian, Pearson, David   +2 more
core   +1 more source