Qin, Xuemei Liu, Peng Li, Yihai Hu, Liming Liao, Yexin Cao, Tingting Yang, Lifang
Published in
Bioorganic & medicinal chemistry letters
Starting with our previously reported work, a novel series of 3,4-dihydro-2H-[1,4]oxazino[2,3-f]quinazolin-derivatives were designed, synthesized and evaluated as potent EGFR tyrosine kinase inhibitors. All of the compounds showed significant inhibitory activities against EGFRwt kinase (IC50 ≤ 937.7 nM). Among them, compound 7j demonstrated the mos...
Kakarala, Kavita Kumari Jamil, Kaiser
Published in
Journal of biomolecular structure & dynamics
EGFR1, VEGFR2, Bcr-Abl and Src kinases are key drug targets in non-small cell lung cancer (NSCLC), bladder cancer, pancreatic cancer, CML, ALL, colorectal cancer, etc. The available drugs targeting these kinases have limited therapeutic efficacy due to novel mutations resulting in drug resistance and toxicity, as they target ATP binding site. Allos...
Moreno, Daniel Antunes Becker, Aline Paixão Scapulatempo-Neto, Cristovam Menezes, Weder Sheren, Jamie Walter, Aline M Clara, Carlos Machado, Hélio R Oliveira, Ricardo S Neder, Luciano
...
Published in
Molecular biology reports
Pilocytic astrocytoma is the most frequent pediatric glioma. Despite its overall good prognosis, complete surgical resection is sometimes unfeasible, especially for patients with deep-seated tumors. For these patients, the identification of targetable genetic alterations such as NTRK fusions, raised as a new hope for therapy. The presence of gene f...
M. Samir, E. M. Mohareb, R.
ABSTRACT. The multi-component reaction of ethyl acetoacetate with each of malononitrile (3) benzaldehyde (1) in ethanol containing triethylamine gave the ethyl 6-amino-5-cyano-2-methyl-4-phenyl-4H-pyran-3-carboxylate (4). The latter compound reacted with hydrazine hydrate to give the hydrazide derivative 6. Compound 6 underwent a series of hetero-c...
García-Alonso, Sara Romero-Pérez, Inés Gandullo-Sánchez, Lucía Chinchilla, Luis Ocaña, Alberto Montero, Juan Carlos Pandiella, Atanasio
Published in
Journal of Experimental & Clinical Cancer Research
BackgroundTreatment of renal cancer has significantly improved with the arrival to the clinic of kinase inhibitors and immunotherapies. However, the disease is still incurable in advanced stages. The fact that several approved inhibitors for kidney cancer target receptor tyrosine kinases (RTKs) suggests that these proteins play a critical role in t...
Rousselot, Philippe Mollica, Luigina Guilhot, Joelle Guerci, Agnes Nicolini, Franck-Emmanuel Etienne, Gabriel Legros, Laurence Charbonnier, Aude Coiteux, Valerie Dartigeas, Caroline
...
Dasatinib is a second-generation BCR-ABL1 tyrosine kinase inhibitor approved for patients with chronic myeloid leukaemia (CML). Dasatinib 100 mg per day is associated with an increased risk of pleural effusion (PlEff). We randomly evaluated whether therapeutic drug monitoring (TDM) may reduce dasatinib-associated significant adverse events (AEs) by...
Mohamed, Esraa Ali Ismail, Nasser S. M. Hagras, Mohamed Refaat, Hanan
Published in
Future Journal of Pharmaceutical Sciences
BackgroundThe heterocyclic compounds particularly pyridine displayed clinical and biological implementation. Pyridine scaffolds have been detected in most relevant drug molecules that included pyridine provided a great possibility for treatment.Main textPyridine-containing compounds have increasing importance for medicinal application as antiviral,...
Ferrao Blanco, M. N. (author) Domenech Garcia, H. (author) Legeai-Mallet, L. (author) van Osch, G.J.V.M. (author)
Osteoarthritis (OA) is a major health problem worldwide that affects the joints and causes severe disability. It is characterized by pain and low-grade inflammation. However, the exact pathogenesis remains unknown and the therapeutic options are limited. In OA articular chondrocytes undergo a phenotypic transition becoming hypertrophic, which leads...
Bajinting, Adam Ng, Ho Leung
Published in
Advances in protein chemistry and structural biology
Receptor tyrosine kinases (RTKs) are important drug targets for cancer and immunological disorders. Crystal structures of individual RTK domains have contributed greatly to the structure-based drug design of clinically used drugs. Low-resolution structures from electron microscopy are now available for the RTKs, EGFR, PDGFR, and Kit. However, there...
Al-Yozbaki, Minnatallah Acha-Sagredo, Amelia George, Alex Liloglou, Triantafillos Wilson, Cornelia M
Published in
Biochimica et biophysica acta. Reviews on cancer
Neurotensin receptor-3 or sortilin is a vacuolar protein sorting 10 protein domain (Vps10p) has been firstly discovered in the human brain, it acts as receptor or co-receptor of the cell and traffics different proteins within the cell. Sortilin deregulation contributes to the development of several diseases, including neurological diseases and canc...