Synthesis, Antitumor Activity, and In Silico Drug Design of New Thieno[2,3‑d]Pyrimidine-4-One Derivatives as Nonclassical Lipophilic Dihydrofolate Reductase Inhibitors

Autor: Ola A. Abdelaziz, Walaa M. El Husseiny, Khalid B. Selim, Hassan M. Eisa

Publikováno v: ACS Omega, Vol 7, Iss 49, Pp 45455-45468 (2022)

Externí odkaz: https://doaj.org/article/1f0ac9d7bf7941d4a51722cc044494e9

Synthesis, antitumour and antioxidant activities of novel α,β-unsaturated ketones and related heterocyclic analogues: EGFR inhibition and molecular modelling study

Autor: Walaa M. El-Husseiny, Magda A.-A. El-Sayed, Naglaa I. Abdel-Aziz, Adel S. El-Azab, Esam R. Ahmed, Alaa A.-M. Abdel-Aziz

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 33, Iss 1, Pp 507-518 (2018)

New α,β-unsaturated ketones 4a,b; 5a–c; and 6a,b; as well as 4-H pyran 7; pyrazoline 8a,b; isoxazoline 9; pyridine 10–11; and quinoline-4-carboxylic acid 12a,b derivatives were synthesized and evaluated for in vitro antitumour activity against

Externí odkaz: https://doaj.org/article/ffe7cb284bb742a5b8b4fb2fc4452d4a

Synthesis, antitumor activity, and molecular docking study of 2-cyclopentyloxyanisole derivatives: mechanistic study of enzyme inhibition

Autor: Mohammed M. Alanazi, Walaa M. El-Husseiny, Adel S. El-Azab, Alaa A.-M. Abdel-Aziz, Magda A.-A. El-Sayed, Nawaf A. Alsaif

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 35, Iss 1, Pp 744-758 (2020)

A series of 24 compounds was synthesised based on a 2-cyclopentyloxyanisole scaffold 3–14 and their in vitro antitumor activity was evaluated. Compounds 4a, 4b, 6b, 7b, 13, and 14 had the most potent antitumor activity (IC50 range: 5.13–17.95 μM

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0dfea8980554abbcef0e19e47a894df
http://europepmc.org/articles/PMC7144195

Synthesis and biological evaluation of 2-styrylquinolines as antitumour agents and EGFR kinase inhibitors: molecular docking study

Autor: Naglaa I. Abdel-Aziz, Alaa A.-M. Abdel-Aziz, Hatem A. Abuelizz, Magda A.-A. El-Sayed, Walaa M. El-Husseiny, Adel S. El-Azab

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 33, Iss 1, Pp 199-209 (2018)
Journal of Enzyme Inhibition and Medicinal Chemistry

A new series of 4,6-disubstituted 2-(4-(dimethylamino)styryl)quinoline 4a,b–9a,b was synthesized by the reaction of 2-(4-(dimethylamino)styryl)-6-substituted quinoline-4-carboxylic acids 3a,b with thiosemicarbazide, p-hydroxybenzaldehyde, ethylcyan

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c2fb686749f09762b1a48dcc7af2af3
https://doaj.org/article/c21610cab0e24712bbdc93c22001da4c

Synthesis, antitumour activities and molecular docking of thiocarboxylic acid ester-based NSAID scaffolds: COX-2 inhibition and mechanistic studies

Autor: Laila A. Abou-Zeid, Magda A.-A. El-Sayed, Adel S. El-Azab, Alaa A.-M. Abdel-Aziz, Walaa M. El-Husseiny, Ahmad M. El_Morsy, Manal A. El-Gendy

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 33, Iss 1, Pp 989-998 (2018)

A new series of NSAID thioesters were synthesized and evaluated for their in vitro antitumor effects against a panel of four human tumor cell lines, namely: HepG2, MCF-7, HCT-116 and Caco-2, using the MTT assay. Compared to the reference drugs 5-FU,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f363bef692bf5f37d77a2d28dbe78850
https://pubmed.ncbi.nlm.nih.gov/29806488