[HTML][HTML] The bioactivity of thiazolidin-4-ones: A short review of the most recent studies

D Mech, A Kurowska, N Trotsko - International Journal of Molecular …, 2021 - mdpi.com
Thiazolidin-4-ones is an important heterocyclic ring system of a pharmacophore and a
privileged scaffold in medicinal chemistry. This review is focused on the latest scientific …

Thiazolidinone‐Heterocycle Frameworks: A Concise Review of Their Pharmacological Significance

P Seboletswe, N Cele, P Singh - ChemMedChem, 2023 - Wiley Online Library
Molecular hybridization is deemed an optimistic approach in drug design and the discovery
of novel biologically active molecules as it may advance their affinity and potency while …

[HTML][HTML] Design and synthesis of new thiazolidinone/uracil derivatives as antiproliferative agents targeting EGFR and/or BRAFV600E

MB Alshammari, AA Aly, BGM Youssif, S Bräse… - Frontiers in …, 2022 - frontiersin.org
Thiourea derivatives of uracil were efficiently synthesized via the reaction of 5-aminouracil
with isothiocyanates. Then, we prepared uracil-containing thiazoles via condensation of …

Triple targeting of mutant EGFRL858R/T790M, COX-2, and 15-LOX: design and synthesis of novel quinazolinone tethered phenyl urea derivatives for anti …

H Kothayer, S Rezq, AS Abdelkhalek… - Journal of Enzyme …, 2023 - Taylor & Francis
We designed and synthesised novel quinazolinone tethered phenyl urea derivatives (6a–p)
that triple target the double mutant EGFRL858R/T790M, COX-2, and 15-LOX. Compounds …

Design, synthesis and Molecular modeling study of certain EGFR inhibitors with a quinazolinone scaffold as anti-hepatocellular carcinoma and Radio-sensitizers

WM Ghorab, SA El-Sebaey, MM Ghorab - Bioorganic Chemistry, 2023 - Elsevier
A set of novel N-substituted-2-((4-oxo-3-phenyl-3, 4-dihydroquinazolin-2-yl) thio) acetamide
3–16 were designed and synthesized from 2-mercapto-3-phenylquinazolinone 2. The …

Synthesis and biological evaluation of 1-phenyl-tetrahydro-β-carboline-based first dual PRMT5/EGFR inhibitors as potential anticancer agents

J Zhang, X Liu, N Sa, JH Zhang, YS Cai… - European Journal of …, 2024 - Elsevier
Abstract Protein arginine methyltransferase 5 (PRMT5) and epidermal growth factor receptor
(EGFR) are both involved in the regulation of various cancer-related processes, and their …

Design, synthesis and biological evaluation of a series of dianilinopyrimidines as EGFR inhibitors

L Yan, Q Wang, L Liu, Y Le - Journal of Enzyme Inhibition and …, 2022 - Taylor & Francis
This paper described our efforts to develop dianilinopyrimidines as novel EGFR inhibitors.
All the target compounds were tested for inhibitory effects against wild type EGFR (EGFRwt) …

Development of new thieno [2, 3-d] pyrimidines as dual EGFR and STAT3 inhibitors endowed with anticancer and pro-apoptotic activities

HA Elsebaie, TF El-Moselhy, EA El-Bastawissy… - Bioorganic …, 2024 - Elsevier
In part due to the resilience of cellular feedback pathways that develop therapeutic
resistance to targeting the EGFR alone, using EGFR inhibitors alone was demonstrated to …

Discovery of new symmetrical and asymmetrical nitrile-containing 1, 4-dihydropyridine derivatives as dual kinases and P-glycoprotein inhibitors: synthesis, in vitro …

MH Saad, TF El-Moselhy, NS, El-Din… - Journal of Enzyme …, 2022 - Taylor & Francis
Two new series of symmetric (1a-h) and asymmetric (2a-l) 1, 4-DHP derivatives were
designed, synthesised, and evaluated as anticancer agents. In vitro anticancer screening of …

Rational design and eco-friendly one-pot multicomponent synthesis of novel ethylidenehydrazineylthiazol-4 (5H)-ones as potential apoptotic inducers targeting wild …

EM Abbass, AA Al-Karmalawy, M Sharaky… - Bioorganic …, 2024 - Elsevier
A novel series of ethylidenehydrazineylthiazol-4 (5H)-ones were synthesized using various
eco-friendly one-pot multicomponent synthetic techniques. The anticancer activity of …