Novel topoisomerase II/EGFR dual inhibitors: design, synthesis and docking studies of naphtho[2′,3′:4,5]thiazolo[3,2-a]pyrimidine hybrids as potential anticancer …
MAE Mourad, A Abo Elmaaty, I Zaki… - Journal of Enzyme …, 2023 - Taylor & Francis
Topoisomerases II are ubiquitous enzymes with significant genotoxic effects in many critical
DNA processes. Additionally, epidermal growth factor receptor (EGFR) plays pivotal role in …
DNA processes. Additionally, epidermal growth factor receptor (EGFR) plays pivotal role in …
New benzothienopyran and benzothienopyranopyrimidine derivatives as topoisomerase I inhibitors: Design, synthesis, anticancer screening, apoptosis induction and …
New benzothienopyran and benzothienopyranopyrimidine derivatives were synthesized
based on the structural requirements of topoisomerase I inhibitors. All target compounds …
based on the structural requirements of topoisomerase I inhibitors. All target compounds …
Design, synthesis and anti-tumor activity of novel benzimidazole-chalcone hybrids as non-intercalative topoisomerase II catalytic inhibitors
Chemical diversification of type II topoisomerase (Topo II) inhibitors remains indispensable
to extend their anti-tumor therapeutic values which are limited by their side effects. Herein …
to extend their anti-tumor therapeutic values which are limited by their side effects. Herein …
Design, synthesis, docking, and anticancer evaluations of new thiazolo[3,2-a] pyrimidines as topoisomerase II inhibitors
MS El-Zoghbi, SA El-Sebaey… - Journal of Enzyme …, 2023 - Taylor & Francis
Abstract New thiazolopyrimidine derivatives 2, 3a-d, 4a-c, 5, 6a-c, and 7a, b were
synthesised. All prepared compounds were evaluated by MTT cytotoxicity assay against …
synthesised. All prepared compounds were evaluated by MTT cytotoxicity assay against …
Design and novel synthetic approach supported with molecular docking and biological evidence for naphthoquinone-hydrazinotriazolothiadiazine analogs as …
A novel synthetic approach was developed for the synthesis of 3-
hydrazinotriazolothiadiazines in just one step from Purpald and phenacyl bromides. They …
hydrazinotriazolothiadiazines in just one step from Purpald and phenacyl bromides. They …
Synthesis and biological evaluation of new 2, 5-dimethylthiophene/furan based N-acetyl pyrazolines as selective topoisomerase II inhibitors
Based on reported pharmacophores as topoisomerase inhibitors, 2, 5-dimethylthiophene/
furan based N-acetyl pyrazolines were designed and envisaged as topoisomerase …
furan based N-acetyl pyrazolines were designed and envisaged as topoisomerase …
Design, synthesis and biological evaluation of novel 7-alkylamino substituted benzo [a] phenazin derivatives as dual topoisomerase I/II inhibitors
BL Yao, YW Mai, SB Chen, HT Xie, PF Yao… - European journal of …, 2015 - Elsevier
A novel series of benzo [a] phenazin derivatives bearing alkylamino side chains were
designed, synthesized and evaluated for their topoisomerases inhibitory activity as well as …
designed, synthesized and evaluated for their topoisomerases inhibitory activity as well as …
New pyranopyrazole based derivatives: Design, synthesis, and biological evaluation as potential topoisomerase II inhibitors, apoptotic inducers, and antiproliferative …
A new series of pyranopyrazole-based derivatives were designed and synthesized. The
synthesized compounds were assessed for their cytotoxic efficacy against A549 human lung …
synthesized compounds were assessed for their cytotoxic efficacy against A549 human lung …
Design, molecular modeling and anticancer evaluation of thieno [2, 3-d] pyrimidine derivatives as inhibitors of topoisomerase II
SA El-Metwally, AK Khalil, WM El-Sayed - Bioorganic Chemistry, 2020 - Elsevier
Abstract Synthesis of 4-(3, 5-dimethyl-1H-pyrazol-1-yl)-5, 6, 7, 8-tetrahydrobenzo [4, 5]
thieno [2, 3-d] pyrimidine 1 and its functionalized reactions as nucleophile with various …
thieno [2, 3-d] pyrimidine 1 and its functionalized reactions as nucleophile with various …
Novel Thiazolidine-2, 4-dione-trimethoxybenzene-thiazole Hybrids as Human Topoisomerases Inhibitors
MS Sinicropi, J Ceramella, P Vanelle, D Iacopetta… - Pharmaceuticals, 2023 - mdpi.com
Cancer is a complex and heterogeneous disease and is still one of the leading causes of
morbidity and mortality worldwide, mostly as the population ages. Despite the encouraging …
morbidity and mortality worldwide, mostly as the population ages. Despite the encouraging …