Design and synthesis of indenoisoquinolines targeting topoisomerase I and other biological macromolecules for cancer chemotherapy

M Cushman - Journal of Medicinal Chemistry, 2021 - ACS Publications
… that some of the 7-azaindenoisoquinolines had the ability to … research led to very potent
cytotoxic anticancer agents, it also … rewarded with the extremely cytotoxic 3-fluoro derivative 62 (…

Development in the Synthesis, Topoisomerase I inhibitor and Cytototoxic Properties of Indenoisoquinoline and Its Analogs

D Zeleke, AM Yadessa - Ethiopian Journal of Science and …, 2021 - 213.55.101.19
… chance to develop more effective anticancer drugs in addition to those … Design and Synthesis
of Chlorinated and Fluorinated 7-Azaindenoisoquinolines as Potent Cytotoxic Anticancer

Discovery of 4-alkoxy-2-aryl-6, 7-dimethoxyquinolines as a new class of topoisomerase I inhibitors endowed with potent in vitro anticancer activity

MM Elbadawi, WM Eldehna, W Wang… - European journal of …, 2021 - Elsevier
… potential anticancer agents targeting Topoisomerase I (TOP1), … synthesis of compounds with
different scaffolds can inhibit … TOP1 poisoning activity of the most potent cytotoxic 4-alkoxy-2-…

… of the Pharmacokinetics and Anticancer Activities of Indenoisoquinoline Derivatives That Stabilize the G-Quadruplex in the MYC Promoter and Inhibit Topoisomerase …

Y Han, A Buric, V Chintareddy, M DeMoss… - Journal of Medicinal …, 2024 - ACS Publications
anticancer drugs, dual-downregulation of MYC and … in Raji vs CA-46 cells and cytotoxicity
in MYC-dependent cell lines. … the design and synthesis of new 7-azaindenoisoquinolines and …

2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights

MM Elbadawi, WM Eldehna… - … of Enzyme Inhibition …, 2022 - Taylor & Francis
… Recently, we have developed a new series of 6,7-dimethoxy-4-alkoxy-2-arylquinolines as
Topoisomerase I (TOP1) inhibitors with potent anticancer activity. Utilising the SAR outputs …

Multiple Topoisomerase I (TopoI), Topoisomerase II (TopoII) and Tyrosyl-DNA Phosphodiesterase (TDP) inhibitors in the development of anticancer drugs

E Baglini, S Salerno, E Barresi, M Robello… - European Journal of …, 2021 - Elsevier
… to inhibition of one class of topoisomerase enzymes is … in the development of potent, efficient
and safe anticancer agents. … only few differences in their cytotoxicity activity, which could …

The indenoisoquinoline LMP517: A novel antitumor agent targeting both TOP1 and TOP2

L Marzi, Y Sun, SN Huang, A James… - Molecular cancer …, 2020 - AACR
… mode of inhibition, termed interfacial inhibition, was first discovered for the topoisomerase
, in which the addition of a fluorine at position 3 replaces the methoxy groups at position 2, 3 of …

Design, synthesis, and anticancer activities of 8, 9-substituted Luotonin A analogs as novel topoisomerase I inhibitors

Y Xiang, H Li, J Wang, X Peng, C Hu, L Luo - Medicinal Chemistry …, 2021 - Springer
… replication by inhibiting bacterial DNA gyrase and topoisomerase IV … and anticancer
compounds contained the 6-fluoro and 7-… The more potent cytotoxicity of 6g might be due to a …

Recent advances in the synthetic thymidine phosphorylase inhibitors for cancer therapy

Q Feng, W Yang, Z Peng, G Wang - European Journal of Pharmacology, 2022 - Elsevier
… activity of TP inhibitors in combination with other anticancer drugs is less. Therefore, it is …
affect for potency, and the introduction fluorine showed better activity than the chlorine group at …

Development of a metabolically stable topoisomerase I poison as anticancer agent

B Kundu, D Sarkar, SP Chowdhuri, S Pal… - European Journal of …, 2020 - Elsevier
… 16 with fluoro substitution resulted in marked decrease in the … To our satisfaction, compound
3 was found to be less cytotoxic in … the way for the development of effective anticancer drugs. …