Topoisomerase I inhibitors: Challenges, progress and the road ahead

A Talukdar, B Kundu, D Sarkar, S Goon… - European Journal of …, 2022 - Elsevier
Abstract Topoisomerase IB (Top1), a subcategory of DNA topoisomerase enzymes is
expressed much higher in several tumor cells. Therefore, modulating the activity of Top1 in …

Quinoline anticancer agents active on DNA and DNA-interacting proteins: From classical to emerging therapeutic targets

A Lauria, G La Monica, A Bono, A Martorana - European Journal of …, 2021 - Elsevier
Quinoline is one of the most important and versatile nitrogen heterocycles embodied in
several biologically active molecules. Within the numerous quinolines developed as …

The design and discovery of topoisomerase I inhibitors as anticancer therapies

E Martín-Encinas, A Selas, F Palacios… - Expert Opinion on Drug …, 2022 - Taylor & Francis
Introduction Cancer has been identified as one of the leading causes of death worldwide.
The biological target of some anticancer agents is topoisomerase I, an enzyme involved in …

Development, optimization, and in vivo validation of new imidazopyridine chemotypes as dual TLR7/TLR9 antagonists through activity-directed sequential …

N Das, P Bandopadhyay, S Roy, BP Sinha… - Journal of Medicinal …, 2022 - ACS Publications
Undesirable activation of endosomal toll-like receptors TLR7 and TLR9 present in specific
immune cells in response to host-derived ligands is implicated in several autoimmune …

1, 3, 4-Oxadiazole containing compounds as therapeutic targets for cancer therapy

MJ Ahsan - Mini Reviews in Medicinal Chemistry, 2022 - ingentaconnect.com
Background: Cancer is the first or second leading cause of premature death in 134 of 183
countries in the world. 1, 3, 4-Oxadiazoles are five membered heterocyclic rings containing …

Development of selective class I protein arginine methyltransferase inhibitors through fragment-based drug design approach

D Bhattacharya, ASM Li, B Paul, UG Dastidar… - European Journal of …, 2023 - Elsevier
Protein arginine methyltransferases (PRMTs) catalyze the methylation of the terminal
nitrogen atoms of the guanidino group of arginine of protein substrates. The aberrant …

Novel pyrido [2′, 1′: 2, 3] imidazo [4, 5-c] quinoline derivative selectively poisons leishmania donovani bisubunit topoisomerase 1 to inhibit the antimony-resistant …

SP Chowdhuri, S Dhiman, SK Das… - Journal of Medicinal …, 2023 - ACS Publications
The unique bisubunit structure of Leishmania donovani topoisomerase 1B (LdTop1) is a
potential drug target in the parasites unlike the monomeric Top1 from its human host …

Discovery of novel benzofuro [3, 2-b] quinoline derivatives as dual CDK2/Topo I inhibitors

Y Huang, W Liu, S Huang, D Li, C Xu, X Jiang, M Liu… - Bioorganic …, 2022 - Elsevier
Uncontrolled cell proliferation is a hallmark of cancer. The major regulator of the cell cycle,
cyclin dependent kinase 2 (CDK2), has become a mature target for cancer treatment …

Methods and compounds for restoring mutant p53 function

B Vu, R Dominique, H Li, B Fahr, Y Chen - US Patent 11,926,632, 2024 - Google Patents
KZPYGQFFRCFCPP-UHFFFAOYSA-N 1, 1'-bis (diphenylphosphino) ferrocene Chemical
compound [Fe+2]. C1= CC= C [C-] 1P (C= 1C= CC= CC= 1) C1= CC= CC= C1. C1= CC= C …