Quinoline anticancer agents active on DNA and DNA-interacting proteins: From classical to emerging therapeutic targets
| Autor: | Gabriele La Monica, Annamaria Martorana, Alessia Bono, Antonino Lauria |
|---|---|
| Přispěvatelé: | Lauria, Antonino, La Monica, Gabriele, Bono, Alessia, Martorana, Annamaria |
| Rok vydání: | 2021 |
| Předmět: |
medicine.drug_class
Antineoplastic Agents 01 natural sciences 03 medical and health sciences chemistry.chemical_compound Drug Discovery medicine Humans Amsacrine 030304 developmental biology Cell Proliferation Pharmacology 0303 health sciences DNA Intercalators G-quadruplex Topoisomerase Epigenetic targets Antiproliferative compounds SAR studies biology Molecular Structure 010405 organic chemistry Topoisomerase Organic Chemistry Quinoline General Medicine DNA Neoplasm Settore CHIM/08 - Chimica Farmaceutica 0104 chemical sciences DNA-Binding Proteins G-Quadruplexes Histone chemistry Biochemistry biology.protein Quinolines Histone deacetylase Camptothecin DNA Topoisomerase inhibitor medicine.drug |
| Zdroj: | European journal of medicinal chemistry. 220 |
| ISSN: | 1768-3254 |
| Popis: | Quinoline is one of the most important and versatile nitrogen heterocycles embodied in several biologically active molecules. Within the numerous quinolines developed as antiproliferative agents, this review is focused on compounds interfering with DNA structure or with proteins/enzymes involved in the regulation of double helix functional processes. In this light, a special focus is given to the quinoline compounds, acting with classical/well-known mechanisms of action (DNA intercalators or Topoisomerase inhibitors). In particular, the quinoline drugs amsacrine and camptothecin (CPT) have been studied as key lead compounds for the development of new agents with improved PK and tolerability properties. Moreover, notable attention has been paid to the quinoline molecules, which are able to interfere with emerging targets involved in cancer progression, as G-quadruplexes or the epigenetic ones (e.g.: histone deacetylase, DNA and histones methyltransferase). The antiproliferative and the enzymatic inhibition data of the reviewed compounds have been analyzed. Furthermore, concerning the SAR (structure-activity relationship) aspects, the most recurrent ligand-protein interactions are summarized, underling the structural requirements for each kind of mechanism of action. |
| Databáze: | OpenAIRE |
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