Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces was written by Rabal, Obdulia;Sanchez-Arias, Juan Antonio;San Jose-Eneriz, Edurne;Agirre, Xabier;de Miguel, Irene;Garate, Leire;Miranda, Estibaliz;Saez, Elena;Roa, Sergio;Martinez-Climent, Jose Angel;Liu, Yingying;Wu, Wei;Xu, Musheng;Prosper, Felipe;Oyarzabal, Julen. And the article was included in Journal of Medicinal Chemistry in 2018.Recommanded Product: 144222-22-0 This article mentions the following:
Epigenetic regulators that exhibit aberrant enzymic activities or expression profiles are potential therapeutic targets for cancers. Specifically, enzymes responsible for methylation at histone-3 lysine-9 (like G9a) and aberrant DNA hypermethylation (DNMTs) have been implicated in a number of cancers. Recently, mols. bearing a 4-aminoquinoline scaffold were reported as dual inhibitors of these targets and showed a significant in-vivo efficacy in animal models of hematol. malignancies. Here, we report a detailed exploration around three growing vectors born by this chemotype. Exploring this chem. space led to the identification of features to navigate G9a and DNMT1 biol. spaces; not only their corresponding exclusive areas, selective compounds, but also common spaces. Thus, we identified from selective G9a and first-in-class DNMT1 inhibitors, > 1 log unit between their IC50 values, with IC50 < 25nM (e.g. 43 and 26, resp.) to equipotent inhibitors with IC50 < 50nM for both targets (e.g. 13). Their ADME/Tox profiling and antiproliferative efficacies, vs. some cancer cell lines, are also reported. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0Recommanded Product: 144222-22-0).
1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives.Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Recommanded Product: 144222-22-0
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem