Multifaceted activity of polycyclic MDR revertant agents in drug-resistant leukemic cells: Role of the spacer was written by Caciolla, Jessica;Picone, Giovanna;Farruggia, Giovanna;Valenti, Dario;Rampa, Angela;Malucelli, Emil;Belluti, Federica;Trezza, Alfonso;Spiga, Ottavia;Iotti, Stefano;Gobbi, Silvia;Cappadone, Concettina;Bisi, Alessandra. And the article was included in Bioorganic Chemistry in 2021.HPLC of Formula: 27469-60-9 This article mentions the following:
A small library of derivatives carrying a polycyclic scaffold recently identified by us as a new privileged structure in medicinal chem. was designed and synthesized, aiming at obtaining potent MDR reverting agents also endowed with antitumor properties. In particular, as a follow-up of our previous studies, attention was focused on the role of the spacer connecting the polycyclic core with a properly selected nitrogen-containing group. A relevant increase in reverting potency was observed, going from the previously employed but-2-ynyl- to a pent-3-ynylamino moiety, as in compounds 3d and 3e, while the introduction of a triazole ring proved to differently impact on the activity of the compounds The docking results supported the data obtained by biol. tests, showing, for the most active compounds, the ability to establish specific bonds with P-glycoprotein. Moreover, a multifaceted anticancer profile and dual in vitro activity was observed for all compounds, showing both revertant and antitumor effects on leukemic cells. In this respect, 3c emerged as a “triple-target” agent, endowed with a relevant reverting potency, a considerable antiproliferative activity and a collateral sensitivity profile. In the experiment, the researchers used many compounds, for example, 4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9HPLC of Formula: 27469-60-9).
4,4-Difluorobenzhydrylpiperazine (cas: 27469-60-9) belongs to piperazine derivatives. The piperazine scaffold is often found in biologically active compounds in different therapeutic areas. These therapeutic areas include antifungals, antidepressants, antivirals, and serotonin receptor (5-HT) antagonists/agonists. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.HPLC of Formula: 27469-60-9
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics