Development, synthesis and biological investigation of a novel class of potent PC-PLC inhibitors was written by Pilkington, Lisa I.;Sparrow, Kevin;Rees, Shaun W. P.;Paulin, Emily K.;van Rensburg, Michelle;Xu, Chris Sun;Langley, Ries J.;Leung, Ivanhoe K. H.;Reynisson, Johannes;Leung, Euphemia;Barker, David. And the article was included in European Journal of Medicinal Chemistry in 2020.SDS of cas: 182618-86-6 This article mentions the following:
Phospholipases are enzymes that are involved in the hydrolysis of acyl and phosphate esters of phospholipids, generating secondary messengers that have implications in various cellular processes including proliferation, differentiation and motility. As such inhibitors of phospholipases have been widely studied for their use as anti-cancer therapeutics. Phosphatidylcholine-specific phospholipase C (PC-PLC) is implicated in the progression of a number of cancer cell lines including aggressing triple-neg. breast cancers. Most current studies on PC-PLC have utilized D609 as the standard inhibitor however it is known to have multiple failings, including poor stability in aqueous media. 2-Morpholinobenzoic acids were recently identified using vHTS as a potential class of lead compounds, with improvements over D609. In this work 129 analogs in this class were prepared and their PC-PLC inhibitory activity was assessed. It was found that the majority of these novel compounds had improved activity when compared to D609 with the most potent inhibitors completely inhibiting enzyme activity. It was determined that the best compound/s contained a morpholino and 2-substituted N-benzyl moieties with these findings explained using mol. modeling. The compounds reported here will allow for improved study of PC-PLC activity. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6SDS of cas: 182618-86-6).
1-Boc-4-(4-Nitrophenyl)piperazine (cas: 182618-86-6) belongs to piperazine derivatives. Piperazine is a fairly basic compound and is an amine solvent. 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.SDS of cas: 182618-86-6
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics