Dei, Silvia published the artcileDesign and synthesis of new potent N,N-bis(arylalkyl)piperazine derivatives as multidrug resistance (MDR) reversing agents, Computed Properties of 87179-40-6, the publication is European Journal of Medicinal Chemistry (2018), 7-20, database is CAplus and MEDLINE.
A series of 1,4-substituted arylalkyl piperazine derivatives I (Ar = 2-phenoxyethyl, 4,4-diphenylbutyl, 9-anthracenylmethyl, etc.; Ar1 = cinnamyl, 4,4-bis(4-fluorophenyl)butyl, 4,4-bis(4-methoxyphenyl)butyl, etc.) were synthesized and studied with the aim to obtain potent P-gp-dependent multidrug-resistant (MDR) reversers. The new compounds were designed on the basis of the structures of previous arylamine ester derivatives endowed with high P-gp-dependent multidrug resistance reversing activity. All new compounds were active in the pirarubicin uptake assay on the doxorubicin-resistant erythroleukemia K562cells (K562/DOX). In particular, compounds bearing methoxy aromatic moieties showed fairly high reversal activities. The most potent compounds, I (Ar = (3,4,5-trimethoxyphenoxy)ethyl, 3,4,5-trimethoxycinnamyl, 3,4,5-trimethoxybenzyl; Ar1 = 4,4-bis-(4-methoxyphenyl)butyl, 9-anthracenylmethyl) were further studied by evaluating their doxorubicin cytotoxicity enhancement (reversal fold, RF) and the inhibition of P-gp-mediated rhodamine-123 (Rhd 123) efflux on the K562/DOX cell line. The results of all pharmacol. assays indicated that the combination of a basic piperazine scaffold with arylalkyl residues allowed us to obtain very interesting P-gp modulating compounds Overall compound I (Ar = (3,4,5-trimethoxyphenyl)allyl; Ar1 = 4,4-bis-(4-methoxyphenyl)butyl) appeared the most promising compound being a potent and long-lasting P-gp-dependent MDR modulator.
European Journal of Medicinal Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Computed Properties of 87179-40-6.
Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics