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4-Phenyl quinoline derivatives as potential serotonin receptor ligands with antiproliferative activity.

Abstract：

:Antagonists of signaling receptors are often effective non-toxic therapeutic agents. Over the years, there have been evidences describing the role of serotonin or 5-hydroxytryptamine (5-HT) in development of cancer. Although there are reports on the antiproliferative effects of some serotonin receptor antagonists, there are very few investigations related to understanding their structure-activity relationships. In this study, we report the screening of a library of 4-phenyl quinoline derivatives for their antiproliferative activities. Preliminary docking studies indicated that these ligands had the ability to bind to two of the serotonin receptors, 5-HT1B and 5-HT2B. The results of the in silico experiments were validated by performing in vitro studies on MCF-7 breast cancer cell line. The ethylpiperazine derivatives showed maximum toxicity against this cancer cell line. The compounds inhibited Calcium ion efflux (induced by serotonin) and ERK activation. One of the most active 4-phenyl quinoline derivatives (H3a) also induced apoptosis, thereby, suggesting the use of this scaffold as a potential anticancer drug.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Joshi PV,Sayed AA,RaviKumar A,Puranik VG,Zinjarde SS

doi

10.1016/j.ejmech.2017.05.002

subject

Has Abstract

pub_date

2017-08-18 00:00:00

pages

246-258

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(17)30363-X

journal_volume

136

pub_type

杂志文章

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