Investigation of 2-phenylimidazo[1,2- a ]quinolines as potential antiproliferative agents

It has been demonstrated that the lead compound 2-phenylimidazo[1,2- ]quinoline selectively inhibits CYP1 enzymes. Additionally, CYP1 inhibition has been linked to inducing antiproliferative effects in various breast cancer cell lines as well as relieving drug resistance caused by CYP1 upregulation....

Full description

Saved in:
Bibliographic Details
Published in:Future medicinal chemistry 2023-02, Vol.15 (3), p.229-239
Main Authors: Rees, Shaun W P, Jones-Moore, Hayden, Leung, Euphemia, Barker, David, Pilkington, Lisa I
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemistry
Cell Line, Tumor
Cell Proliferation
Cytochrome P-450 CYP1A1 - metabolism
Cytochrome P-450 CYP1A1 - pharmacology
Drug Screening Assays, Antitumor
Humans
MCF-7 Cells
Models, Molecular
Quinolines - pharmacology
Structure-Activity Relationship
Citations: Items that this one cites
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:It has been demonstrated that the lead compound 2-phenylimidazo[1,2- ]quinoline selectively inhibits CYP1 enzymes. Additionally, CYP1 inhibition has been linked to inducing antiproliferative effects in various breast cancer cell lines as well as relieving drug resistance caused by CYP1 upregulation. Herein, 54 novel analogs of 2-phenylimidazo[1,2- ]quinoline have been synthesized with varied substitution on the phenyl and imidazole rings. Antiproliferative testing was conducted using H thymidine uptake assays. 2-Phenylimidazo[1,2- ]quinoline and phenyl-substituted analogs (3-OMe), (2,3-napthalene) displayed excellent anti-proliferative activities, demonstrating their potency against cancer cell lines for the first time. Molecular modeling suggested that and bind similarly to in the CYP1 binding site.
ISSN:1756-8919
1756-8927
DOI:10.4155/fmc-2022-0152