Options
Synthesis and biological evaluation of anthra[1,9-cd]pyrazol-6(2H)-one scaffold derivatives as potential anticancer agents
Journal
Arabian Journal of Chemistry
Journal Volume
12
Journal Issue
8
Pages
2864-2881
Date Issued
2019
Author(s)
Chen T.-C.
Hsu H.-W.
Chen C.-L.
Lee C.-C.
Wu C.-L.
Lee Y.-R.
Yu D.-S.
Huang H.-S.
Abstract
Several anthrapyrazolone derivatives derived from 7-chloroanthra[1,9-cd]pyrazol-6(2H)-one and 7-chloro-2-(2-hydroxyethyl)anthra[1,9-cd] pyrazol-6(2H)-one have been prepared by the addition or substitution nucleophilic reactions and further transformed into extended tetracyclic systems and fused to different nitrogenheterocyclic rings into the pharmacophore structure moiety. The compounds synthesized were evaluated for their cytotoxic activity and telomerase activity in prostate cancer cell line by SRB assay and in human non-small cell lung carcinoma cell line by TRAP assay, respectively. Compounds 1–6, 13, 14, 16, 17, 19, 21, 23, 28 and 31 were selected by the NCI and only 1, 4, and 16 represent the GI50, TGI and LC50, respectively. Among them, 1 and 16 exhibited distinctive selectivity of GI50 of 10.498 μM and 4.542 μM over 60 cell lines which is better than the average GI50 (20.3 μM) for SP600125 (NSC75890). Overall, the test compounds exhibited different telomerase and cytotoxic activities and only few compounds displayed antitumor activity in the low range. ? 2015 The Authors
SDGs
Other Subjects
Cell culture; Cytotoxicity; Diseases; Anthrapyrazolone; Anti-tumor activities; Antiproliferation; Biological evaluation; Non-small cell lung carcinomata; Nucleophilic reaction; Potential anticancer agents; Prostate cancer cells; Cells
Publisher
Elsevier B.V.
Type
journal article