Design, Synthesis, and Evaluation of a New Series of 2-Pyrazolines as Potential Antileukemic Agents

1Citations
Citations of this article
7Readers
Mendeley users who have this article in their library.

This article is free to access.

Abstract

In an attempt to identify small molecules for the treatment of leukemia, 12 new pyrazolines (2a-l) were synthesized efficiently. WST-1 assay was performed to examine their cytotoxic features on HL-60 human acute promyelocytic leukemia (APL), K562 human chronic myeloid leukemia (CML), and THP-1 human acute monocytic leukemia cells. Four compounds (2e, 2f, 2g, and 2h) were determined as promising antileukemic agents on HL-60 and K562 cells. IC50 values of compounds 2f, 2h, 2e, 2g, and bortezomib for the HL-60 cell line were found as 33.52, 42.89, 48.02, 62.34, and 31.75 μM, while IC50 values of compounds 2h, 2g, 2f, 2e, and bortezomib for K562 cells were determined as 33.61, 50.23, 57.28, 76.90, and 42.69 μM, respectively. Further studies were carried out to shed light on the mechanism of antileukemic action. According to the data obtained by in vitro experiments, 1-(4-fluorophenyl)-3-(thiophen-3-yl)-5-(4-(4-methylpiperazin-1-yl)phenyl)-2-pyrazoline (2f) and 1-(3-bromophenyl)-3-(thiophen-3-yl)-5-(4-(4-methylpiperazin-1-yl)phenyl)-2-pyrazoline (2h) have proved to be potential antileukemic agents with remarkable cytotoxicity against HL-60 and K562 cells by activation of caspase 3, thereby inducing apoptosis.

Cite

CITATION STYLE

APA

Altıntop, M. D., Cantürk, Z., & Özdemir, A. (2023). Design, Synthesis, and Evaluation of a New Series of 2-Pyrazolines as Potential Antileukemic Agents. ACS Omega, 8(45), 42867–42877. https://doi.org/10.1021/acsomega.3c05860

Register to see more suggestions

Mendeley helps you to discover research relevant for your work.

Already have an account?

Save time finding and organizing research with Mendeley

Sign up for free