Design, Synthesis, and Evaluation of a New Series of 2-Pyrazolines as Potential Antileukemic Agents
Year: 2023
Type: article
Abstract: High Resolution Image Download MS PowerPoint Slide 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. IC 50 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 IC 50 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.
Source: ACS Omega
Institution: Anadolu University
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: gold
Estimated APC paid: $1,685
Funder: Anadolu Üniversitesi
Award: G8851789934
OpenAlex ID: W4388103727