New β-carboline derivatives containing imidazolium as potential VEGFR2 inhibitors: synthesis, X-ray structure, antiproliferative evaluations, and molecular modeling.

ABSTRACT: A series of new β-carboline derivatives containing an imidazolium moiety were designed and synthesized via the reaction of β-carboline-1-carboxaldehydes, acetyl chloride, primary amine, and formaldehyde. The antitumor activity of the synthesized compounds was examined against lung carcinoma (A549), gastric carcinoma (BGC-823), murine colon carcinoma (CT-26), liver carcinoma (Bel-7402) and breast carcinoma (MCF-7) cells. The results indicated that most compounds exhibited significant antiproliferative activity, in some cases greater than that of cisplatin, and compound 3z was found to be the most potent antiproliferative agent against A549, BGC823, CT-26, Bel-7402 and MCF-7 cell lines with an IC₅₀ value of 2.7 ± 0.4, 2.7 ± 0.6, 2.4 ± 0.2, 3.2 ± 0.2, and 5.6 ± 0.3 μM, respe

SUBMITTER: Ma L 

PROVIDER: S-EPMC9491354 | biostudies-literature | 2022 Sep

REPOSITORIES: biostudies-literature