Piperidine and valproic acid hybrid compound (F2S4-<i>p</i>-VPA) outperforms methotrexate as anti-proliferative and cells migration inhibition.

ABSTRACT: Glioblastoma and triple-negative breast cancer (TNBC) pose significant challenges in treatment due to their invasive nature and propensity for metastasis. Methotrexate (MTX) is a common chemotherapeutic agent; however, it has limited efficacy owing to its low aqueous solubility and cytostatic rather than cytotoxic effects. Valproic acid (VPA) has been used as chemotherapeutic agent, but with low potency. In this study, two novel VPA derivatives (F2S4-p-VPA and F3S4-m-VPA) were designed, chemically synthesized, and evaluated in vitro. These compounds contain tertiary amines as pharmacophore groups reminiscent of methotrexate. Cytotoxicity, migration, assays were conducted on glioblastoma (LN-18, U373) and breast cancer (MDA-MB-231) cell lines, using fibroblast (3T3-L1;

SUBMITTER: Rosales Hernandez MC 

PROVIDER: S-EPMC12266131 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature