Synthesis of novel SRPK1-targeting hybrid compounds incorporating antimetabolites for cancer therapy
Year: 2025
Type: article
Abstract: assays were performed to evaluate SRPK1 inhibition and antiproliferative activity in selected cancer cell lines. Among the tested compounds, the JH-VII-139-1-based hybrid geo140 exhibited notable SRPK1 inhibitory potency and cytotoxic effects, demonstrating a favorable profile for further optimization. Interestingly, treatment with geo140 did not appear to alter the overall SRPK1 distribution in interphase cells but resulted in a notable increase of mitotic cells that displayed a substantial accumulation of SRPK1, thus suggesting that the hybrid compound may have an impact on cell cycle progression. This work supports the potential of molecular hybridization as a strategy for the development of novel SRPK1-targeting anticancer agents.
Source: RSC Medicinal Chemistry
DOI: 10.1039/d5md00731c
Authors: George Leonidis, Ioanna Sigala, Michail Spathakis, George Kolios, Thomas Giannakouros, Eleni Nikolakaki, Vasiliki Sarli
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: hybrid
OpenAlex ID: W4414613099