| Abstrakt: |
A recent report from the University of Szeged in Hungary discusses research on antiproliferative activity, specifically focusing on the synthesis of estrone heterodimers and their evaluation in vitro. The researchers combined different molecular entities to create these hybrids, aiming to develop drug candidates with selective action and reduced side effects. The newly synthesized dimers were tested against various human adherent gynecological cancer cell lines, and one heterodimer showed significant antiproliferative activity. The researchers also observed a proapoptotic effect and cell cycle blockade in the G2/M phase, potentially due to the dimer's impact on tubulin polymerization. Computational calculations suggested potential binding of the steroidal building blocks to the taxoid binding site of tubulin. [Extracted from the article] |
