AI Article Synopsis
- Six rhodium(III) and palladium(II) pyrazolopyrimidine complexes were created and tested for their effectiveness against cancer cells.
- * These complexes demonstrated strong cytotoxic effects, particularly showing greater toxicity than the commonly used drug cisplatin in T-24 cancer cells.
- * Complexes 5 and 6 worked by causing DNA damage and triggering apoptosis through cell cycle arrest, while complex 5 also affected cell death via mitochondrial dysfunction, with complex 5 displaying more significant tumor growth inhibition in live mice.
Article Abstract
Six pyrazolopyrimidine rhodium(III) or palladium(II) complexes, [Rh(L)(HO)Cl] (1), [Rh(L)(CHOH)Cl] (2), [Rh(L)(HO)Cl] (3), [Rh(L)Cl]·CHOH (4), [Rh(L)(CHCN)Cl]·0.5CHCN (5), and [Pd(L)Cl] (6), were synthesized and characterized. These complexes showed high cytotoxicity against six tested cancer cell lines. Most of the complexes showed higher cytotoxicity to T-24 cells in vitro than cisplatin. Mechanism studies indicated that complexes 5 and 6 induced G2/M phase cell cycle arrest through DNA damage, and induced apoptosis via endoplasmic reticulum stress response. In addition, complex 5 also induced cell apoptosis via mitochondrial dysfunction. Complexes 5 and 6 showed low in vivo toxicity and high tumor growth inhibitory activity in mouse tumor models. The inhibitory effect of rhodium complex 5 on tumor growth in vivo was more pronounced than that of palladium complex 6.
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| http://dx.doi.org/10.1016/j.bioorg.2023.106838 | DOI Listing |
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