Qin, Qi-Pin; Wang, Zhen-Feng; Tan, Ming-Xiong; Huang, Xiao-Ling; Zou, Hua-Hong; Zou, Bi-Qun; Shi, Bei-Bei; Zhang, Shu-Hua published the artcile< Complexes of lanthanides(III) with mixed 2,2'-bipyridyl and 5,7-dibromo-8-quinolinoline chelating ligands as a new class of promising anti-cancer agents>, Application of C10H8N2, the main research area is cervical ovarian cancer lanthanide III metal chelation.
Five novel lanthanides(III) complexes, [Lu(Me)(MBrQ)2NO3] (MeMBrQ-Lu), [Ho(MeO)(MBrQ)2NO3] (MeOMBrQ-Ho), [Ho(Me)(MBrQ)2NO3] (MeMBrQ-Ho), [La(Me)2(BrQ)2NO3] (MeBrQ-La) and [Sm(Me)(BrQ)2(CH3OH)NO3] (MeBrQ-Sm) were synthesized in which 2,2′-bipyridyl (4,4′-dimethyl-2,2′-bipyridyl (Me) and 4,4′-dimethoxy-2,2′-bipyridine (MeO)) and 5,7-dibromo-8-quinolinoline derivatives (5,7-dibromo-2-methyl-8-quinolinol (MBrQ-H) and 5,7-dibromo-8-quinolinol (BrQ-H)) act as chelating ligands. The in vitro cytotoxic activities of five Ln(III) complexes have been studied with SK-OV-3/DDP, NCI-H460 and HeLa cancer cells. MeMBrQ-Lu, MeOMBrQ-Ho, MeMBrQ-Ho, MeBrQ-La and MeBrQ-Sm show higher cytotoxicity against the HeLa cells than cisplatin (13.11 ± 0.53 μM). In particular, the MeOMBrQ-Ho and MeMBrQ-Ho complexes exhibit superior cytotoxic activity, with IC50 values at 1.00 ± 0.34 nM and 125.00 ± 1.08 nM. We further demonstrate that MeOMBrQ-Ho and MeMBrQ-Ho inhibit the proliferation of HeLa cells by inhibiting telomerase and targeting mitochondria to induce DNA damage-mediated apoptosis. In addition, MeOMBrQ-Ho significantly inhibits tumor growth with a tumor growth inhibition rate (IR) of 50.8% in a HeLa mouse xenograft model. Taken together, MeOMBrQ-Ho is a novel lanthanide(III) complex with promising antitumor activity.
Metallomics published new progress about Antitumor agents. 366-18-7 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2, Application of C10H8N2.