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Exploring the in vitro anticancer activities of Re(I) picolinic acid and its fluorinated complex derivatives on lung cancer cells: a structural study
JBIC Journal of Biological Inorganic Chemistry ( IF 2.7 ) Pub Date : 2022-12-04 , DOI: 10.1007/s00775-022-01971-2
Mabu L Matlou 1 , Frederick P Malan 2 , Sanah Nkadimeng 3 , Lyndy McGaw 4 , Vuyelwa J Tembu 1 , Amanda-Lee E Manicum 1
Affiliation  

Fifteen rhenium(I) tricarbonyl complexes of the form fac-[Re(N,O’)(CO)3(X)], where N,O’-bidentate ligand = 2-picolinic acid (Pico); 3,5-difluoropyridine-2-carboxylic acid (Dfpc); 3-trifluoromethyl-pyridine-2-carboxylic acid (Tfpc) and X = H2O; pyrazole (Pz); pyridine (Py); imidazole (Im); and methanol (CH3OH) were synthesized using the ‘2 + 1’ mixed ligand approach with an average yield of 84%. The complexes were characterized using the following spectroscopic techniques: IR, 1H and 13C NMR, UV/Vis, and single-crystal X-ray diffraction. The effect of the fluorine atoms on the backbone of the N,O’-bidentate ligand was investigated and a trend was noticed in the carbonyl stretching frequencies: with Pico < Tfpc < Dfpc. The in vitro biological screening on Vero (healthy mammalian), HeLa (cervical carcinoma) and A549 (lung cancer) cells revealed one toxic complex, fac-[Re(Pico)(CO)3(H2O)], with respective LC50 values of 9.0 ± 0.9, 15.8 ± 4.9 (SI = 0.570) and 20.9 ± 0.8 (SI = 0.430) μg/mL. As a result, it can be used as a positive control drug of toxicity.



中文翻译:

探索 Re(I) 吡啶甲酸及其氟化复合衍生物对肺癌细胞的体外抗癌活性:一项结构研究

fac -[Re( N,O' )(CO) 3 (X)]形式的十五个铼 (I) 三羰基络合物,其中N,O' -双齿配体 = 2-吡啶甲酸 (Pico);3,5-二氟吡啶-2-甲酸 (Dfpc);3-三氟甲基-吡啶-2-甲酸(Tfpc)且X = H 2 O;吡唑 (Pz); 吡啶 (Py);咪唑(Im);和甲醇 (CH 3 OH) 是使用“2 + 1”混合配体方法合成的,平均产率为 84%。使用以下光谱技术对复合物进行表征:IR、1 H 和13 C NMR、UV/Vis 和单晶 X 射线衍射。氟原子对N,O'主链的影响研究了双齿配体,发现羰基伸缩频率有一个趋势:Pico < Tfpc < Dfpc。对 Vero(健康哺乳动物)、HeLa(宫颈癌)和 A549(肺癌)细胞进行的体外生物筛选揭示了一种毒性复合物,fac-[ Re (Pico)(CO) 3 (H 2 O)],以及相应的 LC 9.0 ± 0.9、15.8 ± 4.9 (SI = 0.570) 和 20.9 ± 0.8 (SI = 0.430) μg/mL 的 50 个值因此,它可以作为毒性的阳性对照药物。

更新日期:2022-12-05
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