Zn(II) and Co(II) derivatives anchored with scorpionate precursor: Antiproliferative evaluation in human cancer cell lines
- Citation:
- Das, K, Datta A, Frontera A, Wen YS, Roma-Rodrigues C, Raposo LR, Fernandes AR, Hung CH. 2020. Zn(II) and Co(II) derivatives anchored with scorpionate precursor: Antiproliferative evaluation in human cancer cell lines, 2020. J Inorg Biochem. 202:110881.
Abstract:
A 'scorpionate' type precursor [bdtbpza=bis(3,5-di-t-butylpyrazol-1-yl)acetate] has been employed to synthesize two mononuclear Zn(II) and Co(II) derivatives, namely [Zn(bdtbpza)2 (H2O)2].2.5CH3OH.2[(CH3)3C-C3H2N2-C(CH3)3] (1) and [Co(bdtbpza)2(CH3OH)4] (2) in good yield. Single crystal X-ray diffraction analysis reveals that in 1, the Zn(II) atom is tetrahedrally surrounded by a pair of Oacetate atoms of two bis(pyrazol-1-yl)acetate units and two water molecules; while in 2, the Co(II) atom shows an octahedral environment coordinating a pair of Oacetate atoms of two bis(pyrazol-1-yl)acetate units along with four methanol molecules. The EPR spectra of 2 recorded at 77 and 298K confirmed the tetragonal symmetry of the high spin Co(II). The DFT (Density functional theory) computation is in good agreement with the geometry proposed for compounds 1 and 2. Both the compounds display a high antiproliferative activity against HCT116 (colorectal carcinoma) and A2780 (ovarian carcinoma) cell lines compared to human normal dermal fibroblasts. In the case of A2780 cells, compounds 1 and 2 exhibit IC50 values that are similar to those described for cisplatin, a widely used chemotherapeutic drug. Exposure of A2780 cells to the IC50 concentration of each compound led to an increase of the number of apoptotic and autophagic cells. In the case of compound 1, the accumulation of intracellular ROS (Reactive oxygen species) is responsible for triggering A2780 cell death.
Notes:
Das, KuheliDatta, Amitabha
Frontera, Antonio
Wen, Yuh-Sheng
Roma-Rodrigues, Catarina
Raposo, Luis R
Fernandes, Alexandra R
Hung, Chen-Hsiung
eng
Research Support, Non-U.S. Gov't
J Inorg Biochem. 2020 Jan;202:110881. doi: 10.1016/j.jinorgbio.2019.110881. Epub 2019 Oct 23.