Abstract
Two new copper(II) and copper(I) complexes were synthesized and tested for their cytotoxic properties.
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Herein, two new copper complexes, {[Cu(dmp)2(H2O)]·(PA)2},(1) and {[Cu(dmp)2]·(PA)},(2) (dmp = 1,10-dimethyl-2,9-phenanthroline, PA = picric acid) have been synthesized solvothermaly and crystal structures were determined by single-crystal X-ray diffraction (SCXRD) technique. Both the complexes 1 and 2 show distorted square planar and distorted tetrahedral geometry around the copper (II) and copper (I) metal centers. In vitro antitumor screening against THP-1 (human leukemia monocytic), PC-3 (human prostate cancer), and SW480 (human colon cancer) cancers indicated their good antiproliferative potential. The morphological assessment data obtained by using dual AO/EB fluorescent staining with THP-1 cell reveal that 1 induces cell death by necrosis, while 2 results in early apoptosis mechanistic pathways. Furthermore, molecular docking of 1′ and 2′ (after removal of picric acid) with DNA of two different conformers were carried out to recognize its preferential binding site either with the minor or major groove of the DNA helix. Together, these results suggest that the copper complexes bearing different oxidation states mediated cell death operates combined mechanism encompassing apoptosis and necrosis possibly due to the DNA damage. The present studies suggest that the picric acid derived copper complexes could be an attractive chemotherapeutic agents against cytotoxic cells.