Synthesis and biological evaluation of heterocyclic hydrazone transition metal complexes as potential anticancer agents. Issue 111 (17th November 2016)

• Record Type: Journal Article
• Authors: Du, Yunpeng; Chen, Wei; Fu, Xiang; Deng, Hang; Deng, JunGang
• Is Part Of: RSC advances. Volume 6:Issue 111(2016)
• Page Start: 109718
• Page End: 109725
• Publication Date: 2016-11-17
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/c6ra23477a
• Languages: English
• ISSNs: 2046-2069

Abstract

Abstract : Only the [Cu(L)2 ] complex can significantly increase the intracellular ROS levels, leading to relatively high antiproliferative potency. Abstract : In an effort to better understand the anticancer activity of the tridentate heterocyclic hydrazone metal complexes, three new transition metal complexes with ( E )-4-hydroxy- N ′-(quinolin-2-ylmethylene)benzohydrazide (HL), [Co(L)2 ] (C1 ), [Ni(L)2 ] (C2 ) and [Cu(L)2 ] (C3 ) were synthesized and characterized. The Cu(ii ) complexC3 had significantly higher intracellular reactive oxygen species (ROS) level and antitumor efficacy thanC1 andC2 . Further apoptosis, mitochondrial membrane potential and western blot studies showed thatC3 can effectively induce caspase-mediated apoptosis in A549 cells through the activation of the mitochondrial signaling pathway. Moreover, the affinity ofC3 towards human serum albumin (HSA) was investigated by fluorescence spectroscopy and molecular docking, which revealed hydrophobic interaction and hydrogen bonds in the subdomain IIA of HSA.