Khursheed, Salman; Tabassum, Sartaj; Arjmand, Farukh published the article 《Comprehensive biological {DNA/RNA binding profile, cleavage &cytotoxicity activity} of structurally well-characterized chromone-appended Cu(II)(L1-3)(phen) potential anticancer drug candidates》. Keywords: preparation copper phenanthroline fluoroformylchromone bromoformylchromone nitrate complex; crystal structure copper phenanthroline fluoroformylchromone bromoformylchromone nitrate complex; mol structure copper phenanthroline fluoroformylchromone bromoformylchromone nitrate complex; DNA RNA interaction copper phenanthroline fluoroformylchromone bromoformylchromone nitrate complex; anticancer activity copper phenanthroline fluoroformylchromone bromoformylchromone nitrate complex; antimicrobial activity copper phenanthroline fluoroformylchromone bromoformylchromone nitrate complex; cyclic voltammetry copper phenanthroline fluoroformylchromone bromoformylchromone nitrate complex.They researched the compound: 1,10-Phenanthroline( cas:66-71-7 ).Category: piperazines. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:66-71-7) here.
A series of chromone-appended copper(II)(phen) complexes (1-3) having the general formulas [Cu(L1)(phen)(H2O)2(NO3)] 1, [Cu(L2)(phen)(NO3)] 2 and [Cu(L3)(phen)(NO3)] 3, where L1 = 3-formylchromone, L2 = 6-fluoro-3-formylchromone, L3 = 6-bromo-3-formylchromone and phen = 1,10-phenanthroline were prepared to examine the effect of halogen on structure activity relation. The mol. solid state structure of (1-3) was fully characterized by employing various spectroscopic techiques, single crystal x-ray diffraction studies and DFT B3LYP (gas phase) computations. Comparative in vitro binding studies of (1-3) with ct-DNA and tRNA were conducted by using a battery of optical {UV-visible, fluorecence and circular dichoric} and electrochem. methods, which implicated strong binding through noncovalent π-π stacking intercalative binding mode. The order of binding is 3 > 2 > 1 as determined by Kb and Ksv values with bromo analog 3 exhibiting the strongest binding affinity for both ct-DNA and tRNA nucleobases, however, underlining more avid predisposed binding with tRNA as compared to ct-DNA. The cleavage activity of (1-3) was studied by electrophoretic assay using pBR322 DNA and tRNA, which exhibited efficient DNA cleaving ability at low micro molar concentrations The cleavage process was mediated by an oxidative pathway involving ROS species viz., singlet oxygen (1O2) and superoxide anions(O•-2), with more pronounced cleaving ability of bromo analog 3 as compared to unsubstituted 1 and fluoro 2 analog derivatives Furthermore, time and concentration dependence of tRNA cleavage was also observed The cytotoxicity activity of tested drug candidates 2 and 3 were evaluated on a panel of human cancer cell lines, viz., MCF-7, MDA-MB-231, AW13516, SiHa and Hop-62 using SRB assay which validated bromo analog 3 and 2 as good anticancer agents, broadly against all the tested cancerous strains (with GI50 values < 10) except with AW13516, SiHa and Hop-62 (GI50 values were found in the range18.00-36.8). Here is just a brief introduction to this compound(66-71-7)Category: piperazines, more information about the compound(1,10-Phenanthroline) is in the article, you can click the link below.
Reference:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics