Kumbar Mahantesh, Patil Sangamesh A, Toragalmath Shivakumar S, Kinnal Shivashankar M, Shettar Arun, Hosakeri Joy H
P. G. Department of Chemistry, Karnatak University, Dharwad, 580003, Karnataka, India.
K L E's, P. C. Jabin Science College, Autonomous, Vidyanagar, Hubballi, 580031, Karnataka, India.
J Organomet Chem. 2020 May 15;914:121219. doi: 10.1016/j.jorganchem.2020.121219. Epub 2020 Mar 7.
Methoxy and -butyl substituted carboxamide, carboxylic acid and hydrazone Schiff base groups have been assembled into our newly designed fluorenone based ligands and prepared coordination compounds of some first row transition metals and characterized thoroughly with spectroscopic (H and C NMR, IR, GC-MS, UV-Vis), analytical, TGA and molar conductance measurements. The stoichiometry of all the metal complexes is found to be 1: 2 (M: L) with the general formula, [M(L)], where L is a singly deprotonated ligand and the geometry of all the metal complexes is found to be octahedral. Ligands and their metal complexes successfully cleaved the pBR322 plasmid DNA and in case of anticancer activity against MCF-7 (human breast adenocarcinoma) cell line, the synthesized compounds found to exhibit excellent activity with prominent apoptotic effect which is characterized by cell shrinkage, cell breakage and turgidity and results were compared with the standard drug cisplatin. Very significant anticancer activity was observed for compounds LH, Cu(L), Cu(L), Ni(L) and Ni(L) with IC value of <10 μgmL. Molecular docking studies were performed to assess the bonding mode of synthesized compounds. In case of antioxidant activity study, the compounds LH, Ni(L), Ni(L), Cu(L) and Cu(L) exhibited significant scavenging activity with good percentage when compared with remaining tested compounds.
甲氧基和丁基取代的羧酰胺、羧酸和腙席夫碱基团已被组装到我们新设计的基于芴酮的配体中，并制备了一些第一排过渡金属的配位化合物，并用光谱法（氢和碳核磁共振、红外光谱、气相色谱-质谱联用、紫外-可见光谱）、分析法、热重分析法和摩尔电导率测量法进行了全面表征。发现所有金属配合物的化学计量比为1:2（M:L），通式为[M(L)]，其中L为单去质子化配体，且所有金属配合物的几何构型均为八面体。配体及其金属配合物成功切割了pBR322质粒DNA，在对MCF-7（人乳腺腺癌）细胞系的抗癌活性方面，合成的化合物表现出优异的活性，并具有显著的凋亡效应，其特征为细胞收缩、细胞破裂和肿胀，且将结果与标准药物顺铂进行了比较。观察到化合物LH、Cu(L)、Cu(L)、Ni(L)和Ni(L)具有非常显著的抗癌活性，其半数抑制浓度值<10μg/mL。进行了分子对接研究以评估合成化合物的键合模式。在抗氧化活性研究中，与其余测试化合物相比，化合物LH、Ni(L)、Ni(L)、Cu(L)和Cu(L)表现出显著的清除活性，清除率良好。
