Probing the antibacterial and anticancer potential of tryptamine based mixed ligand Schiff base Ruthenium(III) complexes

被引：45

作者：

Malik, Manzoor Ahmad ^{[1
]}

Raza, Md Kausar ^{[2
]}

Dar, Ovas Ahmad ^{[1
]}

Amadudin ^{[3
]}

Abid, Mohammad ^{[3
]}

Wani, Mohmmad Younus ^{[4
]}

Al-Bogami, Abdullah Saad ^{[4
]}

Hashmi, Athar Adil ^{[1
]}

机构：

[1] Jamia Millia Islamia, Bioinorgan Lab, Dept Chem, New Delhi 110025, India

[2] Indian Inst Sci, Dept Inorgan & Phys Chem, Bangalore 560012, Karnataka, India

[3] Jamia Millia Islamia, Med Chem Lab, Dept Biosci, New Delhi 110025, India

[4] Univ Jeddah, Chem Dept, Fac Sci, POB 80327, Jeddah 21589, Saudi Arabia

来源：

BIOORGANIC CHEMISTRY | 2019年 / 87卷

关键词：

Ru(III) complexes; X-ray crystallography; Antimicrobial; DNA binding; Anticancer; Docking; DNA-BINDING PROPERTIES; CU(II) COMPLEXES; METAL-COMPLEXES; DRUG CANDIDATES; CANCER-THERAPY; DISCOVERY; LIPOPHILICITY; CYTOTOXICITY; CISPLATIN; ANTITUMOR;

D O I：

10.1016/j.bioorg.2019.03.080

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Development of new chemotherapeutic agents to treat microbial infections and recurrent cancers is of pivotal importance. Metal based drugs particularly ruthenium complexes have the uniqueness and desired properties that make them suitable candidates for the search of potential chemotherapeutic agents. In this study, two mixed ligand Ru(III) complexes [Ru(Cl)(2)(SB)(Phen] (RC-1) and [Ru(Cl)(2)(SB)(Bipy)] (RC-2) were synthesised and characterized by elemental analysis, IR, UV-Vis, H-1, C-13 NMR spectroscopic techniques and their molecular structure was confirmed by X-ray crystallography. Antibacterial activity evaluation against two Gram-positive (S. pneumonia and E. faecalis) and four Gram-negative strains (P. aurogenosa, K. pneumoniae, S. enterica, and E. coli) revealed their moderate antibacterial activity with MIC value of >= 250 mu g/mL. Anticancer activity evaluation against a non-small lung cancer cell line (H1299) revealed the tremendous anticancer activity of these complexes which was further validated by DNA binding and docking results. DNA binding profile of the complexes studied by UV-Visible and fluorescence spectroscopy showed an intercalative binding mode with CT-DNA and an intrinsic binding constant in the range of 3.481-1.015 x 10(5) M-1. Both the complexes were also found to exert weak toxicity to human erythrocytes by haemolytic assay compared to cisplatin. Potential of these complexes as anticancer agents will be further delineated by in vivo studies.

引用

页码：773 / 782

页数：10

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