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Your search keyword '"Perwez Alam Shaikh"' showing total 2 results
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2 results on '"Perwez Alam Shaikh"'

1. Evaluation of Transition Metal Complexes of Benzimidazole-Derived Scaffold as Promising Anticancer Chemotherapeutics

Author

Afzal Hussain, Mohamed F. AlAjmi, Md. Tabish Rehman, Azmat Ali Khan, Perwez Alam Shaikh, and Rais Ahmad Khan

Subjects
metal complexes, DNA binding/cleavage, cytotoxicity, cell migration/adhesion, apoptosis, toxicity profile, Organic chemistry, QD241-441
Abstract

Three new transition metal complexes, Cu(II) 1, Co(II) 2, and Zn(II) 3 with ligand “bimnap” derived from 1-methyl-2-aminobenzimidazole and 2-hydroxynapthaldehyde were synthesized and characterized. The structure of the ligand was determined by single X-ray crystallography. All the three complexes, 1–3, were examined for the mode of interaction with biomolecule viz., calf thymus-DNA (CT-DNA) using various spectroscopic methods. The nuclease activity was performed against pBR322 DNA that exhibited concentration-dependent degradation of the nucleic acid. The mechanism of DNA cleavage was studied by the electrophoretic pattern in the presence of the radical scavengers. Also, the complexes 1–3 were analyzed for groove binding affinity. Moreover, in vitro cytotoxicities of the complexes 1–3 were tested against the five human cancer cell lines, i.e., HeLa, SK-MEL-1, HepG2, HT108, and MDA-MB 231. Also, the cell adhesion and migration properties upon treatment of cell lines with complexes 1–3, and consequently, their cell death pathway via apoptosis and necrosis were analyzed. Further, complexes 1–3 were studied in vivo for their toxicities and tolerabilities in mice. In sum, the complexes 1–3 showed merits of an effective anticancer agent in cell lines–based study while minor side effects were observed in vivo.

Published
2018
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2. Design, Synthesis, and Biological Evaluation of Benzimidazole-Derived Biocompatible Copper(II) and Zinc(II) Complexes as Anticancer Chemotherapeutics

Author

Mohamed F. Alajmi, Afzal Hussain, Perwez Alam Shaikh, Rais Ahmad Khan, Md. Tabish Rehman, and Azmat Ali Khan

Subjects
Models, Molecular, metal complexes, interaction with biomolecules, nuclease activity, cytotoxicity, toxicity, Molecular Conformation, Apoptosis, Chemistry Techniques, Synthetic, Ligands, 01 natural sciences, HeLa, lcsh:Chemistry, chemistry.chemical_compound, Cell Movement, Fluorescence Resonance Energy Transfer, Cytotoxicity, lcsh:QH301-705.5, Spectroscopy, biology, Chemistry, General Medicine, Ligand (biochemistry), Human serum albumin, Computer Science Applications, Zinc, Biochemistry, Thermodynamics, medicine.drug, Antineoplastic Agents, 010402 general chemistry, Catalysis, Article, Inorganic Chemistry, Cell Line, Tumor, medicine, Cell Adhesion, Humans, Physical and Theoretical Chemistry, DNA Cleavage, Molecular Biology, Serum Albumin, Cisplatin, Nuclease, 010405 organic chemistry, Organic Chemistry, DNA, biology.organism_classification, 0104 chemical sciences, lcsh:Biology (General), lcsh:QD1-999, Drug Design, Cancer cell, biology.protein, Nucleic Acid Conformation, Benzimidazoles, Copper
Abstract

Herein, we have synthesized and characterized a new benzimidazole-derived “BnI” ligand and its copper(II) complex, [Cu(BnI)2], 1, and zinc(II) complex, [Zn(BnI)2], 2, using elemental analysis and various spectroscopic techniques. Interaction of complexes 1 and 2 with the biomolecules viz. HSA (human serum albumin) and DNA were studied using absorption titration, fluorescence techniques, and in silico molecular docking studies. The results exhibited the significant binding propensity of both complexes 1 and 2, but complex 1 showed more avid binding to HSA and DNA. Also, the nuclease activity of 1 and 2 was analyzed for pBR322 DNA, and the results obtained confirmed the potential of the complexes to cleave DNA. Moreover, the mechanistic pathway was studied in the presence of various radical scavengers, which revealed that ROS (reactive oxygen species) are responsible for the nuclease activity in complex 1, whereas in complex 2, the possibility of hydrolytic cleavage also exists. Furthermore, the cytotoxicity of the ligand and complexes 1 and 2 were studied on a panel of five different human cancer cells, namely: HepG2, SK-MEL-1, HT018, HeLa, and MDA-MB 231, and compared with the standard drug, cisplatin. The results are quite promising against MDA-MB 231 (breast cancer cell line of 1), with an IC50 value that is nearly the same as the standard drug. Apoptosis was induced by complex 1 on MDA-MB 231 cells predominantly as studied by flow cytometry (FACS). The adhesion and migration of cancer cells were also examined upon treatment of complexes 1 and 2. Furthermore, the in vivo chronic toxicity profile of complexes 1 and 2 was also studied on all of the major organs of the mice, and found them to be less toxic. Thus, the results warrant further investigations of complex 1.

Published
2018

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