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Patent Application Number :- 2001/DEL/2014
Applicant Name :- Dr. RICHA KOTHARI
Date of Filing :- 16/7/ 2014
Title of Invention :- Process of Synthesis of Macrocyclic Copper (II) Complexes and their uuse there of as therapeutic Agents

ABSTRACT OF THE INVENTION

A novel divalent macrocyclic copper (II) complexes are disclosed. The divalent copper species are directly produced by the template method with a combination of carbohydrazone, tridentate thiosemicarbazide and copper (II_) salts. The divalent copper (II) complexes are characterized by elemental analysis, IR, 1HNMR, mass and electronic spectra. The magnetic moments and electronic spectral studies suggested distorted octahedral geometry for all the complexes. The monoanionic thiosemicarbazonate ligands act in a tridentate mode, binding through azomethine nitrogen and sulfur atom. Cytotoxic activity against human Breast Cancer Cell line MCF-7, antibacterial and antioxidant activities were evaluated for all the above compounds. Out of the six Cu (II) complexes, five showed cytotoxic activity against the studied cell line; presenting similar values of IC50 in the range 2-12 µM. The standard antibreast cancer drug Tamoxifen was used as a positive control. The synthesized compounds were screened for their in vitro antibacterial activity using Disc Diffusion method against two strains each of gram negative and gram positive bacteria. Tetracycline was used as positive control in the test. All the compounds showed remarkable antibacterial activity in the range of 2-10 mg/ml. Antioxidant activity of the six macrocyclic copper complexes was screened using the H2O2 scavenging assay. All six compounds showed potent antioxidant activity in the range 80-90%. The compounds would be evaluated further for their possible DNA binding, cleavage, antifungal and anti-diabetic activities.

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