Title

Synthesis, Characterization, and Topoisomerase Studies with a Novel Cobalt(III) Complex Coordinated by an Aromatic Bidentate Ligand and a Thiosemicarbazone

Presenting Author Name/s

Delvin Askew

Faculty Advisor

Alvin A. Holder

Presentation Type

Poster

Disciplines

Chemistry | Inorganic Chemistry | Medicinal-Pharmaceutical Chemistry

Description/Abstract

The need for novel antibiotic drugs is urgent. Tuberculosis (TB) is one of the top ten leading causes of death worldwide, with 1.8 million deaths per year, and the number one killer of people who are HIV-positive. As the war against bacterial pathogens continues, finding novel drugs and drug targets is essential.

Topoisomerase IA is a novel and attractive drug target because it has never yet been targeted by antibiotics used clinically. Over the years, cisplatin and its analogues have been used as anti-cancer agents, but other non-platinum metal complexes (e.g., those with copper(II), ruthenium(II), ruthenium(III), vanadium(IV) metal centers, etc.) have been reported to be used in anti-cancer therapy, but not many have been used as antibacterial agents. Interestingly, biomedically relevant cobalt-containing compounds have provided promising results as antibacterial agents.

In our contribution to the fight against bacterial infection, a novel cobalt(III) complex, [Co(phen)2(MeATSC)](NO3)3·2.5H2O·C2H5OH 1 (where phen = 1,10-phenanthroline and MeATSC = 9-anthraldehyde-N(4)-methylthiosemicarbazone) was synthesized, characterized; then anti-cancer studies were carried out to ascertain its antitumor potential. Elemental analysis, FTIR spectroscopy, 1H, 13C, and 59Co NMR spectroscopy, and high resolution electrospray ionization mass spectroscopy were used to determine the structure of complex 1.

In this study, complex 1 was tested for inhibition of bacterial topoisomerase I as well as antibacterial activities. Complex 1 was a very potent topoisomerase I inhibitor that showed an IC50 against MtbTopI and EcTopI of 0.8 µM. Complex 1 was able to prevent the growth of M. smegmatis, as well as methicillin-resistant Staphylococcus aureus.

Session Title

Poster Session

Location

Learning Commons @ Perry Library, Northwest Atrium

Start Date

2-2-2019 8:00 AM

End Date

2-2-2019 12:30 PM

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Feb 2nd, 8:00 AM Feb 2nd, 12:30 PM

Synthesis, Characterization, and Topoisomerase Studies with a Novel Cobalt(III) Complex Coordinated by an Aromatic Bidentate Ligand and a Thiosemicarbazone

Learning Commons @ Perry Library, Northwest Atrium

The need for novel antibiotic drugs is urgent. Tuberculosis (TB) is one of the top ten leading causes of death worldwide, with 1.8 million deaths per year, and the number one killer of people who are HIV-positive. As the war against bacterial pathogens continues, finding novel drugs and drug targets is essential.

Topoisomerase IA is a novel and attractive drug target because it has never yet been targeted by antibiotics used clinically. Over the years, cisplatin and its analogues have been used as anti-cancer agents, but other non-platinum metal complexes (e.g., those with copper(II), ruthenium(II), ruthenium(III), vanadium(IV) metal centers, etc.) have been reported to be used in anti-cancer therapy, but not many have been used as antibacterial agents. Interestingly, biomedically relevant cobalt-containing compounds have provided promising results as antibacterial agents.

In our contribution to the fight against bacterial infection, a novel cobalt(III) complex, [Co(phen)2(MeATSC)](NO3)3·2.5H2O·C2H5OH 1 (where phen = 1,10-phenanthroline and MeATSC = 9-anthraldehyde-N(4)-methylthiosemicarbazone) was synthesized, characterized; then anti-cancer studies were carried out to ascertain its antitumor potential. Elemental analysis, FTIR spectroscopy, 1H, 13C, and 59Co NMR spectroscopy, and high resolution electrospray ionization mass spectroscopy were used to determine the structure of complex 1.

In this study, complex 1 was tested for inhibition of bacterial topoisomerase I as well as antibacterial activities. Complex 1 was a very potent topoisomerase I inhibitor that showed an IC50 against MtbTopI and EcTopI of 0.8 µM. Complex 1 was able to prevent the growth of M. smegmatis, as well as methicillin-resistant Staphylococcus aureus.