Highly potent anti-proliferative effects of a gallium(III) complex with 7-chloroquinoline thiosemicarbazone as a ligand: synthesis, cytotoxic and antimalarial evaluation

Kewal Kumar; Sarah Schniper; Antonio González-Sarrías; Alvin A Holder; Natalie Sanders; David Sullivan; William L Jarrett; Krystyn Davis; Fengwei Bai; Navindra P Seeram; Vipan Kumar

doi:10.1016/j.ejmech.2014.08.054

Highly potent anti-proliferative effects of a gallium(III) complex with 7-chloroquinoline thiosemicarbazone as a ligand: synthesis, cytotoxic and antimalarial evaluation

Eur J Med Chem. 2014 Oct 30:86:81-6. doi: 10.1016/j.ejmech.2014.08.054. Epub 2014 Aug 16.

Authors

Affiliations

¹ Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
² Department of Chemistry and Biochemistry, The University of Southern Mississippi, 118 College Drive, # 5043, Hattiesburg, MS 39406-0001, USA.
³ Bioactive Botanical Research Laboratory, Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI 02881, USA.
⁴ Department of Chemistry and Biochemistry, Old Dominion University, 4541 Hampton Boulevard, Norfolk, VA 23529-0126, USA.
⁵ W. Harry Feinstone Department of Molecular Microbiology and Immunology, Bloomberg School of Public Health, The Johns Hopkins University, Baltimore, MD, 21205, USA.
⁶ School of Polymers and High-Performance Materials, The University of Southern Mississippi, 118 College Dive, #5050, Hattiesburg, MS 39406-0076, USA.
⁷ Department of Biological Sciences, The University of Southern Mississippi, 118 College Drive, # 5018, Hattiesburg, MS 39406-0001, USA.
⁸ Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India. Electronic address: vipan_org@yahoo.com.

PMID: 25147149
DOI: 10.1016/j.ejmech.2014.08.054

Abstract

A gallium(III) complex with 7-chloroquinoline thiosemicarbazone was synthesized and characterized. The complex proved to be thirty-one times more potent on colon cancer cell line, HCT-116, with considerably less cytotoxicity on non-cancerous colon fibroblast, CCD-18Co, when compared to etoposide. Its anti-malarial potential on 3D7 isolate of Plasmodium falciparum was better than lumefantrine.

Keywords: 7-Chloroquinoline thiosemicarbazone; Anti-plasmodial activity; Cytotoxic activity; Gallium(III) complex; Selectivity index.

Publication types

Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't

MeSH terms

Antimalarials / chemical synthesis
Antimalarials / chemistry
Antimalarials / pharmacology*
Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology
Caco-2 Cells
Cell Proliferation / drug effects
Cell Survival / drug effects
Cells, Cultured
Coordination Complexes / chemical synthesis
Coordination Complexes / chemistry
Coordination Complexes / pharmacology*
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Gallium / chemistry*
HCT116 Cells
HT29 Cells
Humans
Ligands
Molecular Structure
Parasitic Sensitivity Tests
Plasmodium falciparum / drug effects*
Structure-Activity Relationship

Substances

Antimalarials
Antineoplastic Agents
Coordination Complexes
Ligands
N1-(7-chloroquinolin-4-yl)-ethylamino-2-acetylpyridine thiosemicarbazone gallium(III) complex
Gallium

Grants and funding

RR0052/RR/NCRR NIH HHS/United States