Affiliations 

  • 1 Department of Chemistry, University of Agriculture Faisalabad-38040, Faisalabad, Pakistan
  • 2 School of Chemical Science, Universiti Sains Malaysia, 11800, Penang, Malaysia
  • 3 Department of Chemistry, University of Agriculture Faisalabad-38040, Faisalabad, Pakistan. adnan.iqbal@uaf.edu.pk
  • 4 EMAN Biodiscoveries Sdn. Bhd., A1-4, Lot 5, Persiaran 2/1, Kedah Halal Park, Kawasan Perindustrian Sungai Petani, 08000, Sungai Petani, Kedah, Malaysia
  • 5 Department of Pharmacology, School of Pharmaceutical Sciences, Universiti Sains Malaysia, 11800, Minden, Pulau Penang, Malaysia
Appl Biochem Biotechnol, 2020 Jul;191(3):1171-1189.
PMID: 32002729 DOI: 10.1007/s12010-019-03186-9

Abstract

Synthesis and anticancer studies of three symmetrically and non-symmetrically substituted silver(I)-N-Heterocyclic carbene complexes of type [(NHC)2-Ag]PF6 (7-9) and their respective (ligands) benzimidazolium salts (4-6) are described herein. Compound 5 and Ag-NHC-complex 7 were characterized by the single crystal X-ray diffraction technique. Structural studies for 7 showed that the silver(I) center has linear C-Ag-C coordination geometry (180.00(10)o). Other azolium and Ag-NHC analogues were confirmed by H1 and C13-NMR spectroscopy. The synthesized analogues were biologically characterized for in vitro anticancer activity against three cancer cell lines including human colorectal cancer (HCT 116), breast cancer (MCF-7), and erythromyeloblastoid leukemia (K-562) cell lines and in terms of in vivo acute oral toxicity (IAOT) in view of agility and body weight of female rats. In vitro anticancer activity showed the values of IC50 in range 0.31-17.9 μM in case of K-562 and HCT-116 cancer cell lines and 15.1-35.2 μM in case of MCF-7 while taking commercially known anticancer agents 5-fluorouracil, tamoxifen, and betulinic acid which have IC50 values 5.2, 5.5, and 17.0 μM, respectively. In vivo study revealed vigor and agility of all test animals which explores the biocompatibility and non-toxicity of the test analogues.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.