Synthesis, DNA binding, hemolysis assays and anticancer studies of copper(II), nickel(II) and iron(III) complexes of a pyrazoline-based ligand.
BACKGROUND
Over the last few decades, metal-based drugs, particularly cisplatin and its analogs have been used for the treatment of various cancers. Currently, scientists are developing other metal complexes as anticancer agents to eliminate the toxicity associated with platinum drugs.


RESULTS
Claisen-Schmidt condensation was used to synthesize the pyrazoline-based ligand; (5-(4-chlorophenyl)-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide), followed by the synthesis of its complexes with copper(II), nickel(II) and iron(III) metal ions. DNA binding and in silico studies indicated quite good binding with DNA; requirements for good anticancer drugs.


CONCLUSIONS
DNA binding constants for ligand, copper, nickel and iron complexes were 1.42 × 10(4), 3.16 × 10(4), 5.82 × 10(5) and 6.72 × 10(5) M(-1), respectively, indicating strong binding with DNA. All the reported compounds were slightly hemolytic towards rabbit red blood corpuscles and exhibited moderate activities against MCF-7 cancer cell lines.
Department of Chemistry, Jamia Millia Islamia (Central University), New Delhi 110025, India. saleem.kishwar@gmail.com
Kishwar
K
Saleem
Waseem A
WA
Wani
Ashanul
A
Haque
Mohamad Nadeem
MN
Lone
Ming-Fa
MF
Hsieh
Mohamad Aman
MA
Jairajpuri
Imran
I
Ali
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology; D045744:Cell Line, Tumor; D003300:Copper / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D004247:DNA / Q000378:metabolism*; D006461:Hemolysis / Q000187:drug effects / Q000235:genetics*; D006801:Humans; D058085:Iron Compounds / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology; D008024:Ligands; D061986:MCF-7 Cells; D009532:Nickel / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D011485:Protein Binding / Q000235:genetics; D011720:Pyrazoles / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology; D011817:Rabbits
D000970:Antineoplastic Agents; D058085:Iron Compounds; D008024:Ligands; D011720:Pyrazoles; D003300:Copper; D009532:Nickel; D004247:DNA