The aim of the study was the synthesis of novel platinum compounds
having benzimidazole ligands and screening for their in vitro cytotoxic
activity on human cervical carcinoma HeLa, human lung carcinoma
A549, and human lung epithelial Beas-2B cell lines. 2-Substituted
benzimidazole ligands were synthesized by using appropriate
aldehydes and o-phenylenediamine. Subsequently, 2-substituted
benzimidazole ligands and potassium tetrachloroplatinate(II)
(K2PtCl4) were used to synthesize 2-isopropylbenzimidazole
tetrachloroplatinate(II) (K1) and 2-(1-methylpropyl)benzimidazole
tetrachloroplatinate(II) monohydrate (K2). HRMS, IR, elemental
analysis, 1H-NMR, and melting point were used to characterize
the synthesized compounds. Cytotoxic activities against HeLa,
A549, and Beas-2B cells after 48 h and 72 h incubation of the
platinum compounds were investigated via MTT assay. Cisplatin
and carboplatin were used as reference drugs. The cytotoxic activity
results showed that K2 platinum compound displayed 53.42%±2.21
(at 160 μM) on HeLa, 88.16%±0.22 (at 160 μM) on A549 and
92.09%±0.57 (at 160 μM) on Beas-2B after 48 h incubation, K2
displayed 27.42%±2.03 (at 160 μM) on HeLa, 93.95%±0.53
(at 160 μM) on A549 and 91.99±0.22 (at 160 μM) on Beas-2B
after 72 h incubation. Both of the platinum compounds have higher
cell inhibitory effects than reference drug carboplatin after 48 h incubation for tested cells.
Primary Language | English |
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Subjects | Pharmacology and Pharmaceutical Sciences |
Journal Section | Research Article |
Authors | |
Publication Date | October 19, 2022 |
Submission Date | April 9, 2022 |
Published in Issue | Year 2022 Volume: 47 Issue: 3 |