Anticancer activity of novel silicon phthalocyanines against colorectal adenocarcinoma cell line (DLD-1)

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Farajzadeh N., Kuşçulu N., Yenilmez H. Y., Bahar D., Bayır Z.

NEW JOURNAL OF CHEMISTRY, vol.1, no.1, pp.5-20, 2022 (SCI-Expanded)

  • Publication Type: Article / Article
  • Volume: 1 Issue: 1
  • Publication Date: 2022
  • Doi Number: 10.1039/d2nj02891c
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED)
  • Page Numbers: pp.5-20
  • Kayseri University Affiliated: Yes


In this study, the DNA cleavage activities of a series of new silicon phthalocyanines were studied to measure their potential
for cancer treatment. For this purpose, 2-(2,4,6-tris((dimethylamino)methyl)phenoxy)ethan-1-ol (2) and 2-(2-(2,4,6-
tris((dimethylamino)methyl)phenoxy)ethoxy)ethan-1-ol (3) were synthesized and used for the preparation of axially disubstituted
silicon phthalocyanines. The resulting phthalocyanines were quaternized in the presence of iodomethane.
Characterization of all the newly synthesized compounds was carried out using several spectroscopic approaches including
mass, UV-vis, FT-IR, and NMR spectroscopies. Plasmid DNA (pBR322) cleavage, topoisomerase enzyme activity and binding
situation with calf thymus DNA (CT-DNA) of the new silicon phthalocyanines were measured using agarose gel
electrophoresis assay. 1-QSi exhibited remarkable cleavage activities on supercoiled plasmid DNA at all the studied
concentrations. Compound 3-QSi displayed significant cleavage activities on supercoiled plasmid DNA only at 200 μg/mL.
Besides, compound 3-QSi exhibited higher human topoisomerase I inhibition activity compared to compound 2-QSi.
Moreover, all the compounds were screened for biological activities. The cytotoxicity and apoptosis activities effects were
test against DLD-1 colorectal cancer cell line were studied at different concentrations ranging from 6.25 to 100 μg/mL. The
results indicated that the studied compounds can be utilized as anticarcinogenic agents