In vitro anticancer activity of N-benzyl 1,10-phenanthroline derivatives on human cancer cell lines and their selectivity

Eti Nurwening Sholikhah(1*), Jumina Jumina(2), Sitarina Widyarini(3), Ruslin Hadanu(4), Mustofa Mustofa(5)

(1) Department of Pharmacology & Therapy, Faculty of Medicine, Public Health, and Nursing, Universitas Gadjah Mada, Jalan Farmako, Sekip Utara, Yogyakarta 55281, Indonesia
(2) Department of Chemistry, Faculty of Mathemathics and Natural Sciences, Universitas Gadjah Mada, Sekip Utara, Yogyakarta 55281, Indonesia
(3) Department of Pathology, Faculty of Veterinary Medicine, Universitas Gadjah Mada, Jl. Fauna No. 2, Karang Gayam, Caturtunggal, Depok, Sleman, Yogyakarta 55281, Indonesia
(4) Department of Chemistry Education, Faculty of Teacher Training and Education Science, Pattimura University, Jalan Ir. M. Putuhena, Poka Ambon, Maluku 97234, Indonesia; Department of Chemistry Education, Faculty of Teacher Training and Education Science, Sembilanbelas November Kolaka University, Jalan Pemuda No. 339, Kolaka, Sulawesi Tenggara 93517, Indonesia
(5) Department of Pharmacology & Therapy, Faculty of Medicine, Public Health, and Nursing, Universitas Gadjah Mada, Jalan Farmako, Sekip Utara, Yogyakarta 55281, Indonesia
(*) Corresponding Author


This research was conducted to evaluate the anticancer activity of new compounds of benzyl-1,10-phenanthroline derivatives and their selectivity. In vitro anticancer activity of 11 benzyl-1,10-phenanthroline derivatives were conducted on three human cancer cell lines, cervical cancer (HeLa), myeloma (NS-1), and breast cancer (MCF-7) using
MTT-based cytotoxicity assay. The cytotoxicity of each compound was assessed to normal Vero cell line by the same method. The in vitro anticancer activity and cytotoxicity was expressed by the concentration inhibiting 50% of the cell growth (IC50),
and the selectivity index (SI) was determined by calculating ratio of the IC50 on Vero cell line and the human cancer cell lines. The results showed that among the 11 compounds tested, the (1)-N-(4-butoxybenzyl)-1,10-phenanthrolinium bromide
exhibited the best in vitro anticancer activity with an IC50 27.602.76 μM on HeLa, 6.425.53 μM on NS-1 and 9.442.17 μM on MCF-7 cell lines. Its SI were 377.65 39.97 on HeLa, 6158.72 5306.34 on NS-1 and 1140.11 261.85 on MCF-7 cell lines. This study demonstrated that (1)-N-(4-butoxybenzyl)-1,10-phenanthrolinium bromide possessed a potential in vitro anticancer activity on cancer cell lines with high selectivity.


cytotoxicity; human cancer cell lines; in vitro anticancer activity; selectivity index


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