JOURNAL 2322
Bioorganic and Medicinal Chemistry Reports
Year: 2022 Issue: 1 January-June
p.1 - 8
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Ronak Haj Ersan
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Kajeen Hassan Jasim
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Haytham Sabeeh
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Knar Ahmed
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Darya Abdulsatar
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Shana Ali
GRAPHICAL ABSTRACT
ABSTRACT
Compounds bearing naphthalene and benzimidazole pharmacophores have been reported to possess excellent anticancer activity. In view of this, we designed, synthesized and characterized a series of naphthalene substituted benzimidazole derivatives (11–19), and further evaluated them for antiproliferative activities by employing MTT method. Among the nine investigated molecules, compounds (11 and 13) showed good antiproliferation of the tested cancer cell lines with IC50 values ranging from 0.078 to 0.625 µM. In addition, compound (18) exhibited selective cytotoxicity against HepG2 cell lines with high safety to normal cell (HEK293). Furthermore, cytotoxicity studies of these compounds against normal Human embryonic kidney cells (HEK293) revealed that the target molecules were less selective against HEK293 as compared to methotrexate (positive control). The high potency and selective cytotoxicity suggested that compound 18 could be a starting point for further optimization to develop novel antitumor agents towards liver cancer.
KEYWORDS- Benzimidazole
- naphthalene
- anticancer
- liver cancer
