Abstract
Cancer is a complex disease which involves abnormalities of multiple cellular pathways. Current chemotherapeutic drugs are mainly designed to target the DNA and cell division. Therefore, in the present study, we have synthesized a new series of 1,2,3-triazolo-naphthalimide/phthalimide conjugates and evaluated their in vitro cytotoxicity against selected human cancer cells. Among the tested compounds, one of them displayed notable cytotoxic activity against A549 lung cancer cells with an IC50 (half maximal inhibitory concentration) value of 7.6 ± 0.78 µM. To determine the effect of this compound on cell viability, acridine orange/ethidium bromide (AO/EB) and 4',6-diamidino-2-phenylindole (DAPI) staining studies were performed. These apoptotic features were clearly indicating that the compound inhibited cell proliferation by apoptosis. Further, relative viscosity measurements and molecular docking studies with the most three active compounds indicated that these new compounds bind to DNA by intercalation.
Highlights
Cancer is considered as one of the lethal diseases worldwide and the incidence of cancer has been rising in major regions of the world with predicted substantive increase to 19.3 million by the year 2025.1 the scientific advances focused on finding exact pathophysiology of the disease and tremendous efforts have been made on early detection of cancer, the overall mortality rate has not declined.[2]
The syntheses of 1,2,3-triazole based naphthalimide/ phthalimide conjugates 6a-x, and 7a-c have been achieved by a two-step reaction as depicted in Scheme 1
In the presence of sodium azide, naphthalimide and phthalimide azides are formed in situ from N-alkylated naphthalimides and phthalimides, respectively
Summary
Cancer is considered as one of the lethal diseases worldwide and the incidence of cancer has been rising in major regions of the world with predicted substantive increase to 19.3 million by the year 2025.1 the scientific advances focused on finding exact pathophysiology of the disease and tremendous efforts have been made on early detection of cancer, the overall mortality rate has not declined.[2]. Prompted by the above reports, in the present study we have designed and synthesized a library of 1,2,3-triazolo based naphthalimide/phthalimide conjugates and evaluated their in vitro cytotoxicity and DNA intercalating capabilities. Soc. sodium azide and alkynes for the regioselective synthesis of 1,4-disubstituted 1,2,3-triazoles in water.[24] we have applied this efficient protocol for the synthesis of a variety of diversely substituted 1,2,3-triazolo-naphthalimide/ phthalimide conjugates.
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