Selenium-containing naphthalimides as anticancer agents: design, synthesis and bioactivity

Area of Science:

• Medicinal Chemistry
• Organic Chemistry
• Pharmacology

Background:

• Sulfur-containing compounds are known for their biological activities.
• Exploring selenium analogues can lead to novel therapeutic agents.
• Organochalcogen compounds offer unique chemical properties for drug development.

Purpose of the Study:

• To synthesize novel selenium analogues of known sulfur compounds.
• To evaluate the anticancer activities of these synthesized compounds.
• To investigate the DNA-binding interactions of selected analogues.

Main Methods:

• Synthesis of selenium analogues (compounds 4b-4h, and 4j).
• Anticancer activity screening using IC(50) values against various cancer cell lines.
• DNA-binding studies using techniques to determine binding constants (K(b)).

Main Results:

• Most synthesized compounds exhibited moderate anticancer activities with IC(50) values in the 10(-6) to 10(-5) M range.
• Selenium compound 4b showed activity comparable to its sulfur analogue 4a, with similar DNA interaction.
• Selenium analogue 4j displayed the highest potency, with IC(50) values around 5.3 μM against K562 and MCF-7 cells.
• Organochalcogen compounds demonstrated enhanced anticancer effects against the K562 cell line compared to other tested cell lines.

Conclusions:

• Selenium analogues of sulfur compounds possess significant anticancer potential.
• Compound 4j is a promising candidate for further investigation as an anticancer agent.
• The K562 cell line appears particularly sensitive to the tested organochalcogen compounds.