Novel carboranyl-BODIPY conjugates: design, synthesis and anti-cancer activity

Area of Science:

• Organic Chemistry
• Medicinal Chemistry
• Cancer Research

Background:

• Boron clusters and BODIPY fluorophores are key components in developing novel therapeutic agents.
• Carboranyl-BODIPY conjugates combine the unique properties of boron clusters with the photophysical characteristics of BODIPY.

Purpose of the Study:

• To synthesize and characterize novel carboranyl-BODIPY and phenylene-BODIPY conjugates.
• To evaluate the in vitro cytotoxicity and anticancer potential of these synthesized compounds against the HeLa cervical cancer cell line.

Main Methods:

• Synthesis of carboranyl-BODIPY and phenylene-BODIPY conjugates.
• Characterization using NMR (1H, 13C, 11B, 19F), FT-IR, and high-resolution mass spectrometry.
• In vitro cytotoxicity assays and flow cytometry analysis on HeLa cells.

Main Results:

• The synthesized conjugates, including o-CB-10, m-CB-15, Me-o-CB-28, Me-o-CB-35, and PB-20, were successfully prepared and characterized.
• o-CB-10 exhibited significant cytotoxicity against HeLa cells at low concentrations (12.03 μM), inhibiting cell proliferation and migration.
• o-CB-10 and Me-o-CB-28 were found to arrest the cell cycle at the S phase.

Conclusions:

• Carboranyl-BODIPY conjugates demonstrate potential as effective anticancer agents.
• The compound o-CB-10 shows particular promise due to its potent cytotoxic effects and ability to inhibit cancer cell growth and movement.
• Further investigation into these carboranyl-BODIPY conjugates is warranted for their development as therapeutic drugs.