Newly Constructed Cancer Drug – Carboranes

Carboranes have three main structural components: boron, carbon, and hydrogen. This compound doesn’t directly target cancer cells. Instead, they help work synergistically with other cancer drugs by making them bind more tightly to their respective targets, thus killing cancer cells. Thus carborane-conjugated or carborane-derived chemotherapeutic drugs may be useful clinically for enhancing the potency of existing cancer drugs.

Furthermore, carboranes derivatives selectively shut off energy reserves in cancer cells and inhibits the repair mechanism within these cells. In addition to these benefits, cancer drugs made up of carboranes also minimize side effects of cancer drugs and therapies and increases their effectiveness. An excerpt from a recent publication:


In this contribution, the specific interactions of carborane pharmacophore agents, namely carborane–carboxylic acid derivatives (denoted as Cbac1 and Cbac2), with cadmium telluride quantum dots capped with cysteamine (CA-CdTe QDs) are explored. The corresponding carborane–carboxylic acid derivatives–CdTe nanoconjugates exhibit synergistic inhibition on target cancer cells, raising the possibility of carborane anticancer agents in combination with safe-dosage QDs for cancer chemotherapy.

Research continues and medicinal scientists claim that in the near future, these carborane-based drugs could boost chemotherapy to thousands of times stronger than the clinical drugs used today. As a novel group of chemical structures, carboranes can be conjugated or modified chemically to enhance cytotoxicity. For example, Zhang et al. found complexing ruthenium with carboranes are effective anticancer agents in human lung cancer cell lines.

The ruthenium(II)-arene complex could significantly induce apoptosis in human lung cancer HCC827 cell line. Treatment of HCC827 cells with the ruthenium(II)-arene complex resulted in dose-dependent cell apoptosis as indicated by high cleaved Caspase-8,9 ratio. Besides ruthenium(II)-arene complex caused a rapid induction of cleaved Caspase-3 activity and stimulated proteolytic cleavage of poly-(ADP-ribose) polymerase (PARP) in vitro and in vivo. Our results suggest that ruthenium(II)-arene complex could be a candidate for further evaluation as a chemotherapeutic agent for human cancers, especially lung cancer.

Source 1, 2, 3

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