10.1016/j.ejmech.2014.07.073
This research aimed to develop a "switch off/switch on" regulation of drug cytotoxicity for targeted cancer therapy by conjugating anticancer drugs to bi-nuclear amino acid platforms (MAAPs) through solid-phase organic synthesis (SPOS). The purpose was to enhance the therapeutic efficacy of multiple drugs linked to a single carrier molecule, potentially improving target cell specificity and reducing side effects. The researchers synthesized MAAPs loaded with various anticancer agents, including Azatoxin (AZA), Camptothecin (CAMP), Prednisone (PRED), Chlorambucil (CLB), and the 9-aminoacridine anticancer compound YG-42. They demonstrated that the cytotoxic activity of these drugs could be controlled by chemical modification and delivery, effectively "switching off" the activity when conjugated to the MAAP and "switching on" when delivered to target cancer cells via a cell-targeting peptide. The conclusions supported the versatility of this approach for constructing MAAPs with various drugs and linkages, showing high variability in bio-stability and drug release kinetics. This research paves the way for more sophisticated MAAPs bearing diverse chemotherapeutic "cocktails" for preclinical cancer therapy assessment.
10.1007/s12272-012-0504-1
This research aimed to synthesize rutaecarpine derivatives and evaluate their inhibitory activities against topoisomerase I and II, enzymes crucial in DNA replication and transcription. The study was driven by the potential of these alkaloids, isolated from Rutaceous plants, to serve as natural product-based cytotoxic agents. The researchers synthesized a series of rutaecarpine derivatives using methods such as Fischer indole synthesis, acetic anhydride-mediated condensation, and ozonolysis, involving chemicals like 2-amino-5-chlorobenzoic acid, piperidin-2-one, benzaldehyde, and phenylhydrazine-HCl. The conclusions drawn from the study were that among the tested compounds, 10-bromorutaecarpine and 3-chlororutaecarpine exhibited strong inhibitory activities against both topo I and II, with effects somewhat stronger than those of the reference drugs camptothecin (CPT) and etoposide. These findings suggest that these rutaecarpine derivatives could be potential candidates for further development as topoisomerase inhibitors for therapeutic applications.
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