Synthetic Strategies for Some Carborane Analogues of Coumarins with Anticancer Activity
Session
Pharmaceutical and Natural Sciences
Description
The intense investigation in medicinal chemistry showed that many of the coumarin derivatives with expressed anticoagulant activity, are showing anticancer effects in the same time. Thus, very known and commercially available medicaments as Warfarin, Phenprocoumon, Sintrom (acenocoumarol) and Bromadiolone are intensively studied for their cytostatic, apoptotic and antiproliferative activities. On the other hand, recently, carborane clusters that can be regarded as phenyl mimics have attracted attention. Most boranes are not very suitable for biological applications due to instability; however, carboranes, where two BH- units of closo-B12 H12 2- are formally substituted by two CH fragments, had shown remarkable biological stability. Thus, many compounds containing carboranes as pharmacophore have received much attention in the last decade, especially in the search of novel effective chemotherapeutic agents. Taking into consideration that many flavonoids and their constitutional isomers, coumarins, have shown noticeable anticancer properties, it was planned to synthesize novel compounds by replacing the aromatic ring of some of their derivatives by a carborane cluster to enhanced metabolic stability as well as enhanced hydrophobicity. Many strategies were employed in order to synthetize the desired carborane analogues of Warfarin and the other coumarin derivatives but only few of them were fully applicable due to the complex steps into the retrosynthetic strategies.
Keywords:
Synthesis, Carborane analogues, Coumarin derivatives, Anticancer activity.
Proceedings Editor
Edmond Hajrizi
ISBN
978-9951-982-15-3
Location
UBT Kampus, Lipjan
Start Date
25-10-2024 9:00 AM
End Date
27-10-2024 6:00 PM
DOI
10.33107/ubt-ic.2024.156
Recommended Citation
Jashari, Ahmed and Hawkins, Eva Maria Hey, "Synthetic Strategies for Some Carborane Analogues of Coumarins with Anticancer Activity" (2024). UBT International Conference. 1.
https://knowledgecenter.ubt-uni.net/conference/2024UBTIC/PNS/1
Synthetic Strategies for Some Carborane Analogues of Coumarins with Anticancer Activity
UBT Kampus, Lipjan
The intense investigation in medicinal chemistry showed that many of the coumarin derivatives with expressed anticoagulant activity, are showing anticancer effects in the same time. Thus, very known and commercially available medicaments as Warfarin, Phenprocoumon, Sintrom (acenocoumarol) and Bromadiolone are intensively studied for their cytostatic, apoptotic and antiproliferative activities. On the other hand, recently, carborane clusters that can be regarded as phenyl mimics have attracted attention. Most boranes are not very suitable for biological applications due to instability; however, carboranes, where two BH- units of closo-B12 H12 2- are formally substituted by two CH fragments, had shown remarkable biological stability. Thus, many compounds containing carboranes as pharmacophore have received much attention in the last decade, especially in the search of novel effective chemotherapeutic agents. Taking into consideration that many flavonoids and their constitutional isomers, coumarins, have shown noticeable anticancer properties, it was planned to synthesize novel compounds by replacing the aromatic ring of some of their derivatives by a carborane cluster to enhanced metabolic stability as well as enhanced hydrophobicity. Many strategies were employed in order to synthetize the desired carborane analogues of Warfarin and the other coumarin derivatives but only few of them were fully applicable due to the complex steps into the retrosynthetic strategies.