Synthetic Approaches and Pharmacological Attributes of Benzosuberone Skeleton

Abstract

Background: Benzocycloheptanone is the main structural feature of numerous famous natural pharmacophores such as Colchicine and Theaflavins. It has gained popularity in the field of medicinal chemistry, attributing to its broad-spectrum effect.

Objective: Numerous research publications addressing the derivatization of the benzosuberone molecule have been published, and their biological and pharmacological features have been extensively addressed. Numerous derivatives have been discovered as lead compounds for the development of novel medications. Thus, the goal of this article is to summarize and analyze all published findings on the synthesis and biological assessment of the benzosuberone skeleton.

Methods: All main databases including SciFinder, PubMed and google scholar were used with appropriate keywords to select related reported literature, and further bibliography in related literature was also used to find linked reports.

Results: Synthetic routes to benzosuberone-based ring systems were identified from the literature and explained stepwise and after this, pharmacological activities of all benzosuberone derivatives are listed target-wise and a detailed structure-activity relationship is developed.

Conclusion: The current review discusses numerous synthetic approaches for the synthesis of benzosuberone skeleton and its applications in many domains of medical chemistry. Compounds possessing the benzosuberone skeleton play an important role in the drug development process due to their wide range of biological actions such as anti-cancer, antibacterial, antifungal, antiinflammatory, and so on. The results of antibacterial screening and Structure-Activity Relationship (SAR) revealed that the compounds containing this skeleton with the piperazine and morpholine rings have antimicrobial potential when compared to the commercial antibiotic Norfloxacin. Despite extensive study to date, there is still room for the development of novel and efficient pharmacophores using the structure-based drug design technique.

Keywords: Structural modifications; anti-inflammatory; anti-malarial; anti-tubercular; anti-tumor; human cancer cell lines.