Title:Synthetic Approaches and Pharmacological Attributes of Benzosuberone
Skeleton
Volume: 23
Issue: 1
Author(s): Syed Nasir Abbas Bukhari*
Affiliation:
- Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka, Aljouf 2014, Saudi Arabia
Keywords:
Structural modifications, human cancer cell lines, anti-tumor, anti-malarial, anti-inflammatory, anti-tubercular.
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.
