Results in Chemistry (Jun 2024)
Linearly ring-fused coumarins: A review of their cancer-fighting attributes
Abstract
Despite the up-to-date advancements in its treatment, cancer is still being harvested the lives of millions of people annually; this health threat necessitates exploring more potent agents that can effectively fight it. The class of heterocycles known as coumarin, and its natural and synthetic derivatives are thought to be biomedically valuable. Coumarins have low side effects, outstanding selectivity, a straightforward design for maximum efficiency, and various pharmacological actions. For these characteristics, coumarins are continuously isolated from natural sources and synthesized in laboratories, alongside with examining them for possible bioactivities. In addition to garnering significant attention, coumarin has emerged as a valuable scaffold and a potentially important precursor in the development of innovative anticancer medicines. Researchers are working to create new cancer-fighting coumarins, as well as investigating the old ones. Integration two or more cyclic moieties into a single molecular framework might enhance existing pharmacological effects or perhaps provide entirely new ones. Numerous studies have shown a synergistic or additive impact when various heterocycles are fused with coumarin, where the fusion may occur at coumarin-benzene or coumarin-lactone. The current paper explores in detail how linearly ring-fused coumarins can combat cancer. The derivative with the number 42 was determined to be the best among the fused coumarins that were reviewed. Compared with 5-flourouracil, the IC50 values of 42 against six cancer cell lines are promising. These values are 25.08, 13.42, 41.45, 28.43, 31.15, and 13.08 μM against SK-OV-3, HeLa, KYSE-30, AMN3, SKG, and MCF-7, respectively. The cancer-fighting attribute of 42 was obvious when compared with those of the reference, which has the following IC50 values in the same order of cancer cell lines: 22.43, 13.37, 30.72, 24.89, 22.12, and 12.42 μM. The researchers conducted searches across multiple data repositories, such as Scopus, Google Scholar, Web of Science, and PubMed. After conducting a thorough analysis, the authors found and included 59 pertinent publications published by the end of 2023. The reviewed data may help medicinal chemists create and manufacture functionally active leads using the scaffolds that have been mentioned. The knowledge derived from this data may offer substantial medical benefits in the short term for the development of powerful drugs that could boost cancer chemotherapeutics.
