Synthesis and In Vitro Evaluation of Azole‐Based 1H Benzo(c)Isoxazole‐3‐one Derivatives for Antiproliferative and Immunomodulatory Activities

ABSTRACT Azoles represent a significant group of compounds used as nonsteroidal anti‐inflammatory drugs and have additionally demonstrated their potential in combating cancer. In this work, eight synthetic derivatives of 1H Benzo(c)isoxazole‐3‐one have been tested for their anticancer effects to develop them as candidate drugs for cancer. 1H Benzo(c)isoxazole‐3‐one was previously isolated from a marine bacterium, planococcus maritimus , which exhibited antiproliferative activity against proliferating PBMCs and a few cancerous cell lines. Eight derivatives were synthesized from the parent compound and the results represent the initial attempt to assess the antiproliferative effects of synthetic compounds on a cancerous cell line (HeLa) through the SRB assay and on mitogen‐induced using the MTT assay. All the compounds showed anticancer and anti‐inflammatory potential. Moreover, the results of in vitro DNA cleavage demonstrated that these compounds can be effective nucleases, as they completely degrade template DNA. In conclusion, the synthetic derivatives can be used as candidate drugs against cancer and inflammation.