Synthesis of a series of new sulfonamide substituted isoindolo[2,1-a]quinazoline-6,12-dione derivatives and evaluation of their biological activity

Cancer and inflammatory diseases constitute two major public health concerns. Although radiotherapy and surgery are considered for the treatment of cancer cases, chemotherapy remains the most effective therapeutic strategy. However, because of its side effects, there is still an urgent need for the generation of more selective novel synthetic or natural bioactive molecules. Inflammation is a biological response for tissue damage and activities pathways that are involved in tissue repair. Chronic inflammation results from simultaneous and prolonged tissue destruction and repair and is often related to an infection. In diseases caused by chronic inflammation, as TNF-α immunomodulator is overproduced, the therapeutic strategy consists of using molecules that regulate the TNF-α levels. Moreover, since in chronic inflammative tissues, cells are repeatedly exposed to high levels of reactive oxygen and nitrogen species, there are many studies that suggest that their DNA is consequently damaged which results in cancer development. In this research, sulfonamide substituted isoindolo[2,1-a]quinazoline derivatives were synthesized via molecular hybridization, to develop new structures that can potentially show both anti-inflammatory and anticancer activity. Eleven new sulfonamide substituted isoindoloquinazoline were thus obtained. Their structure was elucidated via spectral analyses and the compounds were evaluated for their biological activity.