The present invention provides a series of novel indeno[1,2-c]quinolin-11-one derivatives, and further provides a preparation method of those derivatives and their applications. The applications comprise uses of those derivatives as medicinal compositions to cure cancer, and comprise uses of the abilities of those derivatives to obviously inhibit the growth of cancer cells and to inhibit the activity of the first type topoisomerase, and thereby curing cancer.本發明係提供一系列新穎茚并[1,2-c]喹啉-11-酮衍生物,並進一步提供該些衍生物之製備方法及其應用,該應用包含將該類衍生物作為治療癌症之醫藥組合物,且其應用包含該類衍生物具有明顯抑制癌細胞生長的能力、抑制第一型拓樸異構酶的活性,進而治療癌症等功效。