N-(2-Methylphenyl)-9-oxo-9H-fluorene-1-carboxamide (2a) was identified as a novel apoptosis inducer through our caspase- and cell-based high-throughput screening assay. Compound 2a was found to be active with sub-micromolar potencies for both caspase induction and growth inhibition in T47D human breast cancer, HCT116 human colon cancer, and SNU398 hepatocellular carcinoma cancer cells. It arrested HCT116 cells in G₂/M followed by apoptosis as assayed by the flow cytometry. Structure–activity relationship (SAR) studies of the carboxamide group identified the lead compound N-(2-(1H-pyrazol-1-yl)phenyl)-9-oxo-9H-fluorene-1-carboxamide (6s). Compound 6s, with increased aqueous solubility, was found to retain the broad activity in the caspase activation assay and in the cell growth inhibition assay with sub-micromolar EC₅₀ and GI₅₀ values in T47D, HCT116, and SNU398 cells, respectively.

N-（2-甲基苯基）-9-氧代-9 H-芴-1-羧酰胺（2a）通过我们的基于半胱天冬酶和基于细胞的高通量筛选测定被鉴定为新型凋亡诱导剂。发现化合物2a具有亚微摩尔效能，在T47D人乳腺癌，HCT116人结肠癌和SNU398肝细胞癌细胞中对胱天蛋白酶的诱导和生长抑制均具有活性。如通过流式细胞术测定的，其将HCT116细胞阻滞在G ₂ / M中，随后凋亡。羧酰胺基团的结构-活性关系（SAR）研究确定了先导化合物N-（2-（1 H-吡唑-1-基）苯基）-9-氧代-9 H-芴-1-羧酰胺（6s）。发现具有增加的水溶性的化合物6s在半胱天冬酶激活测定和在T47D，HCT116和SNU398细胞中分别具有亚微摩尔EC ₅₀和GI ₅₀值的细胞生长抑制测定中保留了广泛的活性。