Libraries of spiro[cyclopropane-1,3′-indolin]-2′-ones were synthesized and evaluated for their biological activity against five different human cancer cell lines HT-29 (colon cancer), DU-145 (prostate cancer), Hela (cervical cancer), A-549 (Lung cancer), and MCF-7 (breast cancer). Many compounds of the series exhibited promising anticancer activity (IC₅₀ <20 μM) against the studied cell lines. Based on the screening results, a structure activity relationship (SAR) of the pharmacophore was proposed. Among the series compound 6b and 6u showed significant activity against human prostate cancer cell line, DU-145. Flow cytometric analysis showed that these two compounds arrested the cell cycle in the G0/G1 phase leading to caspase-3 dependent apoptotic cell death. Further, measurement of mitochondrial membrane potential and Annexin V-FITC assay also suggested that 6b and 6u induced cell death by apoptosis.

合成了螺[cyclopropane-1,3'-吲哚啉] -2'-的文库，并评估了其对五种不同的人类癌细胞系HT-29（结肠癌），DU-145（前列腺癌），Hela的生物学活性（子宫颈癌），A-549（肺癌）和MCF-7（乳腺癌）。该系列的许多化合物 对所研究的细胞系均显示出有希望的抗癌活性（IC ₅₀ <20μM）。根据筛选结果，提出了药效基团的结构活性关系（SAR）。在系列化合物6b和6u中对人前列腺癌细胞系DU-145表现出显着的活性。流式细胞仪分析表明，这两种化合物将细胞周期阻滞在G0 / G1期，导致caspase-3依赖性凋亡细胞死亡。此外，线粒体膜电位的测定和膜联蛋白V-FITC测定还表明6b和6u通过凋亡诱导细胞死亡。