Isatin (1H-indole-2,3-dione) was reported to possess anticancer activities through its effect on tumor proliferation, apoptosis, and metastasis in vitro and in vivo. Here, we described the synthesis of a novel series of 1,5-disubstituted isatin derivatives with 2-indolinone scaffold as antitumor agents. Most of the synthesized compounds revealed potent antiproliferative effects in mantle cell lymphoma (MCL) cell lines, among which 7l possessed promising activities with IC₅₀ values ranging from 0.4 to 1.3 μM. Following flow cytometric analysis, compound 7l efficiently arrested the cell cycle at G2/M phase, and induced apoptosis. Thus, this study shows promise in therapeutics of 1,5-disubstituted isatin derivatives in MCL and provides novel potential and efficient antitumor agents.

据报道，Isatin（1 H-吲哚-2,3-dione）通过在体内外对肿瘤的增殖，凋亡和转移具有抗癌活性。在这里，我们描述了以2-吲哚满酮骨架为抗肿瘤剂的一系列新的1，5-二取代的靛红衍生物的合成。大多数合成的化合物在套细胞淋巴瘤（MCL）细胞系中显示出有效的抗增殖作用，其中7l具有有希望的活性，IC ₅₀值在0.4至1.3μM之间。流式细胞分析后，化合物7l有效地将细胞周期阻滞在G2 / M期，并诱导凋亡。因此，这项研究显示了在MCL中治疗1,5-二取代的靛红衍生物的前景，并提供了新的潜在和有效的抗肿瘤药。