已经设计和合成了一系列新的二取代6-氮杂吲哚化合物，与类似的抗增殖活性化合物相比，这些化合物具有关键的结构改变。合成采用适当改变后的2-氨基-3-硝基-4-哌啶并转化为7-氯-3-碘-6-氮杂吲哚，并使用这种中心骨架进行了连续的Suzuki偶联反应，从而得到了目标化合物。通过对四种人类癌细胞系和正常人纤维母细胞株的细胞毒活性进行评估，发现某些化合物具有强烈的抗癌活性且不影响正常细胞。在抗癌细胞的亚细胞毒浓度下，这些化合物表现出抑制细胞周期G2/M期的抗增殖效应，这可能与观察到的MEK1-ERK1/2信号通路磷酸化水平下降和/或p53-p21WAF1轴的激活有关。 版权所有 © 2023 Elsevier Masson SAS. 保留所有权利。

A number of new disubstituted 6-azaindoles have been designed and synthesized bearing a crucial structural modification in respect to an analogous antiproliferative hit compound. The synthesis was performed using 2-amino-3-nitro-4-picoline, that was suitably modified and converted to 7-chloro-3-iodo-6-azaindole and this central scaffold was used for successive Suzuki-type couplings, to result in the target compounds. The evaluation of the cytotoxic activity was performed against four human cancer cell lines, as well as a normal human fibroblast strain. Certain compounds possessed strong anticancer activity without affecting normal cells. At subcytotoxic concentrations for cancer cells, these compounds displayed an anti-proliferative effect by arresting the cells at the G2/M phase of the cell cycle, which could be associated with the observed decrease in the phosphorylation levels of the MEK1- ERK1/2 pathway and/or the activation of the p53-p21WAF1 axis.Copyright © 2023 Elsevier Masson SAS. All rights reserved.