Gao Zilin, Chen Yu, Nie Yufei, Chen Keming, Cao Xiufang, Ke Shaoyong
College of Science, Huazhong Agricultural University, Wuhan, China.
National Biopesticide Engineering Research Centre, Hubei Biopesticide Engineering Research Centre, Hubei Academy of Agricultural Sciences, Wuhan, China.
Front Chem. 2023 Jan 18;11:1104868. doi: 10.3389/fchem.2023.1104868. eCollection 2023.
Carbazole alkaloids, as an important class of natural products, have been widely reported to have extensive biological activities. Based on our previous three-component reaction to construct carbazole scaffolds, we introduced a methylene group to provide a rotatable bond, and designed series of carbazole derivatives with structural diversity including carbazole amide, carbazole hydrazide and carbazole hydrazone. All synthesized carbazole derivatives were evaluated for their cytotoxic activity against 7901 (gastric adenocarcinoma), A875 (human melanoma) and MARC145 (African green monkey kidney) cell lines. The preliminary results indicated that compound exhibited high inhibitory activities on 7901 and A875 cancer cells with the lowest IC of 11.8 ± 1.26 and 9.77 ± 8.32 μM, respectively, which might be the new lead compound for discovery of novel carbazole-type anticancer agents.
咔唑生物碱作为一类重要的天然产物，已有广泛报道表明其具有多种生物活性。基于我们之前构建咔唑骨架的三组分反应，我们引入了一个亚甲基以提供一个可旋转键，并设计了一系列具有结构多样性的咔唑衍生物，包括咔唑酰胺、咔唑酰肼和咔唑腙。对所有合成的咔唑衍生物针对7901（胃腺癌）、A875（人黑色素瘤）和MARC145（非洲绿猴肾）细胞系进行了细胞毒性活性评估。初步结果表明，该化合物对7901和A875癌细胞表现出高抑制活性，最低IC分别为11.8±1.26和9.77±8.32 μM，这可能是发现新型咔唑类抗癌药物的新先导化合物。
