Aromatic Ring Substituted Aaptamine Analogues as Potential Cytotoxic Agents against Extranodal Natural Killer/T-Cell Lymphoma,Journal of Natural Products

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Aromatic Ring Substituted Aaptamine Analogues as Potential Cytotoxic Agents against Extranodal Natural Killer/T-Cell Lymphoma
Journal of Natural Products ( IF 3.3 ) Pub Date : 2020-11-10 , DOI: 10.1021/acs.jnatprod.0c00769
Fan Yang ₁ , Yuan Gao ₁ , Yung-Ting Chang ₁ , Yike Zou ₂ , K N Houk ₂ , Jing-Rong Lu ₁ , Jing He ₁ , Wei-Zhuo Tang ₃ , Hong-Ze Liao ₁ , Hua Han ₄ , Hou-Wen Lin ₁

Affiliation

A chemical modification study was conducted on the marine natural product aaptamine (1), isolated from the marine sponge Aaptos aaptos. Thirty new derivatives substituted by various aromatic rings at the 3- and 7-positions of aaptamine were prepared by bromination, followed by the Suzuki coupling reaction. Sixteen compounds displayed cytotoxicities to four cancer cell lines (IC₅₀ < 10 μM). In particular, compound 5i demonstrated a significant antiproliferative effect on the extranodal natural killer/T-cell lymphoma (ENKT) cell line SNK-6 with an IC₅₀ value of 0.6 μM. Additionally, compound 5i showed cytotoxicities to multiple lymphoma cell lines, including Ramos, Raji, WSU-DLCL2, and SU-DHL-4 cells.

中文翻译：

芳香环取代的 Aaptamine 类似物作为潜在的细胞毒性剂对抗结外自然杀伤/T 细胞淋巴瘤

对从海洋海绵Aaptos aaptos 中分离的海洋天然产物 aaptamine ( 1 )进行了化学改性研究。通过溴化和 Suzuki 偶联反应制备了 30 种在 aaptamine 的 3-和 7-位被各种芳环取代的新衍生物。16 种化合物对四种癌细胞系显示出细胞毒性 (IC ₅₀ < 10 μM)。特别是，化合物5i对结外自然杀伤/T 细胞淋巴瘤 (ENKT) 细胞系 SNK-6 显示出显着的抗增殖作用，IC ₅₀值为 0.6 μM。此外，化合物5i 对多种淋巴瘤细胞系显示出细胞毒性，包括 Ramos、Raji、WSU-DLCL2 和 SU-DHL-4 细胞。

更新日期：2020-12-24

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