通过微波辅助多组分多米诺反应合成新型有效细胞毒性鬼臼毒素-萘醌化合物。
Synthesis of novel potent cytotoxicy podophyllotoxin-naphthoquinone compounds via microwave-assited multicomponent domino reactions.
机构信息
Institute of Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam; Graduate University of Science and Technology, VAST, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
Institute of Chemistry, Vietnam Academy of Science and Technology (VAST), 18 Hoang Quoc Viet, Cau Giay, Hanoi, Viet Nam.
出版信息
Bioorg Med Chem Lett. 2021 Apr 1;37:127841. doi: 10.1016/j.bmcl.2021.127841. Epub 2021 Feb 5.
A series of novel podophyllotoxin-naphthoquinone compounds 5a-p were synthesized in good yields using microwave-assisted four-component reactions of 2-hydroxy-1,4-naphthoquinone, aromatic benzaldehydes, tetronic acid and ammonium acetate. All the synthesized compounds were fully characterized by spectral data and evaluated for their cytotoxicity activities against KB, HepG2, Lu1, MCF7, and non-cancerous Hek-293 cell lines. Among 16 new compounds screened, compounds 5a, 5d, 5h, and 5k displayed high potent inhibitory activities with IC < 40 nM against HepG2 and SK-Lu-1 cell lines, and showed lower toxicity for non-cancerous Hek-293 cell line, demonstrating the potential importance of these compounds in the development of potential anticancer agents.
采用微波辅助的四组分反应，以 2-羟基-1,4-萘醌、芳香苯甲醛、四氢呋喃酸和醋酸铵为原料，高产率地合成了一系列新型鬼臼毒素-萘醌类化合物 5a-p。所有合成的化合物均通过光谱数据进行了充分表征，并对其对 KB、HepG2、Lu1、MCF7 和非癌细胞系 Hek-293 的细胞毒性活性进行了评价。在所筛选的 16 种新化合物中，化合物 5a、5d、5h 和 5k 对 HepG2 和 SK-Lu-1 细胞系表现出高抑制活性，IC < 40 nM，对非癌细胞系 Hek-293 的毒性较低，表明这些化合物在开发潜在的抗癌药物方面具有重要意义。
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