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Synthesis and antitumor activity of novel nitrogen mustard-linked chalcones

机译：新型氮芥连接的查耳酮的合成及其抗肿瘤活性

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摘要

A series of nitrogen mustard-linked chalcones were synthesized and evaluated for their antitumor activity in vitro against the K562 and HepG2 cell lines. The aldol condensation of [N,N-bis(chloroethyl)-3-amino]-acetophenone (2) with aromatic aldehydes afforded the nitrogen mustard-linked chalcones. Among the analogs tested, compounds 5e and 5k exhibited significant anti-proliferation activities against K562 cells with IC50 values of 2.55 and 0.61 μM, respectively, which revealed higher cell toxicity than the standard drugs cisplatin (IC50 200 μM) and adriamycin (IC50 = 14.88 μM). The methoxyl and N,N-dimethyl groups on the B-ring of the chalcone frame enhanced the inhibitory activities against both the K562 and HepG2 cell lines. The structure-activity relationship study indicated that the inhibitory activities significantly varied with the position(s) and species of the substituted group(s). A series of nitrogen mustard-linked chalcones were prepared and evaluated for their antitumor activities against the K562 and HepG2 cell lines. The structure-activity relationship study indicated that the methoxyl and N,N-dimethyl groups on the B-ring of the chalcone frame may enhance the inhibitory activities of the chalcones.
机译：合成了一系列氮芥末连接的查耳酮，并在体外评估了其对K562和HepG2细胞系的抗肿瘤活性。 [N，N-双（氯乙基）-3-氨基]-苯乙酮（2）与芳族醛的醛醇缩合得到氮芥末连接的查耳酮。在测试的类似物中，化合物5e和5k对K562细胞表现出显着的抗增殖活性，IC50值分别为2.55和0.61μM，与标准药物顺铂（IC50> 200μM）和阿霉素（IC50 = 14.88μM）。查耳酮骨架的B环上的甲氧基和N，N-二甲基增强了对K562和HepG2细胞系的抑制活性。结构-活性关系研究表明，抑制活性随取代基的位置和种类而显着变化。制备了一系列氮芥末连接的查耳酮，并评估了它们对K562和HepG2细胞系的抗肿瘤活性。构效关系研究表明，查耳酮骨架B环上的甲氧基和N，N-二甲基可能增强了查耳酮的抑制活性。

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