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Synthesis and biological evaluation of peptidomimetics containing the tryptamine moiety as a potential antitumor agent

机译：含色胺盐部分作为潜在抗肿瘤药的拟肽的合成和生物学评估

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摘要

Three series of novel peptidomimetics bearing the tryptamine moiety were designed, synthesized, and evaluated for their inhibition activities against cell proliferation. According to the preliminary studies on cytotoxic activities, some of the newly prepared compounds (Ia-k, IIa-d, IIIa-g) displayed significant inhibition activities against human hepatoma cancer (HepG2 and Huh-7), and human melanoma (A875) cell lines compared with the control 5-fluorouracil. Especially, compounds Ih and Ij exhibited obvious inhibition activities (Ih IC50 = 4.88 +/- 0.78 mu g mL(-1); Ij IC50 = 6.60 +/- 1.20 mu g mL(-1)) against 5-fluorouracil-resistant human hepatocellular carcinoma (BEL-7402/5-FU) cell lines.
机译：设计，合成并评估了三组带有类固醇胺部分的新型拟肽，并评估了它们对细胞增殖的抑制活性。根据细胞毒活性的初步研究，一些新制备的化合物（Ia-k，IIa-d，IIIa-g）显示出对人肝癌（HepG2和Huh-7）和人黑素瘤（A875）的显着抑制活性。细胞系与对照5-氟尿嘧啶相比。特别是化合物Ih和Ij对5-氟尿嘧啶耐药的人表现出明显的抑制活性（Ih IC50 = 4.88 +/- 0.78μg mL（-1）; Ij IC50 = 6.60 +/- 1.20μgmL（-1））肝细胞癌（BEL-7402 / 5-FU）细胞系。

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