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首页> 外文期刊>Bioorganic and Medicinal Chemistry >Synthesis of furopyrazole analogs of 1-benzyl-3-(5-hydroxymethyl-2-furyl)indazole (YC-1) as novel anti-leukemia agents.
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Synthesis of furopyrazole analogs of 1-benzyl-3-(5-hydroxymethyl-2-furyl)indazole (YC-1) as novel anti-leukemia agents.

机译：合成新型抗白血病药物1-苄基-3-（5-羟甲基-2-呋喃基）吲唑（YC-1）的呋喃唑类似物。

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摘要

As part of our continuing search for potential anticancer drug candidates in YC-1 analogs, several 1-benzyl-3-(substituted aryl)-5-methylfuro[3,2-c]pyrazoles were synthesized and evaluated for their cytotoxicity against HL-60 cell line. Among these compounds, 1-benzyl-3-(5-hydroxymethyl-2-furyl)-5-methylfuro[3,2-c]pyrazole (1) showed more potency than YC-1. Through investigation of action mechanism, it was found that compound 1 induced terminal differentiation of HL-60 cells toward granulocyte lineage and promoted HL-60 cell differentiation by regulation of Bcl-2 and c-Myc proteins. Meanwhile, compound 1 also demonstrated apoptosis inducing effect. Such anti-leukemia mechanism of action is apparently different from that of YC-1 which mainly works by inducing apoptosis, but not cell differentiation. Therefore, compound 1 is identified here as a new lead compound of cell differentiating agent and apoptosis inducer for further development of new anti-leukemia agents.
机译：作为我们继续寻找YC-1类似物中潜在抗癌药物候选物的一部分，合成了几种1-苄基-3-（取代的芳基）-5-甲基呋喃[3,2-c]吡唑并评估了它们对HL-的细胞毒性。 60细胞系。在这些化合物中，1-苄基-3-（5-羟甲基-2-呋喃基）-5-甲基呋喃[3,2-c]吡唑（1）比YC-1具有更高的效价。通过作用机理的研究，发现化合物1通过调节Bcl-2和c-Myc蛋白诱导HL-60细胞向粒细胞谱系的终末分化并促进HL-60细胞的分化。同时，化合物1也显示出凋亡诱导作用。这种抗白血病的作用机制显然不同于YC-1，后者主要通过诱导细胞凋亡而不是细胞分化来起作用。因此，在此将化合物1鉴定为细胞分化剂和细胞凋亡诱导剂的新的先导化合物，用于进一步开发新的抗白血病剂。

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