Adenosine deaminase (ADA) inhibitors have been found to have antitumor activities. Here, thirteen potential adenosine deaminase inhibitors 5-amino-1H-pyrazole-4-carboxamide derivatives were designed, synthesized and screened for antitumor activities. Compound 8e exhibited strong growth-inhibitory effects which showed selectivity toward the estrogen receptor positive breast cancer cells (MCF-7) compared to other 5-amino-1H-pyrazole-4-carboxamide derivatives. In addition, it also exhibited appropriate (μM) adenosine deaminase inhibitory potency. Preliminary structure-activity relationships indicated that the incorporation of long chain branching on nitrogen atoms at pyrazole moiety was responsible for their activity.

已经发现腺苷脱氨酶（ADA）抑制剂具有抗肿瘤活性。在这里，设计，合成和筛选抗肿瘤活性的十三种潜在的腺苷脱氨酶抑制剂5-氨基-1H-吡唑-4-羧酰胺衍生物。与其他5-氨基-1H-吡唑-4-羧酰胺衍生物相比，化合物8e具有很强的生长抑制作用，对雌激素受体阳性乳腺癌细胞（MCF-7）具有选择性。此外，它还表现出适当的（μM）腺苷脱氨酶抑制能力。初步的结构-活性关系表明，吡唑部分氮原子上长链支化的引入是其活性的原因。