Novel hybrids, pyrazolinylpyrazoles, and pyrazolinyltriazoles were designed, synthesized, and screened for their anticancer activity. Eleven compounds were selected by the National Cancer Institute (NCI)/USA for anticancer screening at single high dose (10⁻⁵ M) in full NCI 60 cell panels. Two compounds: 4‐aminopyrazole‐5‐carbonitrile, 5c (NSC‐747630/1) and ethyl 4‐aminopyrazole‐5‐ carboxylate, 7d (NSC‐747634/1) were the most active candidates of the series and were selected for further evaluation at five dose screening as they displayed significant growth inhibition with full panel median growth inhibition (GI₅₀) 5.47 and 2.24 μM, respectively. Both 5c and 7d hybrids exhibited broad spectrum antitumor activity; however 7d showed moderate selectivity (selectivity ratio 3.6) toward leukemia.

中文翻译：

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新型吡唑啉基吡唑/ 1，2，3-三唑杂种的设计，合成和体外抗癌筛选

设计，合成并筛选了新型杂种，吡唑啉基吡唑和吡唑啉基三唑，以研究其抗癌活性。美国国家癌症研究所（NCI）/美国选择了11种化合物用于在完整NCI 60细胞组中以单次高剂量（10 ^-5 M）进行抗癌筛选。两种化合物：4-氨基吡唑-5-碳腈5c（NSC-747630 / 1）和4-氨基吡唑-5-羧酸乙酯7d（NSC-747634 / 1）是该系列中最活跃的候选化合物，并被选择用于进一步研究在五次剂量筛选中进行了评估，因为它们显示出显着的生长抑制，分别具有全面板中位生长抑制（GI ₅₀）5.47和2.24μM。无论5C和7D杂种表现出广谱的抗肿瘤活性；然而7d显示出对白血病的中等选择性（选择性比3.6）。