In an effort to find new leads as anticancer or antimicrobial agents, the present work deals with the synthesis of some novel 1-substituted 1,2,4-triazolo[4,3-a]quinoxalines 7, 9a,b, and 14–19 and 1,2,4-triazino[4,3-a]quinoxalines 10a–c as well as 2-[5-amino-3-(4-chlorophenyl)pyrazol-1-yl]-3-benzylquinoxaline 13. These were synthesized using the key intermediate 3-benzyl-2-hydrazinoquinoxaline 6 with various reagents. Ten compounds, namely 7, 9a, 10b, 11, and 13–18 were chosen by the National Cancer Institute of Bethesda (NCI) for evaluation of their anticancer activity. The results indicated that 9a was the most active and was further evaluated for in vitro five dose assay against 60 human cell lines. It was proven to possess the highest broad spectrum anticancer activity. It showed particular effectiveness towards leukemia SR, non-small cell lung cancer HOP-92, NCI-H460, colon cancer HCT-116, HCT-15, CNS cancer U251, melanoma LOX IMVI, renal cancer A498, prostate cancer PC-3, and breast cancer MDA-MB-468 cell lines (GI₅₀ = 3.91, 3.45, 3.49, 3.21, 1.96, 5.18, 3.69, 1.80, 5.19, and 5.55 μM, respectively). All new compounds were screened for their antimicrobial activity and were very active against P. aeruginosa. Compounds 10a and 16 were twice as active as ampicillin against P. aeruginosa. Five compounds, 9a, b, 10b, 13, and 14 were equipotent to ampicillin against P. aeruginosa. In addition, compound 16 showed a broad spectrum antimicrobial activity. Furthermore, compound 9a showed dual activity as an anticancer and antimicrobial agent.

中文翻译：

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新型1,2,4-三唑和1,2,4-三嗪[4,3- a ]喹喔啉作为潜在的抗癌药和抗菌剂的设计，合成和生物学评价†

在努力发现新的线索作为抗癌或抗微生物剂，一些新的1-取代的1,2,4-三唑并[4,3-合成本工作涉及一个]喹喔啉7，图9A，B，和14- 19和1,2,4-三嗪[4,3- a ]喹喔啉10a–c以及2- [5-氨基-3-（4-氯苯基）吡唑-1-基] -3-苄基喹喔啉13。这些是使用关键中间体3-苄基-2-肼基喹喔啉6与各种试剂合成的。10个化合物，即7，图9A，图10B，11，和13-18贝塞斯达国家癌症研究所（NCI）选择了它们来评估其抗癌活性。结果表明9a是最活跃的，并进一步针对60种人类细胞系进行了体外五剂量试验评估。被证明具有最高的广谱抗癌活性。它对白血病SR，非小细胞肺癌HOP-92，NCI-H460，结肠癌HCT-116，HCT-15，CNS癌症U251，黑素瘤LOX IMVI，肾癌A498，前列腺癌PC-3，和乳腺癌MDA-MB-468细胞系（GI ₅₀ = 3.91、3.45、3.49、3.21、1.96、5.18、3.69、1.80、5.19和5.55μM）。筛选所有新化合物的抗菌活性，并对铜绿假单胞菌。化合物10a和16的活性是化合物的两倍氨苄西林对铜绿假单胞菌。五个化合物9a，b，10b，13和14等价于氨苄西林对铜绿假单胞菌。另外，化合物16显示出广谱的抗菌活性。此外，化合物9a显示出作为抗癌和抗微生物剂的双重活性。