Two novel series of quinoxalines derived from 3-phenylquinoxalin-2(1H)-one and 2-hydrazino-3-phenylquinoxaline, namely 1-substituted-3-phenylquinoxaline-2(1H)-ones, 2a-c, 3a-d, and 4; 2-(3-oxo-3,3a,4,5,6,7-hexahydroindazol-2-yl)-3-phenylquinoxaline 6; N- cyclopentylidene or benzylidene-N'-(3-phenylquinoxaline-2-yl)hydrazines, 7 and 18; 1-substituted-4-phenyl-1,2,4-triazolo[4,3-a]quinoxalines, 9, 10, 12, 13, 14, and 16 have been synthesized in order to evaluate their antitumor and antimicrobial activities. Preliminary screening at NCI showed that compounds 2b, 2c, 3b, 3c, and 9 exhibited a moderate to strong growth inhibition activity on various tumor panel cell lines between 10(-6) to 10(-5) molar concentrations. Compound 3b was the most active with a broad spectrum of activity. Compound 3c showed selectivity towards CNS-cancer SF-639, leukemia CCRF-CEM, and melanoma SK-MEL-5 (GI(50) = 4.03, 6.46, and 4.17 microM, respectively). On the other hand, the in vitro microbiological data revealed that the prepared compounds showed mild antimicrobial activity.

译文

:由3-苯基喹喔啉-2(1H)-one和2-肼基-3-苯基喹喔啉衍生的两个新颖的喹喔啉系列,即1-取代-3-苯基喹喔啉-2(1H)-ones,2a-c,3a-d ,和4; 2-(3-氧代-3,3a,4,5,6,7-六氢吲唑-2-基)-3-苯基喹喔啉6; N-环戊叉基或亚苄基-N'-(3-苯基喹喔啉-2-基)肼,7和18;为了评估它们的抗肿瘤和抗菌活性,已经合成了1-取代的4-苯基-1,2,4-三唑并[4,3-a]喹喔啉,9、10、12、13、14和16。在NCI上进行的初步筛选显示,化合物2b,2c,3b,3c和9对摩尔浓度在10(-6)至10(-5)之间的各种肿瘤细胞系表现出中等至强的生长抑制活性。化合物3b是最活跃的,具有广泛的活性。化合物3c显示出对CNS癌症SF-639,白血病CCRF-CEM和黑色素瘤SK-MEL-5的选择性(分别为GI(50)= 4.03、6.46和4.17 microM)。另一方面,体外微生物学数据显示所制备的化合物显示出温和的抗微生物活性。

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