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

衍生自3-苯基喹喔啉-2(1H)-酮和2-肼基-3-苯基喹喔啉的两个新系列喹喔啉,即1-取代-3-苯基喹喔啉-2(1H)-酮,2a-c,3a-d和4; 2-(3-氧代-3,3a,4,5,6,7-六氢吲哚-2-基)-3-苯基喹喔啉6; N-环戊基或亚苄基-N'-(3-苯基喹喔啉-2-基) 肼,7和18; 1-取代-4-苯基-1,2,4-三唑并 [4,3-a] 喹喔啉,9,10,12,13,14,合成了16个化合物,以评估其抗肿瘤和抗菌活性。NCI的初步筛选表明,化合物2b,2c,3b,3c,和9在10(-6) 至10(-5) 摩尔浓度之间的各种肿瘤细胞株上表现出中等至强的生长抑制活性。化合物3b是活性最强的,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的选择性,和黑色素瘤SK-MEL-5 (GI(50) 分别为4.03、6.46和4.17 microM)。另一方面,体外微生物数据显示制备的化合物显示出温和的抗菌活性。

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