首页> 外文期刊>Heterocycles: An International Journal for Reviews and Communications in Heterocyclic Chemistry >SOME NEW C3- AND Cs-SYMMETRICAL TRIALKYLAMINO-SUBSTITUTED 1,3,5-TRIAZINES AND THEIR BIOLOGICAL EVALUATION
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SOME NEW C3- AND Cs-SYMMETRICAL TRIALKYLAMINO-SUBSTITUTED 1,3,5-TRIAZINES AND THEIR BIOLOGICAL EVALUATION

机译:一些新的C3和CS-对称三烷基氨基取代的1,3,5-三嗪及其生物学评估

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摘要

We report the preparation of some new additionally synthesized symmetrical 1,3,5-triazines (TAZ) and the results of biological evaluation of their anti-herpes simplex virus type 1 (anti-HSV-1) activity and cytotoxic activity against Vero cells. All of the new trisubstituted TAZ derivatives 3a-3e showed considerable levels of anti-HSV-1 activity (EC50 = 4.4 similar to 30.3 mu M). Among the tested compounds, two compounds (3c-2 and 3d) that have three 3,4-methylenedioxyphenylalkylamino groups showed low levels of cytotoxicity (CC50> 200 mu M) against Vero cells. On the other hand, the C-3-symmetrical TAZ derivatives 3a-2, 3b-2 and 3e showed considerably high levels of cytotoxicity (CC50 = 8.91 similar to 15.2 mu M). The structure-activity relationships for anti-HSV-1 activity and cytotoxicity of synthesized single-drug type 2,4,6-trisubstituted TAZ derivatives are also discussed.
机译:我们报道了一些新合成的对称1,3,5-三嗪类化合物(TAZ)的制备及其抗单纯疱疹病毒1型(抗HSV-1)活性和抗Vero细胞毒性活性的生物学评价结果。所有新的三取代TAZ衍生物3a-3e均显示出相当水平的抗HSV-1活性(EC50=4.4,类似于30.3μM)。在受试化合物中,含有三个3,4-亚甲基二氧苯基烷基氨基的两种化合物(3c-2和3d)对Vero细胞的细胞毒性水平较低(CC50>200μM)。另一方面,C-3对称TAZ衍生物3a-2、3b-2和3e显示出相当高的细胞毒性水平(CC50=8.91,类似于15.2μM)。还讨论了合成的单药2,4,6-三取代TAZ衍生物抗HSV-1活性和细胞毒性的构效关系。

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