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首页> 外文期刊>Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents >Synthesis and antitumor activity of new pyrido2,3-dpyrimidine derivatives
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Synthesis and antitumor activity of new pyrido2,3-dpyrimidine derivatives

机译：新型吡啶并2,3-d嘧啶衍生物的合成及抗肿瘤活性

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摘要

New series of pyrido2,3-dpyrimidines such as; 5-(4-aryl-5-sulfanyl-4H-l,2,4triazol-3-yl) lH,3H,8H-pyr-ido2,3-dpyrirnidine~2,4,7-triones 6,7; S-3-(2,4,7-trioxo-l ,2, 3,4,7,8-hexahydropyrido2,3-dpyrimidin-5-yl)-4-(4-substituted phenyl)-4H-l ,2,4triazol-5-yl-2-(4-phenylpi-perazin-l-yl)ethanethioates 10, 11; 2,4,7-trioxo-N'-(4-substituted piperazin-l-yl)acetyl-l,2,3,4,7,8-hexahydro-pyrido2,3-dpyrimidine-5-carbohydrazides 13-16 and 7V-arylidene-2,4,7-trioxo-l,2,3,4,7,8-hexahydropyrido2,3-dpyrimidine-5-carbohydrazides 17-19 was synthesized through the reaction of the key intermediate 2,4, 7-trioxo-l,2,3,4,7,8-hexahydropyrido2,3-dpyrimidine-5-carbohydrazide 3 with different reagents. The structures of the newly synthesized compounds were elucidated through microanalysis, IR, ~1H NMR, 13C NMR, and mass spec-troscopy. These compounds have been subjected to in vitro antitumor evaluation by bleomycin-dependant DNA damage assay. The most active antitumor compound 6 was selected for further in vivo evaluation of antineoplastic activity against Ehrlich ascites carcinoma in mice. It was observed that our target compound has a potent antitumor activity.
机译：新系列的吡啶并[2,3-d]嘧啶，如;5-（4-芳基-5-硫基-4H-[l，2,4]三唑-3-基）lH，3H，8H-吡喃并[2,3-d]吡啶~2,4,7-三酮 6,7;S-[3-（2,4,7-三氧代-l，2,3,4,7,8-六氢吡啶并[2,3-d]嘧啶-5-基）-4-（4-取代苯基）-4H-[l，2,4]三唑-5-基]-2-（4-苯基吡啶-啌嗪-l-基）硫代乙酯 10， 11;2,4,7-三氧代-N'-[（4-取代哌嗪-l-基）乙酰基]-l，2,3,4,7,8-六氢吡啶并[2,3-d]嘧啶-5-甲酰肼13-16和7V-亚基-2,4,7-三氧代-l，2,3,4,7,8-六氢吡啶并[2,3-d]嘧啶-5-甲酰肼17-19由关键中间体2,4,7,7,8-六氢吡啶并[2,3-d]嘧啶-5-甲酰肼3与不同试剂反应合成。通过显微分析、红外光谱、~1H NMR、13C NMR和质谱分析阐明了新合成化合物的结构。这些化合物已通过博来霉素依赖性 DNA 损伤测定进行体外抗肿瘤评估。选择最活跃的抗肿瘤化合物 6 用于进一步体内评估小鼠对埃利希腹水癌的抗肿瘤活性。据观察，我们的靶化合物具有有效的抗肿瘤活性。

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