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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis of some new pyrazolo(3,4-d)pyrimidine derivatives of expected anticancer and radioprotective activity.
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Synthesis of some new pyrazolo(3,4-d)pyrimidine derivatives of expected anticancer and radioprotective activity.

机译：合成的一些新的具有预期抗癌和辐射防护活性的吡唑并（3,4-d）嘧啶衍生物。

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摘要

On the account of the reported anticancer activity of pyrazolo[3,4-d]pyrimidines, a new series of pyrazolo[3,4-d]pyrimidine derivatives were synthesized and tested for in-vitro anticancer activity against Ehrlich Ascites Carcinoma (EAC) cell line. Moreover, one of the target products was evaluated for in-vivo radioprotective activity. The reaction of o-aminoester 1 with benzylamine in presence of triethylorthoformate yielded the corresponding 5-benzylpyrazolopyrimidine derivative 2. The N-amino derivative 3 was used to synthesize new derivatives of pyrazolopyrimidines 4-7. The corresponding 1,3,4-oxadiazolopyrazolopyrimidine derivatives 12 and 14 were obtained via reaction of compound 9 with reagent 10 and/or triethylorthoformate. Thiophosgenation of compound 1 furnished the corresponding 5-isothiocyanate derivative 15, which was reacted with o-phenylenediamine, thiosemicarbazide and anthranilic acid to give benzimidazolopyrazolopyrimidine, 17, pyrazolotriazolopyrimidine, 19 and pyrazolopyrimidobenzoxazine, 20 respectively. The structures of the synthesized compounds were confirmed by microanalyses, IR, NMR, and mass spectral data. Compounds 2 and 9 showed intermediate anticancer activity compared to doxorubicin as positive control with IC50 values of 90 and 100 microg/ml, respectively. On the other hand, compound 5 showed significant radioprotective effect.
机译：由于报道了吡唑并[3,4-d]嘧啶的抗癌活性，合成了一系列新的吡唑并[3,4-d]嘧啶衍生物并测试了其对艾氏腹水癌（EAC）的体外抗癌活性。细胞系。此外，评估了一种目标产品的体内放射防护活性。邻氨基酯1与苄胺在原甲酸三乙酯存在下反应，生成相应的5-苄基吡唑并嘧啶衍生物2。N-氨基衍生物3用于合成吡唑并嘧啶4-7的新衍生物。通过化合物9与试剂10和/或原甲酸三乙酯的反应获得相应的1,3,4-恶二唑并吡唑并嘧啶衍生物12和14。化合物1的硫光气化作用提供了相应的5-异硫氰酸酯衍生物15，其与邻苯二胺，硫代氨基脲和邻氨基苯甲酸反应，分别得到苯并咪唑并吡唑并嘧啶17，吡唑并三唑并嘧啶19和吡唑并嘧啶并苯并恶嗪20。通过微分析，IR，NMR和质谱数据确认了合成化合物的结构。与作为阳性对照的阿霉素相比，化合物2和9显示出中等的抗癌活性，IC50值分别为90和100 microg / ml。另一方面，化合物5显示出显着的辐射防护作用。

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