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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：预期抗癌活性的一些新吡唑（3,4-D）嘧啶衍生物的合成。

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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：对账户的报告吡唑并[3,4-d]嘧啶类，一系列新的吡唑并[3,4-d]嘧啶衍生物的抗癌活性的合成和针对艾氏腹水癌的体外抗癌活性试验（EAC）细胞系。此外，目标产品的一个被评价用于体内辐射防护活性。与在原甲酸三乙酯的存在苄胺邻氨基酯1所述的反应，得到相应的5- benzylpyrazolopyrimidine衍生物2. N-氨基衍生物3用于合成吡唑并嘧啶4-7中新衍生物。相应的1,3,4- oxadiazolopyrazolopyrimidine衍生物12和14通过与试剂10和/或原甲酸三乙酯化合物9的反应而获得。化合物1的Thiophosgenation提供的相应的5-异硫氰酸酯衍生物15，将其与邻苯二胺反应，氨基硫脲和氨茴酸，分别得到benzimidazolopyrazolopyrimidine，17，pyrazolotriazolopyrimidine，19和pyrazolopyrimidobenzoxazine，20。合成的化合物的结构通过微量分析，IR，NMR和质谱数据证实。化合物2和9显示出相比于多柔比星与分别的90的IC 50个值和100微克/毫升，阳性对照中间抗癌活性。在另一方面，化合物5显示显著防护作用。

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