| 碘化1-甲基-2,4-二氨基-6-(N-甲基-取代苄氨基)喹唑啉鎓的合成及其抗疟和抗肿瘤作用 |
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| 引用本文： | 周伟澄,忻志铭,李炳生,李高德,张秀平.碘化1-甲基-2,4-二氨基-6-(N-甲基-取代苄氨基)喹唑啉鎓的合成及其抗疟和抗肿瘤作用[J].药学学报,1989,24(12):953-956. |
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| 作者姓名： | 周伟澄 忻志铭 李炳生 李高德 张秀平 |
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| 作者单位： | 上海医药工业研究院，上海医药工业研究院，上海医药工业研究院，第二军医大学，上海医药工业研究院 上海 200040，上海 200040，上海 200040，上海，上海 200040 |
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| 基金项目： | 国家自然科学基金No.2860202 |
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| 摘 要： | 2,4-二氨基喹唑啉类化合物具有抗肿瘤、抗菌和抗疟等多方面药理活性,已证明甲氧苄啶(甲氧苄氨嘧啶TMP)和甲氨喋呤(MTX)与受体(二氢叶酸还原酶,DHFR)结合时,杂环上N′质子化,并与DHFR的A_(sp)-27的游离羧基发生电荷转移作用。作者已报道,2,4-二氨基-6-(N-甲基-取代苄氨基)喹唑啉(Ⅰ)有强的抗疟和抗肿瘤作
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| 关 键 词： | 氨基喹唑啉鎓 抗疟作用 抗肿瘤作用 |
| 收稿时间： | 1988-09-19 |
SYNTHESIS AND ANTIMALARIAL AS WELL AS ANTITUMOR ACTIVITIES OF 1-METHYL-2,4-DIAMINO-6-(N-METHYL-SUBSTITUTED BENZYLAMION) QUINAZOLINIUM IODIDES |
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| WC Zhou,ZM Xin,BS Li,GD Li and XP Zhang.SYNTHESIS AND ANTIMALARIAL AS WELL AS ANTITUMOR ACTIVITIES OF 1-METHYL-2,4-DIAMINO-6-(N-METHYL-SUBSTITUTED BENZYLAMION) QUINAZOLINIUM IODIDES[J].Acta Pharmaceutica Sinica,1989,24(12):953-956. |
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| Authors: | WC Zhou ZM Xin BS Li GD Li and XP Zhang |
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| Abstract: | Fourteen 1-methyl-2,4-diamino-6-(N-methyl-substituted benzylamino) quinazolinium iodides (II) were synthesized by treatment of 2,4-diamino-6-substituted benzylaminoquinazolines with methyl iodide. Three compounds (II4,7,10) were shown to produce 100% suppression on Plasmodium berghei in mice at oral dose of 20 mg/kg and II4 was found to inhibit twice as much as methotrexate on L1210 Leukemia cells in culture. |
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| Keywords: | Aminoquinazolinium Antimalarials Antineoplastic |
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