Efficient synthesis and biological evaluation of 1,2,9-trisubstituted 1,9-dihydro-6H-purin-6-ones.
Efficient synthesis and biological evaluation of 1,2,9-trisubstituted 1,9-dihydro-6H-purin-6-ones.
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DOI：
10.1016/j.bmcl.2008.12.007
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发表时间：
2009-02
影响因子：
2.7
通讯作者：
N. Huang;Yong‐ju Liang;M. Ding;Li-wu Fu;H. He
中科院分区：
文献类型：
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作者：
N. Huang;Yong‐ju Liang;M. Ding;Li-wu Fu;H. He
碳二亚胺 4 是由亚氨基正膦 3 与芳香族异氰酸酯进行氮杂维蒂希反应得到的，在催化量的 RO−Na+ 存在下与胺反应，以良好的收率得到 1,2,9-三取代的 1,9-二氢-6H-嘌呤-6-酮 6。化合物6对多种癌细胞表现出细胞毒性。例如，化合物6b对KB、HepG2和OVCAR3表现出最好的抑制活性，IC509.5、20.4和10.0μM。
The carbodiimides 4, obtained from aza-Wittig reactions of iminophosphorane 3 with aromatic isocyanates, reacted with amines in the presence of a catalytic amount of RO−Na+to give the 1,2,9-trisubstituted 1,9-dihydro-6H-purin-6-ones 6 in good yields. Compound 6 exhibited cytotoxicity against various cancer cells. For example, compounds 6b showed the best inhibition activities against KB, HepG2 and OVCAR3 with IC509.5, 20.4 and 10.0μM.