Citation: Lei Zhang, Bing Jia, Chang Feng Hu, Fan Wang, Yu Xin Cui. Synthesis and preliminary biological evaluation of the derivatives of O⁶-benzylguanine as inactivators of O⁶-alkylguanine-DNA alkyltransferase[J]. Chinese Chemical Letters, ;2008, 19(7): 801-804. doi: 10.1016/j.cclet.2008.04.046 shu

Synthesis and preliminary biological evaluation of the derivatives of O⁶-benzylguanine as inactivators of O⁶-alkylguanine-DNA alkyltransferase

Lei Zhang ^a,c, ,
Bing Jia ^b ,
Chang Feng Hu ^a ,
Fan Wang ^b ,
Yu Xin Cui ^a,c

a The State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Science, Peking University, Beijing 100083, PR China;
b Medical Isotope Research Center, Peking University, Beijing 100083, PR China;
c Medical and Healthy Analysis Center, Peking University, Beijing 100083, PR China

Received Date: 25 February 2008

Fund Project: This research was supported by research Grant from Beijing Science and Technology Program (No.00004105040311).

A series of new O⁶-BG derivatives (14-21,23-30) were synthesized as inactivators of O⁶-Alkylguanine-DNA alkyltransferase (AGT), and their ability to inhibit AGT was preliminary evaluated by MTT with O⁶-BG as the control. The result suggested compound 30 displayed a higher activity than O⁶-BG.

Keywords:
O⁶-BG derivatives,

AGT inactivator

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Synthesis and preliminary biological evaluation of the derivatives of O⁶-benzylguanine as inactivators of O⁶-alkylguanine-DNA alkyltransferase