Hypoxia-selective O6-alkylguanine-DNA alkyltransferase inhibitors: design, synthesis, and evaluation of 6-(benzyloxy)-2-(aryldiazenyl)-9H-purines as prodrugs of O6-benzylguanine.
Hypoxia-selective O6-alkylguanine-DNA alkyltransferase inhibitors: design, synthesis, and evaluation of 6-(benzyloxy)-2-(aryldiazenyl)-9H-purines as prodrugs of O6-benzylguanine.
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DOI:
10.1021/jm301804p
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发表时间:
2013-02-14
影响因子:
7.3
通讯作者:
Sartorelli, Alan C.
中科院分区:
文献类型:
--
作者:
Zhu, Rui;Baumann, Raymond P.;Penketh, Philip G.;Shyam, Krishnamurthy;Sartorelli, Alan C.
O6-Alkylguanine-DNA alkyltransferase (AGT) is a DNA repair protein which removes alkyl groups from the O-6 position of guanine, thereby providing strong resistance to anticancer agents which alkylate this position. The clinical usefulness of these anticancer agents would be substantially augmented if AGT could be selectively inhibited in tumor tissue, without a corresponding depletion in normal tissue. We report the synthesis of a new AGT inhibitor (5c) which selectively depletes AGT in hypoxic tumor cells.
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影响因子:
5.7
作者:
Ishiguro, K;Shyam, K;Sartorelli, AC
通讯作者:
Sartorelli, AC
影响因子:
3.4
作者:
Baumann RP;Penketh PG;Seow HA;Shyam K;Sartorelli AC
通讯作者:
Sartorelli AC
影响因子:
2.7
作者:
Zhu, Rui;Seow, Helen A.;Baumann, Raymond P.;Ishiguro, Kimiko;Penketh, Philip G.;Shyam, Krishnamurthy;Sartorelli, Alan C.
通讯作者:
Sartorelli, Alan C.
影响因子:
5.8
作者:
Baumann, Raymond P.;Penketh, Philip G.;Ishiguro, Kimiko;Shyam, Krishnamurthy;Zhu, Yong L.;Sartorelli, Alan C.
通讯作者:
Sartorelli, Alan C.
影响因子:
3
作者:
Baumann, RP;Shyam, K;Sartorelli, AC
通讯作者:
Sartorelli, AC