Replacement of a thiourea-S with an amidine-NH donor group in a platinum-acridine antitumor compound reduces the metal's reactivity with cysteine sulfur.
Replacement of a thiourea-S with an amidine-NH donor group in a platinum-acridine antitumor compound reduces the metal's reactivity with cysteine sulfur.
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DOI：
10.1021/jm900451y
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发表时间：
2009-05-28
影响因子：
7.3
通讯作者：
Bierbach U
中科院分区：
文献类型：
--
作者：
Ma Z;Rao L;Bierbach U
研究了两种靶向DNA的铂-吖啶缀合物与半胱氨酸硫的反应性。与含有硫脲-S键的原型衍生物相比，含有与氯离去基团顺式的脒-NH供体基团的缀合物显示出与N-乙酰半胱氨酸的反应性大大降低。以前在与核碱基氮的反应中观察到相反的情况。独特的目标选择性调整的取代化学的药效学特性和生物活性，这些药剂的可能后果进行了讨论。
The reactivity of two DNA-targeted platinum–acridine conjugates with cysteine sulfur was studied. The conjugate containing an amidine-NH donor group cis to the chloride leaving group showed considerably reduced reactivity with N-acetylcysteine compared to the prototypical derivative containing a thiourea-S linkage. The opposite scenario has been observed previously in reactions with nucleobase nitrogen. Possible consequences of the unique target-selective tuning of the substitution chemistry for the pharmacodynamic properties and biological activity of these agents are discussed.
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影响因子：
7.3
作者：
Ma Z;Choudhury JR;Wright MW;Day CS;Saluta G;Kucera GL;Bierbach U
通讯作者：
Bierbach U
影响因子：
7.3
作者：
Martins, ET;Baruah, H;Bierbach, U
通讯作者：
Bierbach, U
影响因子：
3
作者：
Ackley, MC;Barry, CG;Bierbach, U
通讯作者：
Bierbach, U
影响因子：
4.6
作者：
BONIVENTO, M;CANOVESE, L;TOBE, ML
通讯作者：
TOBE, ML
影响因子：
4.6
作者：
BONIVENTO, M;CATTALINI, L;TOBE, ML
通讯作者：
TOBE, ML