首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Azanonaboranes ((RNH(2))B(8)H(11)NHR) as possible new compounds for use in boron neutron capture therapy.
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Azanonaboranes ((RNH(2))B(8)H(11)NHR) as possible new compounds for use in boron neutron capture therapy.

机译:氮杂硼烷((RNH(2))B(8)H(11)NHR)可能是用于硼中子俘获治疗的新化合物。

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The synthesis and biological in vitro and in vivo activities of possible new compounds for Boron Neutron Capture Therapy (BNCT) are reported. The azanonaboranes of the type [(RNH(2))B(8)H(11)NHR] are water-soluble when hydrophilic groups are introduced. The reaction of B(9)H(13)SMe(2) with primary amines yields azanonaboranes. Five compounds with different numbers of hydroxypropyl groups have been isolated: [(HO(CH(2))(3)NH(2))B(8)H(11)NHCH(3)] (4), [(HO(CH(2))(3)NH(2))B(8)H(11)NH(CH(2))(3)OH] (2), [((HO(CH(2))(3))(2)NH)B(8)H(11)NHCH(3)] (6), [((HO(CH(2))(3))(2)NH)B(8)H(11)NH(CH(2))(3)OCH(3)] (11) and [((HO(CH(2))(3))(2)NH)B(8)H(11)NH(CH(2))(3)OH] (8). In vitro experiments as judged by cloning survival tests showed that two of the synthesised compounds are not toxic. The in vivo experiments were carried out with C3H/He mice bearing SCCVII tumours and C57 mice bearing B16 tumours. Compounds 2 and 6 have no particular affinity to any tissue, but are excluded from the brain.
机译:报道了用于硼中子俘获疗法(BNCT)的可能的新化合物的合成以及体外和体内的生物学活性。当引入亲水基团时,[(RNH(2))B(8)H(11)NHR]型的氮杂硼烷是水溶性的。 B(9)H(13)SMe(2)与伯胺的反应生成金刚烷硼烷。五个化合物具有不同数量的羟丙基已被分离:[[HO(CH(2))(3)NH(2))B(8)H(11)NHCH(3)](4),[(HO( CH(2))(3)NH(2))B(8)H(11)NH(CH(2))(3)OH](2),[(((HO(CH(2))(3) )(2)NH)B(8)H(11)NHCH(3)](6),[((HO(CH(2))(3))(2)NH)B(8)H(11) NH(CH(2))(3)OCH(3)](11)和[((HO(CH(2))(3))(2)NH)B(8)H(11)NH(CH( 2))(3)OH](8)。通过克隆存活测试判断的体外实验表明,两种合成的化合物无毒。体内实验是用带有SCCVII肿瘤的C3H / He小鼠和带有B16肿瘤的C57小鼠进行的。化合物2和6对任何组织都没有特定的亲和力,但被排除在大脑之外。

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