AQUA[1-(2,6-DICHLORO-4-HYDROXYPHENYL)-2-PHENYLETHYLENEDIAMINE](SULFATO)PLATINUM-(II) COMPLEXES WITH VARIABLE SUBSTITUENTS IN THE 2-PHENYL RING .1. SYNTHESIS AND ANTITUMOR AND ESTROGENIC PROPERTIES
AQUA[1-(2,6-DICHLORO-4-HYDROXYPHENYL)-2-PHENYLETHYLENEDIAMINE](SULFATO)PLATINUM-(II) COMPLEXES WITH VARIABLE SUBSTITUENTS IN THE 2-PHENYL RING .1. SYNTHESIS AND ANTITUMOR AND ESTROGENIC PROPERTIES
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DOI：
10.1021/jm00171a031
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发表时间：
1990-09-01
影响因子：
7.3
通讯作者：
SCHONENBERGER, H
中科院分区：
文献类型：
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作者：
GUST, R;BURGEMEISTER, T;SCHONENBERGER, H
合成了赤式和苏式构型的水[1-（2，6-二氯-4-羟基苯基）-2-苯基乙二胺]（硫酸根合）铂（II）配合物，在2-苯基环中具有不同的取代基（2-PtSO 4至9-PtSO 4：H、4-F、3-OH、4-OH、2，6-F2、2，6-Cl 2、2-F/4-OH、2-Cl/4-OH）并测试了雌激素和抗肿瘤活性。通过三步反应得到配体。使芪类与IN 3和NaN 3的混合物反应，得到相应的1，2-二叠氮基-1，2-二苯基乙烷。随后用LiAlH 4还原得到相应的1，2-二苯基乙二胺。通过Ag_2SO_4与二胺与K_2PtI_4配位得到的二碘配合物反应，合成了硫酸根合铂（II）配合物。两个配合物，双-8-PtSO_4和双-9-PtSO_4，具有抗肿瘤和雌激素作用，因此在乳腺癌的治疗中具有重要意义。
Erythro- and threo-configurated aqua[1-(2,6-dichloro-4-hydroxyphenyl)-2-phenylethylenediamine](sulfato)platinum(II) complexes with variable substituents in the 2-phenyl ring (2-PtSO4 to 9-PtSO4: H, 4-F, 3-OH, 4-OH, 2,6-F2, 2,6-Cl2, 2-F/4-OH, 2-Cl/4-OH) were synthesized and tested for estrogenic and antitumor activities. The ligands were obtained by a three-step reaction. The stilbenes were reacted with a mixture of IN3 and NaN3 to yield the respective 1,2-diazido-1,2-diphenylethanes. The subsequent reduction with LiAlH4 led to the corresponding 1,2-diphenylethylenediamines. The (sulfato)platinum(II) complexes were synthesized by reaction of Ag2SO4 with the diiodo complexes, which had been obtained by coordination of the diamines with K2PtI4. Two complexes, erythro-8-PtSO4 and erythro-9-PtSO4, possess antitumor and estrogenic effects and are therefore of interest for the therapy of breast cancer.