Gust R, Burgemeister T, Mannschreck A, Schönenberger H
Institut für Pharmazie, Universität Regensburg, Federal Republic of Germany.
J Med Chem. 1990 Sep;33(9):2535-44. doi: 10.1021/jm00171a031.
Erythro- and threo-configurated aqua1-(2,6-dichloro-4-hydroxyphenyl)-2- phenylethylenediamineplatinum(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-diphenyl-ethylenediamines. 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.
在2-苯基环上具有可变取代基（2-PtSO4至9-PtSO4：H、4-F、3-OH、4-OH、2,6-F2、2,6-Cl2、2-F/4-OH、2-Cl/4-OH）的赤式和苏式构型的水合1-(2,6-二氯-4-羟基苯基)-2-苯基乙二胺铂(II)配合物被合成并测试了雌激素活性和抗肿瘤活性。配体通过三步反应获得。将芪与叠氮化钠和叠氮化锂的混合物反应，得到相应的1,2-二叠氮基-1,2-二苯乙烷。随后用氢化铝锂还原得到相应的1,2-二苯基乙二胺。(硫酸根)铂(II)配合物通过硫酸银与二碘配合物反应合成，二碘配合物是通过二胺与四碘合铂酸钾配位得到的。两种配合物，赤式-8-PtSO4和赤式-9-PtSO4，具有抗肿瘤和雌激素作用，因此对乳腺癌治疗具有重要意义。
