著者

喜谷 喜徳

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.38, no.11, pp.1063-1076, 1980-11-01 (Released:2010-01-22)

参考文献数

31

被引用文献数

1 1

---

Since the discovery of the antitumor activity of cis-dichlorodiammineplatinum (II) (=DDP) by B. Rosenberg et al. in 1969, various diamino Pt complexes have been synthesized and their antitumor activities were tested, in order to prepare more potent Pt complexes, with least toxicity. cis-DDP was found very effective and it had been approved by the Food and Drug Administration, U.S.A. in December, 1978 as an antitumor agent for the treatmet of bladder cancer, ovarian cancer, testis cancer and, head and neck cancer. The problem is the kidney toxicity and severe nausea and vomiting, when DDP was administered to the patients. Ototoxicity is also another problem.Various Pt complexes were synthesized by replacing carrier ligands, and mono- and bi-dentate leaving groups. 1, 2- Cyclohexanediamine (= dach) is considered to be one of the useful carrier ligands. Dach has two geometrical isomers, cis and trans, and the latter is resolved into two optical isomers, d and l.Among the Pt complexes prepared in my laboratory, D-glucuronato and D-gluconato Pt (II) complexes of trans-1-dach are water-soluble and potential antitumor agents.2- (Aminomethyl) cyclohexylamine and stilbenediamine were synthesized. The former has two geometrical isomers, each of which has two optical isomers, while the latter has three isomers, meso, trans-d and trans-l. Preparation of their Pt (II) complexes and their antitumor activities are described.