The present invention relates to a novel class of supermolecular
carboplatin derivatives represented by general formula (I), wherein B is a polycarboxylic acid represented by general formula (II), wherein R1, R2 and n are defined as in the description. The present invention also relates to a process for preparing the same, pharmaceutical compositions containing the same as
active ingredient and the use of the derivatives in the preparation of pharmaceutical compositions which are useful in treating various cellular cancers including hepatoma,
stomach cancer,
lung cancer and the like. The derivatives have stable cage-like chemical structures and constitutions in
solid and in
aqueous solution. The derivatives can not only kill
cancer cells at a rate significantly higher than that by
carboplatin, in particular, in the case of hepatoma cells, at a rate one to two times higher than that by
carboplatin, but also produce little side effects such as vomit, baldness, decreases of leucocytes and platelets, and the like, which can be induced by administration of other chemotherapeutics. In the
acute toxicity tests on mice, the
lethal dose (LD50) of the present derivatives is about 300 mg / kg and 260 mg / kg
body weight for a subcutaneous(sc) and an intraperitoneal(ip) administration, respectively. Therefore, the present derivatives are a novel class of cis-platium which can be widely used as anticancer agents.