Cisplatin amine derivatives

Malik, Duncan, Tomalia, and Esfand [29] reported the use of a variety of amine and acid-containing polymers that chelated platinum forming cisplatin derivatives. They also reported the synthesis of similar dendritic-antineoplastic drugs using vanadocene dichloride. The structure from the poly(propyleneimine) dendrimers contains units are shown in (5) and (6). 

Note Recent results in the authors laboratory have given the unusual result that the in vitro activity of trans- PiC 2(py)2] in LI 210 leukemia is significantly greater than its cis isomer and of the order of cisplatin. The ran -pyridine derivative is not, however, active in vivo but the results do point out that the geometric differences noted so far may not dictate antitumour activity when the neutral ligands are other than primary or secondary amines. 

The D-mannitol derived dimesylate 1 underwent a double displacement with inversion on treatment with tetrabutylammonium azide. Subsequent simple chemical transformations gave the amines 2 and 3 as intermediates for cisplatin-like antitumor agents." Other similar analogues are also described. 

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