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Structure and Properties
Structure and Properties
Figure 3. Cisplatin, the first Platinum Based Anticancer Drug (cis-[Pt(NH3)2Cl2].)
The cisplatin complex has square planar geometry. The two primary groups are cis to each other and are on the opposite sides of the chlorine groups. The ammonia groups may form hydrogen bonds with nucleic acids on the DNA. The chlorine groups act as leaving groups, while the amine groups bind more strongly to the platinum. The cis-orientation proves to be important in the drug’s delivery mechanism.3
Cisplatin or cis-[Pt(NH3)2Cl2] was first characterized as an anticancer therapy by Barnett Rosenberg and researchers at the University of Michigan. Rosenberg observed that cisplatin inhibited cell growth.2 Since then, it has been used to treat cancers such as ovarian, testicular, and cervical.3 Although it has an effective response-- it is correlated to complete remission, partial response, or stabilization of tumors-- it requires additional medication, has undesired side effects, and can lead to resistance.4 The drawbacks of cisplatin spurred the development of more PBDs.
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