Pt(IV) compounds with bioactive ligands (in blue, 7–11): estrogen-tethered Pt(IV) complex (7, n=1–5), ethacraplatin (8), mitaplatin (9), peptide tethered Pt(IV) (10, R1 = RGD, NGR, c(CRGDC), c(RGDfK)), platinacyclobutane (11, L = pyridine for R2 = thymidine, proline, and L = 2,2′-bipyridine for R2 = glucose, cholesterol). Tetra- (12), ipro- (13), satraplatin (14), LA-12 (15), cis,cis,trans-[PtCl2(NH3)(NH2R3)(OOCCH3)2] (16, R3 = H, isopropyl, cyclohexyl), [PtCl4(R42eddp)] (17, R4 = ethyl, n-propyl).