A Novel Water-Soluble Heptaplatin Analogue with Improved Antitumor Activity and Reduced Toxicity

Abstract

A novel water-soluble heptaplatin analogue, cis-[(4R,5R)-4,5-bis-(aminomethyl)-2-isopropyl-1,3-dioxolane](3-hydroxy-1,1-cyclobutanedicarboxylato)platinum(II), has been synthesized and biologically evaluated. The complex shows more activity and less toxicity than its parent drug heptaplatin, exhibiting the great potential for further development.

Recent Advances in Platinum (IV) Complex‐Based Delivery Systems to Improve Platinum (II) Anticancer Therapy

“…Compared to cisplatin, nedaplatin shows less nephrotoxicity and gastrointestinal toxicity, and its pharmacokinetic profile and dose-limiting toxicity is similar to that of carboplatin, and the recommended therapeutic dose of nedaplatin is about 80-100 mg/m 2 via intravenous administration. 33,34 Nedaplatin is widely used in the treatment of NSCLC, esophagus, neck and head, urothelium, and breast cancers. 35 In addition, nedaplatin was also used in combination chemotherapy.…”

Two mixed-NH3/amine platinum (II) anticancer complexes featuring a dichloroacetate moiety in the leaving group

“…K[Pt(NH 3 )Cl 3 ], a commercially available platinum compound, was purchased from Alfa Aesar and 3-hydroxy-1,1-cyclobutanedicarboxylic acid 3 was prepared as previously described1920Composition analyses for C, H and N were performed with a Carlo-Ebra instrument, whereas the content of platinum was determined according to the method in EP6.5. LC/MS measurements were carried out on a Waters Acquity Xevo TQ-S in ESI + mode using MeOH/H 2 O as the solvent.…”

cis‐[PtII(1R,2R‐DACH)(3‐acetoxy‐1,1‐cyclobutanedicarboxylato)], a Water‐Soluble, Oxalate‐Free and Stable Analogue of Oxaliplatin: Synthesis, Characterization, and Biological Evaluations

“…Complex 1 was synthesized by following the route illustrated in Scheme . The preparation of 2 was described in our previous work 15. 16 Acetylation of 2 with acetyl chloride gave rise to 3 , which was converted into the insoluble Ag salt 4 as an intermediate.…”