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Camptothecins in Tumor Homing via an RGD Sequence Mimetic

Domenico Alloatti, Giuseppe Giannini, Loredana Vesci, Massimo Castorina, Claudio Pisano, Elena Badaloni, Walter Cabri

Bioorg Med Chem Lett. 2012 Oct 15;22(20):6509-12.

PMID: 22959246

Abstract:

A RGD peptide mimetic was conjugated to four camptothecins, with the purpose to improve their therapeutic index. The conjugate derivatives were evaluated against two tumor cell lines, one overexpressing integrins (human ovarian carcinoma, A2780) and a second one with a low integrin expression (human prostate cancer, PC3). The in vitro screening was completed with the adhesion behavior to vitronectin. Compound 8 (ST7456CL1) was selected for the in vivo investigation after stability tests over 24h, in PBS solution and in rat plasma, and compared to irinotecan. The former showed a prolonged half-life.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP83380829-C Vitronectin from rat plasma Vitronectin from rat plasma 83380-82-9 Price
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