| Literature DB >> 22959246 |
Domenico Alloatti1, Giuseppe Giannini, Loredana Vesci, Massimo Castorina, Claudio Pisano, Elena Badaloni, Walter Cabri.
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.Entities:
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Year: 2012 PMID： 22959246 DOI： 10.1016/j.bmcl.2012.07.061
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823