| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1369482 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
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 24 h, in PBS solution and in rat plasma, and compared to irinotecan. The former showed a prolonged half-life.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Domenico Alloatti, Giuseppe Giannini, Loredana Vesci, Massimo Castorina, Claudio Pisano, Elena Badaloni, Walter Cabri,