期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 20, 页码 6509-6512出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.07.061
关键词
Tumor homing; Tumor-specific targeting; RGD mimetic and Integrin; Camptothecin-RGD mimetic conjugate; Anticancer drug delivery system
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. (c) 2012 Elsevier Ltd. All rights reserved.
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