| Added by | celine.gongora |
|---|---|
| Group name | EquipeCG |
| Item Type | Journal Article |
| Title | Synthesis and in vitro antitumour activity of carboplatin analogues containing functional handles compatible for conjugation to drug delivery systems |
| Creator | Re?nik et al. |
| Author | Lisa-Maria Re?nik |
| Author | Christophe Cantelli |
| Author | Cyril Fersing |
| Author | Céline Gongora |
| Author | Jean-Pierre Pouget |
| Author | Vincent Lisowski |
| Abstract | We describe herein the synthesis of a series of carboplatin derivatives with different functional groups at position 3 of the cyclobutane ring. This pharmacomodulation approach aims at facilitating the vectorisation of these analogues, via their subsequent conjugation to a drug delivery system. Five different derivatives bearing a hydroxy, keto, iodo, azido or amino function at position 3 were synthesised. One of these compounds was coupled to a bifunctional maleimide-containing linker. All compounds were tested in vitro for their cytotoxicity on four different cell lines including two platinum-resistant colorectal cancer cell line (SK-OV-3, HCT116, D3E2, D5B7) using an MTS assay. Overall, the tested compounds were up to six times more potent than carboplatin, especially on D5B7 human colorectal cancer cells. We demonstrated that these modifications led to potent analogues which are compatible with conjugation to a drug delivery system. |
| Publication | Bioorganic & Medicinal Chemistry Letters |
| Volume | 30 |
| Issue | 22 |
| Pages | 127527 |
| Date | 2020-11-15 |
| Journal Abbr | Bioorg Med Chem Lett |
| Language | eng |
| DOI | 10.1016/j.bmcl.2020.127527 |
| ISSN | 1464-3405 |
| Library Catalog | PubMed |
| Extra | PMID: 32890684 |
| Tags | Anticancer activity, Antineoplastic Agents, Carboplatin, Carboplatin derivatives, Cell Line, Tumor, Cell Proliferation, Cell Survival, Dose-Response Relationship, Drug, Drug Delivery Systems, Drug Screening Assays, Antitumor, Humans, Molecular Structure, MTS assay, original, Platinum resistance, postdoc, Structure-Activity Relationship, Vectorisation |
| Date Added | 2021/08/27 - 17:08:27 |
| Date Modified | 2022/08/29 - 16:26:01 |
| Notes and Attachments | PubMed entry (Attachment) |
Institut de Recherche en Cancérologie de
