Novel c(RGDyK)-based conjugates of POPAM and 5-fluorouracil for integrin-targeted cancer therapy-Reference-Cited by-同舟云学术

Novel c(RGDyK)-based conjugates of POPAM and 5-fluorouracil for integrin-targeted cancer therapy

Published:2017-12 Issue:18 Volume:9 Page:2181-2196
ISSN:1756-8919
Container-title:Future Medicinal Chemistry
language:en
Short-container-title:Future Medicinal Chemistry

Author:

Thysiadis Savvas¹,Katsamakas Sotirios²,Dalezis Panagiotis³,Chatzisideri Theodora¹,Trafalis Dimitrios³,Sarli Vasiliki¹

Affiliation:

1. Department of Chemistry, Aristotle University of Thessaloniki, University Campus, 54124 Thessaloniki, Greece

2. Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, University Campus, 54124 Thessaloniki, Greece

3. Laboratory of Pharmacology, Medical School, National & Kapodistrian University of Athens, 75 Mikras Asias Street, 11527 Athens, Greece

Abstract

Aim: Alkylating agents and antimetabolites are cytotoxic drugs commonly used in cancer treatment. These medications are often associated with serious side effects on normal tissues and organs. Methodology: To improve the pharmacological profile of the alkylating agent POPAM and the antimetabolite 5-fluorouracil, novel integrin-targeted delivery systems based on c(RGDyK) were successfully synthesized. The new conjugates were tested in vitro against different cancer cells such as PC3, SKOV3, A549, MCF7 and MBA-MB-321. Results & conclusion: The c(RGDyK) conjugates of POPAM demonstrated better inhibitory effects and selectivity compared with c(RGDyK) and POPAM. The c(RGDyK) conjugates of 5-FUA demonstrated diverse inhibitory effects compared with c(RGDyK) and 5-FUA related to the levels of integrin expression, the conjugate stability and sensitivity of cancer cells to 5-FUA.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

Link

http://www.future-science.com/doi/pdf/10.4155/fmc-2017-0139

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