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

被引：12
作者：
Thysiadis, Savvas [1 ]
Katsamakas, Sotirios [2 ]
Dalezis, Panagiotis [3 ]
Chatzisieri, Theodora [1 ]
Trafalis, Dimitrios [3 ]
Sarli, Vasiliki [1 ]
机构：
[1] Aristotle Univ Thessaloniki, Dept Chem, Univ Campus, Thessaloniki 54124, Greece
[2] Aristotle Univ Thessaloniki, Sch Pharm, Dept Pharmaceut Chem, Univ Campus, Thessaloniki 54124, Greece
[3] Univ Athens, Med Sch, Lab Pharmacol, 75 Mikras Asias St, Athens 11527, Greece
来源：
FUTURE MEDICINAL CHEMISTRY | 2017年 / 9卷 / 18期
关键词：
5-fluorouracil; angiogenesis; integrin a(v)beta(3); POPAM; RGD conjugate; RGD peptide; targeted drug delivery; tumor therapy; ALPHA(V)BETA(3) INTEGRIN; MALIGNANT-MELANOMA; ANILINE MUSTARDS; EXPRESSION; ADHESION; DELIVERY; DESIGN; AGENTS; PH;
D O I：
10.4155/fmc-2017-0139
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. [GRAPHICS] .
引用
收藏
页码：2181 / 2196
页数：16
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