Synthesis and Evaluation of the Antiproliferative Properties of a Tethered Tubercidin-Platinum(II) Complex

被引:8
作者
D'Errico, Stefano [1 ]
Oliviero, Giorgia [1 ]
Borbone, Nicola [1 ]
Di Gennaro, Elena [2 ]
Zotti, Andrea Ilaria [2 ]
Budillon, Alfredo [2 ]
Cerullo, Vincenzo [3 ]
Nici, Fabrizia [1 ]
Mayol, Luciano [1 ]
Piccialli, Vincenzo [4 ]
Piccialli, Gennaro [1 ,5 ]
机构
[1] Univ Naples Federico II, Dipartimento Farm, I-80131 Naples, Italy
[2] Fdn G Pascale IRCCS, Ist Nazl Tumori, Expt Pharmacol, I-80131 Naples, Italy
[3] Univ Helsinki, Fac Pharm, Div Biopharmaceut & Pharmacokinet, Helsinki 00790, Finland
[4] Univ Naples Federico II, Dipartimento Sci Chim, I-80126 Naples, Italy
[5] Natl Res Council Italy, Inst Prot Biochem, I-80131 Naples, Italy
关键词
Platinum; Nucleosides; Antitumor agents; Medicinal chemistry; PHARMACOLOGICAL EVALUATION; ANTICANCER DRUG; PLATINUM; NUCLEOSIDE; CISPLATIN; CANCER; TUBERCIDIN; SUPPRESSION; RESISTANCE; EFFICACY;
D O I
10.1002/ejoc.201500998
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Herein, the synthesis of a nucleoside platinum(II) complex in which a cisplatin-like unit is joined to 7-deazaadenosine through an amino alkyl chain installed at the C6 position of purine was explored. The capability of the new complex to react with DNA purine bases was confirmed by a model reaction with deoxyguanosine monophosphate, whereas its anti-proliferative activity against A549 and Cal27 human cancer cell lines was studied by sulforhodamine B assay in comparison with its unplatinated precursor and cisplatin.
引用
收藏
页码:7550 / 7556
页数:7
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