Metal Complexes of Uracil Derivatives with Cytotoxicity and Superoxide Scavenging Activity

被引：19

作者：

Prachayasittikul, Supaluk ^{[1
]}

Worachartcheewan, Apilak ^{[2
]}

Pingaew, Ratchanok ^{[1
]}

Suksrichavalit, Thummaruk ^{[2
,3
]}

Isarankura-Na-Ayudhya, Chartchalerm ^{[3
]}

Ruchirawat, Somsak ^{[4
,5
]}

Prachayasittikul, Virapong ^{[3
]}

机构：

[1] Srinakharinwirot Univ, Fac Sci, Dept Chem, Bangkok 10110, Thailand

[2] Mahidol Univ, Fac Med Technol, Ctr Data Min & Biomed Informat, Bangkok 10700, Thailand

[3] Mahidol Univ, Fac Med Technol, Dept Clin Microbiol & Appl Technol, Bangkok 10700, Thailand

[4] Chulabhorn Res Inst, Bangkok 10210, Thailand

[5] Chulabhorn Grad Inst, Bangkok 10210, Thailand

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2012年 / 9卷 / 03期

关键词：

5-iodouracil; 5-nitrouracil; Metal complex; SOD and cytotoxic activities; ANTITUMOR-ACTIVITY; ANTIMICROBIAL ACTIVITIES; COPPER-COMPLEXES; COORDINATION; 5-IODOURACIL; ANTIOXIDANT; CU(II); AGENTS;

D O I：

10.2174/157018012799129918

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5-Substituted uracils were reported to be important core structure of diverse therapeutics. Herein, novel mixed ligand transition metal (Mn, Cu, Ni) complexes of 5-iodouracil (5Iu) with 8-hydroxyquinoline or 8HQ (1-3) and 5-nitrouracil (5Nu) with 8HQ (4-6) have been synthesized. The metal complexes 1-6 exert significant cytotoxicity against HepG2, A-549, HuCCA-1 and MOLT-3 cell lines. Particularly, the cytotoxicities of tested complexes against HepG2 cells show their IC50 values lower than the reference drug. Cu complex of 5Nu (5Nu-Cu-8HQ, 5) is the most potent and promising cytotoxic compound. Mn complex of 5Iu (5Iu-Mn-8HQ, 1) is shown to be the most potent antioxidant. This finding reveals the application of using simple and commercially available bioactive ligands like 5Iu, 5Nu and 8HQ for the design and construction of new lead compounds with significant and promising bioactivities.

引用

页码：282 / 287

页数：6

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