Synthesis and in vitro anti-tumor activity of carboranyl levodopa

被引：8

作者：

Zhu, Yinghuai ^{[1
]}

Lin, Yongxiang ^{[2
]}

Hosmane, Narayan S. ^{[3
]}

机构：

[1] Macau Univ Sci & Technol, Sch Pharm, Ave Wai Long, Taipa 999078, Macao, Peoples R China

[2] Inst Chem & Engn Sci, 1 Pesek Rd, Singapore 627833, Singapore

[3] Northern Illinois Univ, Dept Chem & Biochem, De Kalb, IL 60115 USA

来源：

BIOORGANIC CHEMISTRY | 2019年 / 90卷

关键词：

Neutron capture therapy (NCT); Anti-tumor; Levodopa; Drug delivery; Bio-assessment; NEUTRON-CAPTURE THERAPY; ORAL-CANCER; BIODISTRIBUTION; LIPOSOMES;

D O I：

10.1016/j.bioorg.2019.103090

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Reactions of closo-1-Me-2-Iodobutyl-1,2-closo-dicarborane, 1-Me-2-I(CH2)(4)-C2B10H10, with L-dopa methyl ester can produce carboranyl L-dopa methyl esters in 54% yield in the presence of sodium hydroxide. The appended closo-carboranes can be decapitated with sodium hydroxide in a mixed solvent of ethanol and deionized water to produce highly water-soluble carboranyl levodopa in 64% yield. All the new compounds were characterized by H-1, C-13, B-11 NMR, FT-IR spectroscopy and elemental analysis. The highly water soluble carboranyl levodopa 4 shows promising efficacy of anti-tumors in vitro in the presence of slow neutron beams.

引用

页数：5

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