Antiproliferative effects of novel urea derivatives against human prostate and lung cancer cells; and their inhibition of β-glucuronidase activity

被引:8
作者
Perveen, Shahnaz
Mustafa, Sana [1 ]
Qamar, Kehkashan [2 ]
Dar, Ahsana [2 ]
Khan, Khalid M. [2 ]
Choudhary, Muhammad Iqbal [2 ]
Khan, Ajmal [3 ]
Voelter, Wolfgang [4 ]
机构
[1] Univ Karachi, Dept Chem, Karachi 75270, Pakistan
[2] Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan
[3] King Saud Univ, Fac Sci, Dept Chem, Riyadh, Saudi Arabia
[4] Univ Tubingen, Interfak Inst Biochem, D-72076 Tubingen, Germany
关键词
Urea derivatives; Prostate cancer (PC-3) cell line; Lung cancer (NCI-H460) cell line; beta-Glucuronidase; Urease; Phosphodiesterase; ANTICANCER AGENTS; TOXICITY; DESIGN; SCREEN; ASSAYS;
D O I
10.1007/s00044-013-0702-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Twenty-one novel urea derivatives were synthesized and their structures characterized by mass, NMR, IR, and UV spectroscopy. These compounds were evaluated for their antiproliferative profile against human PC-3 (prostate) and NCI-H460 (lung) cancer cell lines. Among them, compound 21 N-(3-nitrophenyl)-N'-(1-phenylethyl)urea was found to be active against both PC-3 (IC50 +/- A SEM: 20.13 +/- A 0.91 mu M) and NCI-H460 (GI(50): 22 +/- A 2.6 mu M) cell lines; hence has the potential to be further studied as anticancer agent. These compounds were also investigated for their ability to inhibit urease, beta-glucuronidase, and phosphodiesterase enzymes. N-(2,6-Dimethylphenyl)-N'-(4'-nitrophenyl)urea (1) demonstrated 90 % inhibition of beta-glucuronidase enzyme (IC50 +/- A SEM: 3.38 +/- A 0.043 mu M).
引用
收藏
页码:1099 / 1113
页数:15
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