Synthesis of New Thioureas Derivatives and Evaluation of Their Efficacy as Proliferation Inhibitors in MCF-7 Breast Cancer Cells by Using 99mTc-MIBI Radiotracer

被引:1
|
作者
Hormati, Ahmad [1 ,2 ]
Shiran, Jafar Abbasi [3 ,4 ]
Molazadeh, Mikaeil [5 ,6 ]
Kaboudin, Babak [3 ]
Ahmadpour, Sajjad [1 ]
机构
[1] Qom Univ Med Sci, Gastroenterol & Hepatol Dis Res Ctr, Qom, Iran
[2] Iran Univ Med Sci, Gastrointestinal & Liver Dis Res Ctr, Tehran, Iran
[3] Inst Adv Studies Basic Sci IASBS, Dept Chem, Zanjan, Iran
[4] Ardabil Univ Med Sci, Pharmaceut Sci Res Ctr, Ardebil, Iran
[5] Urmia Univ Med Sci, Fac Med, Dept Med Phys, Orumiyeh, Iran
[6] Ardabil Univ Med Sci, Fac Med, Dept Med Phys, Ardebil, Iran
基金
美国国家科学基金会;
关键词
Breast cancer; Thiourea; NMR; MTT assay; Biodistribution; MCF-7; UREA DERIVATIVES; ANTIBACTERIAL; DESIGN; ACID; POLYMERIZATION; PERFORMANCE;
D O I
10.2174/1573406416666200425224921
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Background & Objective: Anti-tumor activity of some thioureas derivatives is well documented in literature and received considerable attention. The present study aims to synthesize and characterize some novel thioureas and carbonylthioureas as anti-tumor agents for MCF-7 breast cancer cells in vitro and in vivo. Materials & Methods: Several 1-allyl-3-(substituted phenyl), N,N'-(phenylene) bis(3-allyldithithiourea) and 1-cyclopropanecarbonyl-3-(substituted phenyl)-thioureas derivatives were synthesized and confirmed by FT-IR spectroscopy, NMR and C-13-NMR. Anti-tumor activity of these compounds was determined by various in vitro and in vivo assays including; MTT, tumor volume measurement as well as, Tc-99m-MIBI tumor uptake in MCF-7 tumor bearing nude mice. Results: Among all of the synthesized compounds, some thioureas derivatives [3i] and [4b] at 100 nM concentration exhibited significant inhibitory effects on the proliferation of MCF-7 cell in vitro. However, this inhibition was not observed in HUVEC human endothelial normal cells. In vivo anti-tumor effects of the synthesized compounds on MCF-7 xenograft mouse models demonstrated a reduction in the tumor volume for various concentrations between 2 to 10 mg/kg after 21 days. These effects were comparable with Tamoxifen as standard anti-estrogen drug. According to the Tc-99m-MIBI biodistribution result, treatment of MCF-7 bearing nude mice with both [3i] and [4b] compounds at the maximum concentration (10 mg/kg) can lead to a significant decrease of Tc-99m-MIBI tumor uptake. Conclusion: Compounds [3i] and [4b] suppressed the growth of MCF-7 cells in the xenograft nude mice at the doses that were well-tolerated. Our study suggests that these new compounds with their significant anti-tumor effects, may serve as useful candidates for breast cancer therapy.
引用
收藏
页码:766 / 778
页数:13
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