Novel 5-Methyl-2-[(un)substituted phenyl]-4-{4,5-dihydro-3-[(un)substituted phenyl]-5-(1,2,3,4-tetrahydroisoquinoline-2-yl)pyrazol-1-yl}-oxazole Derivatives: Synthesis and Anticancer Activity

被引：10
|
作者：
Liu Xinhua [1 ,2 ]
Bai Linshan [1 ]
Pan Chunxiu [1 ]
Song Baoan [3 ]
Zhu Hailiang [1 ,2 ]
机构：
[1] Anhui Univ Technol, Anhui Key Lab Coal Clean Convers & Utilizat, Sch Chem & Chem Engn, Maanshan 243002, Anhui, Peoples R China
[2] Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Jiangsu, Peoples R China
[3] Guizhou Univ, Educ Minist, Key Lab Green Pesticide & Agr Bioengn, Guiyang 550025, Guizhou, Peoples R China
来源：
CHINESE JOURNAL OF CHEMISTRY | 2009年 / 27卷 / 10期
基金：
中国国家自然科学基金;
关键词：
synthesis; aryl-dihydropyrazole; 1,2,3,4-tetrahydroisoquinoline; anticancer activity; BIOACTIVITY; INHIBITORS; OXAZOLES;
D O I：
10.1002/cjoc.200990329
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Eleven novel 5-methyl-2-[(un)substitutedphenyl]-4-{4,5-dihydro-3-[(un)substituted phenyl]-5-(1,2,3,4-tetrahydroisoquinoline-2-yl)pyrazol-1-yl}-oxazole derivatives were synthesized and characterized by elemental analysis, ESI-MS, H-1 NMR and C-13 NMR. All of the compounds have been screened for their antiproliferative activities against PC-3 cell (human prostate cancer) and A431 cell (human epidermoid carcinoma cancer) lines in vitro. The results revealed that compounds 4g, 4j and 4k exhibited the strong inhibitory activities against the PC-3 cell lines (with IC50 values of 2.8 +/- 0.11, 3.1 +/- 0.10 and 3.0 +/- 0.06 mu g/mL, respectively).
引用
收藏
页码：1957 / 1961
页数：5
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