Synthesis and In Vitro Biological Evaluation of Novel Pyrazole Derivatives as Potential Antitumor Agents

被引:0
作者
Christodoulou, Michael S. [2 ]
Fokialakis, Nikolas [3 ]
Nam, Sangkil [4 ]
Jove, Richard [4 ]
Skaltsounis, Alexios-Leandros [3 ]
Haroutounian, Serkos A. [1 ]
机构
[1] Agr Univ Athens, Dept Sci, Chem Lab, Athens 11855, Greece
[2] Univ Milan, Dipartimento Chim Organ & Ind, I-20133 Milan, Italy
[3] Univ Athens, Fac Pharm, Div Pharmacognosy & Chem Nat Prod, GR-15771 Athens, Greece
[4] City Hope Natl Med Ctr, Beckman Res Inst, Dept Mol Med, Duarte, CA 91010 USA
关键词
Pyrazole; Antitumor activity; Breast cancer; Melanoma; Prostate cancer; CELECOXIB; CANCER; DESIGN; IDENTIFICATION; INHIBITORS; APOPTOSIS; SERIES;
D O I
暂无
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of twenty seven novel pyrazole derivatives bearing aryl substituted groups at positions 1 and 3 of the pyrazole structural motif and various functional groups at position 4 is presented. The critical step for their synthesis is the TCT/DMF promoted cyclization of the corresponding hydrazine precursors, which provided the desired pyrazole skeleton. The anticancer properties of the novel pyrazole derivatives were evaluated in vitro against human prostate (DU145), melanoma (A2058) and breast cancer (MCF-7) cell lines. Among the compounds tested, pyrazole 5a and its methoxy derivatives 3d, e were assayed as the most potent, displaying selective activity against the MCF-7 cell line with IC50 values of 14, 10 and 12 mu M respectively. Results herein indicate that the reported backbone represents a promising structural lead for further development as antitumor agents.
引用
收藏
页码:779 / 788
页数:10
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