Synthesis and Antiproliferative Screening of Some Heterocycles Derived from 4-((5-Chloro-3-Methyl-1-Phenyl-1H-Pyrazol-4-yl)Methylene)-2-Phenyloxazol-5(4H)-One

被引:7
|
作者
Youssef, Youssef M. [1 ]
Azab, Mohammad E. [1 ]
Elsayed, Galal A. [1 ]
El-Sayed, Amira A. [1 ]
El-Helw, Eman A. E. [1 ]
机构
[1] Ain Shams Univ, Fac Sci, Dept Chem, Cairo 11566, Egypt
关键词
Antiproliferative; oxazolone; triazinone; pyrazole; triazole thione; RAPID COLORIMETRIC ASSAY; PYRAZOLE DERIVATIVES; ANTITUMOR; SYSTEMS; INHIBITION; SURVIVAL; SCAFFOLD; GROWTH; ACID;
D O I
10.1080/10406638.2022.2130373
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A new series of pyrazole derivatives was synthesized starting from the pyrazole-based oxazolone derivative 3. The activity of compound 3 toward some mono- and bidentate nucleophiles was investigated. Some of the synthesized compounds were screened for their antiproliferative activity against colon and breast cancer cell lines. The results of the biological assay revealed that the triazinone derivative 13 was the most potent against the two HCT116 and MCF7 cell lines since it showed IC50 = 8.37 +/- 0.5 mu M and 3.81 +/- 0.2 mu M, respectively, as compared to the reference drug doxorubicin (IC50 = 5.23 +/- 0.3 and 4.17 +/- 0.2 mu M, respectively).
引用
收藏
页码:7152 / 7163
页数:12
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