Synthesis and Antiproliferative Screening of Some Heterocycles Derived from 4-((5-Chloro-3-Methyl-1-Phenyl-1 <i>H</i> -Pyrazol-4-yl)Methylene)-2-Phenyloxazol-5(4 <i>H</i> )-One
Youssef M. Youssef, Mohammad E. Azab, Galal A. Elsayed, Amira A. El‐Sayed, Eman A. E. El‐Helw
Abstract
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 µM and 3.81 ± 0.2 µM, respectively, as compared to the reference drug doxorubicin (IC50 = 5.23 ± 0.3 and 4.17 ± 0.2 µM, respectively).
Topics & Concepts
ChemistryPyrazoleOxazoloneMethyleneIC50StereochemistryDerivative (finance)DoxorubicinCombinatorial chemistryMedicinal chemistryIn vitroOrganic chemistryBiochemistryChemotherapyEconomicsSurgeryMedicineFinancial economicsSynthesis and Reactions of Organic CompoundsBioactive Compounds and Antitumor AgentsSynthesis and biological activity