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
Youssef, YM; Azab, ME; Elsayed, GA; El-Sayed, AA; El-Helw, EAE;
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).
Other data
Title | 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 | Authors | Youssef, YM; Azab, ME; Elsayed, GA; El-Sayed, AA; El-Helw, EAE | Keywords | Antiproliferative;oxazolone;triazinone;pyrazole;triazole thione;RAPID COLORIMETRIC ASSAY;PYRAZOLE DERIVATIVES;ANTITUMOR;SYSTEMS;INHIBITION;SURVIVAL;SCAFFOLD;GROWTH;ACID | Issue Date | 2022 | Publisher | TAYLOR & FRANCIS LTD | Journal | Polycyclic Aromatic Compounds | ISSN | 1040-6638 | DOI | 10.1080/10406638.2022.2130373 | Scopus ID | 2-s2.0-85139785001 | Web of science ID | WOS:000866068100001 |
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