SYNTHESIS OF NEW ADAMANTANE DERIVATIVES OF PYRAZOLO[3,4-d] PYRIMIDINE AS POTENTIAL ANTICANCER DRUGS
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2026
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| _version_ | 1866901911998824448 |
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| author | Klimko Yu. Koshchii I. |
| author_facet | Klimko Yu. Koshchii I. |
| contents | <p class="MsoNormal"><strong><span>Abstract</span></strong></p> <p class="MsoNormal"><span>Four new pyrazolo[3,4-d]pyrimidines (4)–(7) were successfully synthesized in good yields by reacting 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ol with various alkylating agents (methyl iodide, tert-benzyl bromide, benzyl chloride,) at room temperature in DMF using liquid-solid phase transfer catalysis. The structures of (4)–(7) were proven by NMR spectroscopy. The anticancer activities of (4)–(7) against human colorectal carcinoma (HCT 116), human hepatocellular carcinoma (HepG2), and human breast cancer (MCF-7) cell lines, as well as one normal cell line (WI38) were investigated using MTT assay and sunitinib as a reference. Compounds (4) and (5) exhibited anticancer activity comparable to the reference drug against all tested cells, with an IC50 range of 22.7–40.75 μM. Both compounds also demonstrated high selectivity indices and minimal cytotoxic effects on normal cell lines.</span></p> <p class="MsoNormal"> </p> |
| format | Recurso digital |
| id | zenodo_https___doi_org_10_5281_zenodo_19922882 |
| institution | Zenodo |
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| publishDate | 2026 |
| publisher | Zenodo |
| record_format | zenodo |
| spellingShingle | SYNTHESIS OF NEW ADAMANTANE DERIVATIVES OF PYRAZOLO[3,4-d] PYRIMIDINE AS POTENTIAL ANTICANCER DRUGS Klimko Yu. Koshchii I. pyrazolopyrimidines, adamantane,, anticancer activity, alkylating agents <p class="MsoNormal"><strong><span>Abstract</span></strong></p> <p class="MsoNormal"><span>Four new pyrazolo[3,4-d]pyrimidines (4)–(7) were successfully synthesized in good yields by reacting 3-methyl-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ol with various alkylating agents (methyl iodide, tert-benzyl bromide, benzyl chloride,) at room temperature in DMF using liquid-solid phase transfer catalysis. The structures of (4)–(7) were proven by NMR spectroscopy. The anticancer activities of (4)–(7) against human colorectal carcinoma (HCT 116), human hepatocellular carcinoma (HepG2), and human breast cancer (MCF-7) cell lines, as well as one normal cell line (WI38) were investigated using MTT assay and sunitinib as a reference. Compounds (4) and (5) exhibited anticancer activity comparable to the reference drug against all tested cells, with an IC50 range of 22.7–40.75 μM. Both compounds also demonstrated high selectivity indices and minimal cytotoxic effects on normal cell lines.</span></p> <p class="MsoNormal"> </p> |
| title | SYNTHESIS OF NEW ADAMANTANE DERIVATIVES OF PYRAZOLO[3,4-d] PYRIMIDINE AS POTENTIAL ANTICANCER DRUGS |
| topic | pyrazolopyrimidines, adamantane,, anticancer activity, alkylating agents |
| url | https://doi.org/10.5281/zenodo.19922882 |