Modular Synthesis and Antiproliferative Activity of New Dihydro-1<i>H</i>-pyrazolo[1,3-<i>b</i>]pyridine Embelin Derivatives
A set of new dihydro-1<i>H</i>-pyrazolo[1,3-<i>b</i>]pyridine and pyrazolo[1,3-<i>b</i>]pyridine embelin derivatives was synthesized through a multicomponent reaction from natural embelin, 3-substituted-5-aminopyrazoles and aldehydes. The synthesized compounds wer...
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| Main Authors: | , , , , , |
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| Format: | Book |
| Published: |
MDPI AG,
2021-10-01T00:00:00Z.
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| Summary: | A set of new dihydro-1<i>H</i>-pyrazolo[1,3-<i>b</i>]pyridine and pyrazolo[1,3-<i>b</i>]pyridine embelin derivatives was synthesized through a multicomponent reaction from natural embelin, 3-substituted-5-aminopyrazoles and aldehydes. The synthesized compounds were evaluated against three hematologic tumor cell lines, HEL (acute erythroid leukemia), K-562 (chronic myeloid leukemia) and HL-60 (acute myeloid leukemia), and five breast cancer cell lines (SKBR3, MCF-7, MDA-MB-231, BT-549, HS-578T). The primate non-malignant kidney Vero cell line was used as the control of cytotoxicity. From the obtained results, some structure-activity relationships were outlined. Furthermore, in silico prediction of physicochemical properties and ADME parameters were determined for the derivatives with the best antiproliferative values. |
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| Item Description: | 10.3390/ph14101026 1424-8247 |