Apoptotic activity of substituted 3-O-acetyl-betulinic acid benzylamides
Acetylated betulinic acid (BA) was converted into mono-substituted benzylamides 2-14. Screening in SRB assays showed them as cytotoxic for a variety of different human tumor cell lines. While parent BA was not cytotoxic within the limits of the assay (cut-off 30 μM), the target amides were cytotoxi...
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| Main Authors: | , , , , , |
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| Format: | Book |
| Published: |
Elsevier,
2021-12-01T00:00:00Z.
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| Summary: | Acetylated betulinic acid (BA) was converted into mono-substituted benzylamides 2-14. Screening in SRB assays showed them as cytotoxic for a variety of different human tumor cell lines. While parent BA was not cytotoxic within the limits of the assay (cut-off 30 μM), the target amides were cytotoxic. Their bioactivity as well as their tumor cell/non-tumor cell selectivity depended on the substitution pattern of the aromatic ring. The most active compound 9 (holding an ortho methoxy substituent) acted mainly by apoptosis. |
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| Item Description: | 2772-4174 10.1016/j.ejmcr.2021.100016 |