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Semi-synthesis and anti-tumor activity of novel 25-OCH3-PPD derivatives incorporating aromatic moiety.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Jan2019, Vol. 29 Issue 2, p189-193. 5p. - Publication Year :
- 2019
-
Abstract
- Graphical abstract Highlights • A series of novel 25-OCH 3 -PPD derivatives were synthesized. • Cytotoxic activities of the derivatives were evaluated on five human tumor cell lines. • Compounds 3a , 14a and 18a exhibited strong anti-tumor activities. • Having aromatic ester at the C3 position could enhance the antiproliferative activities. Abstract Previously we have reported that 25-OCH 3 -PPD could suppress the reproduction of cancer cells and cause apoptosis without obvious toxicity. Herein, we aimed to enhance its bioactivity by introducing aromatic groups to its dammarane-type skeleton. These synthesized derivatives were tested for their inhibitory activities against five cancer cell lines. Of them, compounds 3a , 14a and 18a had the strongest antiproliferative activities against tumor cells (IC 50 < 15 µM, 5-fold to 10-fold increases than 25-OCH 3 -PPD). Especially compound 14a displayed the most potent activity against DU145, MCF-7 and HepG2 cells (IC 50 = 6.7 ± 0.8, 4.3 ± 0.8 and 5.8 ± 0.6 µM, respectively). Structure-activity relationships demonstrated that having aromatic ester at the C3 position could improve the bioactivity. The data provided new insights into exploring novel antiproliferative lead compounds. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 29
- Issue :
- 2
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 133781115
- Full Text :
- https://doi.org/10.1016/j.bmcl.2018.12.003