AI Article Synopsis
- HIF-1α is frequently overexpressed in tumors and is crucial for how tumor cells respond to low oxygen levels, making its inhibitors potential cancer treatments.
- Two series of panaxadiol (PD) ester derivatives with pyrazole and pyrrole groups were developed and tested for their HIF-1α inhibitory effects.
- Compounds 18c, 19d, and 19n demonstrated stronger HIF-1α inhibition compared to the original PD, without showing cytotoxicity, suggesting they could serve as promising leads for further drug development.
Article Abstract
Hypoxia-inducing factor-1α (HIF-1α) is overexpressed in variety of tumor patients and plays an important role in the regulation of hypoxia response in tumor cells. Therefore, its inhibitors have become one of the targets for the treatment of a variety of cancers. Two series of panaxadiol (PD) ester derivatives containing pyrazole (18a-j) and pyrrole (19a-n) moiety were synthesized and their HIF-1α inhibitory activities were evaluated. Among all the target compouds, compounds 18c, 19d, and 19n (IC = 8.70-10.44 μM) showed better HIF-1α inhibitory activity than PD (IC = 13.35 μM). None of these compounds showed cytotoxicity above 100 μM and inhibited HIF-1α transcription in a dose-dependent manner. These compounds showed good antitumor activity and provide lead compounds for further design and activity study of PD ester derivatives.
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| http://dx.doi.org/10.1016/j.fitote.2024.106052 | DOI Listing |
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