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- Title
2, 4, 5‐Trideoxyhexopyranosides derivatives of diphyllin: Synthesis and anticancer activity.
- Authors
Cai, Rui; Li, Yu; Zhu, Li; Wei, Caiyan; Bao, Xiaofeng; Zhao, Yu
- Abstract
Diphyllin and its natural derivatives were identified as potent vacuolar H+‐ATPase (V‐ATPase) inhibitors. In this study, twelve 2, 4, 5‐trideoxyhexopyranosides derivatives of diphyllin were synthesized. Most of these compounds showed potent abilities to inhibit the growth of HT‐29, MCF‐7, HepG2 cancer cells with IC50 values at submicromolar concentration. The compounds 5c3 and 5c4 showed the best inhibitory activity on breast cancer cell lines MCF‐7 with IC50 values of 0.09 and 0.10 μM. Compounds 5c3 and 5c4 showed similar V‐ATPase inhibitory potency to diphyllin. Molecular docking showed that a hydrogen bond was found between the hydroxyl of 5c3 and SerA534 in the pocket of the V‐ATPase receptor.
- Subjects
ANTINEOPLASTIC agents; MOLECULAR docking; CANCER cells; HYDROGEN bonding; CELL lines
- Publication
Chemical Biology & Drug Design, 2022, Vol 100, Issue 2, p256
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.14095