Abstract
Novel functionalized quaternary ammonium curcuminoids have been synthesized from piperazinyl curcuminoids and Baylis-Hillman reaction derived allyl bromides. These molecules are found to be highly water soluble with increased cytotoxicity compared to native curcumin against three cancer cell lines MIAPaCa-2, MDA-MB-231, and 4T1. Preliminary in vivo toxicity evaluation of a representative curcuminoid 5a in healthy mice indicates that this molecule is well tolerated based on normal body weight gains compared to control group. Furthermore, the efficacy of 5a has been tested in a pancreatic cancer xenograft model of MIAPaCa-2 and has been found to exhibit good tumor growth inhibition as a single agent and also in combination with clinical pancreatic cancer drug gemcitabine.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 5777-5780 |
| Number of pages | 4 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 25 |
| Issue number | 24 |
| DOIs | |
| State | Published - Dec 15 2015 |
Bibliographical note
Funding Information:This work was supported by Whiteside Clinical Research Institute , Duluth, Minnesota and University of Minnesota Duluth .
Publisher Copyright:
© 2015 Elsevier Ltd.
Copyright:
Copyright 2015 Elsevier B.V., All rights reserved.
UN SDGs
This output contributes to the following UN Sustainable Development Goals (SDGs)
-
SDG 3 Good Health and Well-being
Keywords
- Baylis-Hillman derived allyl bromides
- Breast cancer
- Curcuminoids
- Pancreatic cancer
- Quaternary ammonium salts
Fingerprint
Dive into the research topics of 'Synthesis, in vitro, and in vivo evaluation of novel functionalized quaternary ammonium curcuminoids as potential anti-cancer agents'. Together they form a unique fingerprint.Cite this
- APA
- Standard
- Harvard
- Vancouver
- Author
- BIBTEX
- RIS