Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 59, Issue 18, Pages 8276-8292Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.6b00547
Keywords
-
Categories
Funding
- INSERM
- CNRS
- University of Nice Sophia Antipolis
- INSERM Transfert (COPOC grant)
- Canceropole PACA
- ARC [SFI 20121205378]
- contrat INSERM Transfert [INSERM U1065]
Ask authors/readers for more resources
Cancer is the second cause of deaths worldwide and is forecasted to affect more that 22 million people in 2020. Despite dramatic improvement in its care over the last two decades, the treatment of resistant forms of cancer is still an unmet challenge. Thus, innovative and efficient treatments are still needed. In this context, we report herein the synthesis and the evaluation of a new class of bioactive molecules belonging to the N-(4-(3-aminophenyl(thiazol-2-yl)acetamide family. Structure-activity relationships could be driven and resulted in the discovery of lead compound 6b. The latter display high in vitro potency against both sensitive and resistant cancer cell lines on three models: melanoma, pancreatic cancer, and chronic myeloid leukemia (CML). 6b leads to cell death by concomitant induction of apoptosis and autophagy, shows good pharmacokinetic properties, and demonstrates a significant reduction of tumor growth in vivo on A375 xenograft model in mice.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available