Isoquinoline thiosemicarbazone displays potent anticancer activity with in vivo efficacy against aggressive leukemias

Author:

Sun Daniel L.12342,Poddar Soumya12342,Pan Roy D.12342ORCID,Rosser Ethan W.12342ORCID,Abt Evan R.12342,Van Valkenburgh Juno12342,Le Thuc M.12342,Lok Vincent123,Hernandez Selena P.523,Song Janet123,Li Joanna123,Turlik Aneta523,Chen Xiaohong523,Cheng Chi-An52362ORCID,Chen Wei523,Mona Christine E.12342,Stuparu Andreea D.12342,Vergnes Laurent7823,Reue Karen78239,Damoiseaux Robert102113,Zink Jeffrey I.523ORCID,Czernin Johannes12342,Donahue Timothy R.12342,Houk Kendall N.523ORCID,Jung Michael E.523,Radu Caius G.12342ORCID

Affiliation:

1. Department of Molecular and Medical Pharmacology

2. University of California, Los Angeles

3. USA

4. Ahmanson Translational Imaging Division

5. Department of Chemistry and Biochemistry

6. Department of Bioengineering

7. Department of Human Genetics

8. David Geffen School of Medicine

9. Molecular Biology Institute

10. UCLA Metabolomic Center

11. Los Angeles

Abstract

Potent α-N-heterocyclic carboxaldehyde thiosemicarbazone (HCT) antiproliferatives were synthesized through iterative rounds of methylation and fluorination modifications, with anticancer activities being potentiated by physiological levels of copper.

Funder

National Cancer Institute

National Science Foundation

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

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