A new simple and high-yield synthesis of suberoylanilide hydroxamic acid and its inhibitory effect alone or in combination with retinoids on proliferation of human prostate cancer cells.

Lalji K Gediya, Pankaj Chopra, Puranik Purushottamachar, Neha Maheshwari, Vincent C O Njar

Journal: Journal of medicinal chemistry 2005;48(15):5047-51

PMID: 16033284

Full Text on American Chemical Society View on PubMed

Abstract

We have developed a procedure for the synthesis of N-hydroxy-N(1)-phenyloctanediamide (suberoylanilide hydroxamic acid (SAHA)), providing the product in 79.8% yield. SAHA is a potent inhibitor of histone deacetylase, induces differentiation and/or apoptosis in certain transformed cells in culture, and suppressed the growth of human prostate cancer LNCaP and PC-3 cell lines. The combination of SAHA with other compounds inhibited cell proliferation of LNCaP cells in additive fashion and resulted in synergistic growth inhibition.

Address: Department of Pharmacology and Experimental Therapeutics, University of Maryland School of Medicine, 655 West Baltimore Street, Baltimore, Maryland 21201-1559, USA.

DOI: 10.1021/jm058214k

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https://doi.org/10.1021/jm058214k

MeSH Terms: Antineoplastic Agents, Cell Line, Tumor, Cell Proliferation, Drug Synergism, Histone Deacetylase Inhibitors, Humans, Hydroxamic Acids, Male, Prostatic Neoplasms, Retinoids, Vorinostat