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Chem Biol Drug Des. 2016 Mar;87(3):472-7. doi: 10.1111/cbdd.12678. Epub 2015 Dec 10.

Synthesis and Evaluation of 2-Alkylthio-4-(N-substituted sulfonamide)pyrimidine Hydroxamic Acids as Anti-myeloma Agents.

Author information

1
The Center for Combinatorial Chemistry and Drug Discovery, The School of Pharmaceutical Sciences, The College of Chemistry, Jilin University, 1266 Fujin Road, Changchun, Jilin, 130021, China.
2
Institute for Myeloma & Bone Cancer Research, 9201 West Sunset Blvd, Suite 300, West Hollywood, CA, 90069, USA.
3
Changchun Discovery Sciences, Ltd., 750 Jinbi Street, Changchun, Jilin, 130117, China.

Abstract

A series of pyrimidine hydroxamic acids with a sulfide substituent at the second position and a sulfonamide substituent at the fourth position have been synthesized and evaluated for their activity against human myeloma cell line RPMI 8226. Several compounds exhibited significant anti-cancer potency. It was found that representative compound 6a selectively killed cancerous but not normal cells. Moreover, compound 6a was effective in causing apoptosis in RPMI 8226 cells and exhibited promising HDAC-inhibitory activities.

KEYWORDS:

anti-cancer activity; apoptosis; histone acetylation; multiple myeloma; pyrimidine hydroxamic acid; sulfide substituent

PMID:
26518472
DOI:
10.1111/cbdd.12678
[Indexed for MEDLINE]

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