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

被引：4

作者：

Xiang, Jinbao ^{[1
]}

Leung, Crystal ^{[2
]}

Zhang, Zhuoqi ^{[1
]}

Hu, Cassie ^{[2
]}

Geng, Chao ^{[1
]}

Liu, Lili ^{[3
]}

Yi, Lang ^{[1
]}

Li, Zhiwei ^{[1
]}

Berenson, James ^{[2
]}

Bai, Xu ^{[1
]}

机构：

[1] Jilin Univ, Coll Chem, Sch Pharmaceut Sci, Ctr Combinatorial Chem & Drug Discovery, 1266 Fujin Rd, Changchun 130021, Jilin, Peoples R China

[2] Inst Myeloma & Bone Canc Res, 9201 West Sunset Blvd,Suite 300, West Hollywood, CA 90069 USA

[3] Changchun Discovery Sci Ltd, 750 Jinbi St, Changchun 130117, Jilin, Peoples R China

来源：

CHEMICAL BIOLOGY & DRUG DESIGN | 2016年 / 87卷 / 03期

基金：

中国国家自然科学基金;

关键词：

anti-cancer activity; apoptosis; histone acetylation; multiple myeloma; pyrimidine hydroxamic acid; sulfide substituent; HISTONE DEACETYLASE INHIBITORS; POT 3-COMPONENT CONDENSATION; SMILES REARRANGEMENT; MULTIPLE-MYELOMA; IMINIUM CYCLIZATION; CASCADE REACTION; DESIGN; DIHYDROPTERIDINES; DERIVATIVES; DISCOVERY;

D O I：

10.1111/cbdd.12678

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：472 / 477

页数：6

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