title: Synthesis and Evaluation of 2-Alkylthio-4-(N-substituted sulfonamide)pyrimidine Hydroxamic Acids as Anti-myeloma Agents.
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.
authors.affiliation: 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.
authors.forename: Jinbao
authors.initials: J
authors.lastname: Xiang
authors.affiliation: Institute for Myeloma & Bone Cancer Research, 9201 West Sunset Blvd, Suite 300, West Hollywood, CA, 90069, USA.
authors.forename: Crystal
authors.initials: C
authors.lastname: Leung
authors.affiliation: 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.
authors.forename: Zhuoqi
authors.initials: Z
authors.lastname: Zhang
authors.affiliation: Institute for Myeloma & Bone Cancer Research, 9201 West Sunset Blvd, Suite 300, West Hollywood, CA, 90069, USA.
authors.forename: Cassie
authors.initials: C
authors.lastname: Hu
authors.affiliation: 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.
authors.forename: Chao
authors.initials: C
authors.lastname: Geng
authors.affiliation: Changchun Discovery Sciences, Ltd., 750 Jinbi Street, Changchun, Jilin, 130117, China.
authors.forename: Lili
authors.initials: L
authors.lastname: Liu
authors.affiliation: 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.
authors.forename: Lang
authors.initials: L
authors.lastname: Yi
authors.affiliation: 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.
authors.forename: Zhiwei
authors.initials: Z
authors.lastname: Li
authors.affiliation: Institute for Myeloma & Bone Cancer Research, 9201 West Sunset Blvd, Suite 300, West Hollywood, CA, 90069, USA.
authors.forename: James
authors.initials: J
authors.lastname: Berenson
authors.affiliation: 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.
authors.forename: Xu
authors.initials: X
authors.lastname: Bai
mesh_terms: D000970:Antineoplastic Agents / Q000627:therapeutic use*; D006801:Humans; D006877:Hydroxamic Acids / Q000737:chemistry*; D009101:Multiple Myeloma / Q000188:drug therapy*; D011743:Pyrimidines / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D006877:Hydroxamic Acids; D011743:Pyrimidines; C030986:pyrimidine
keywords: anti-cancer activity; apoptosis; histone acetylation; multiple myeloma; pyrimidine hydroxamic acid; sulfide substituent