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Synthesis and Evaluation of 2‐Alkylthio‐4‐(N‐substituted sulfonamide)pyrimidine Hydroxamic Acids as Anti‐myeloma Agents |
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| Authors: | Jinbao Xiang Crystal Leung Zhuoqi Zhang Cassie Hu Chao Geng Lili Liu Lang Yi Zhiwei Li James Berenson Xu Bai |
| Affiliation: | 1. The Center for Combinatorial Chemistry and Drug Discovery, The School of Pharmaceutical Sciences, The College of Chemistry, Jilin University, Changchun, Jilin, China;2. Institute for Myeloma & Bone Cancer Research, West Hollywood, CA, USA;3. Changchun Discovery Sciences, Ltd., Changchun, Jilin, 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 |