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Synthesis and Evaluation of 2‐Alkylthio‐4‐( N ‐substituted sulfonamide)pyrimidine Hydroxamic Acids as Anti‐myeloma Agents
Author(s) -
Xiang Jinbao,
Leung Crystal,
Zhang Zhuoqi,
Hu Cassie,
Geng Chao,
Liu Lili,
Yi Lang,
Li Zhiwei,
Berenson James,
Bai Xu
Publication year - 2016
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12678
Subject(s) - substituent , sulfonamide , chemistry , pyrimidine , apoptosis , stereochemistry , cell culture , hydroxamic acid , biochemistry , biology , genetics
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.