Premium
Novel Symmetrical trans ‐Bis‐Schiff Bases of N ‐Substituted‐4‐ piperidones: Synthesis, Characterization, and Preliminary Antileukemia Activity Mensurations
Author(s) -
Sun ChuanWen,
Wang HaiFeng,
Zhu Jun,
Yang DingRong,
Xing Jiahua,
Jin Jia
Publication year - 2013
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.916
Subject(s) - chemistry , stereochemistry , k562 cells , ic50 , tumor cells , characterization (materials science) , combinatorial chemistry , cell , in vitro , nanotechnology , biochemistry , cancer research , biology , materials science
A series of novel symmetrical trans ‐bis‐Schiff bases ( 11a , 11b , 11c , 11d , 11e , 11f , 11g , 11h , 11i , 11j , 11k , 11l , 11m ) were designed and prepared as novel anticancer analogues, with the trans ‐configuration confirmed by X‐ray diffraction. Preliminary inhibitory effects of these compounds on CML K562 cell growth were investigated, and the potential analogue 11e showed an excellent anti‐leukemia activity (IC 50 =6.35 μg/mL), which is higher than that of the clinical drug 5‐fluorouracil (IC 50 =8.48 μg/mL). Complete assignments had been achieved for the title compounds by spectroscopic techniques, and their structure–activity relationships have been studied.