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Design, Synthesis and Evaluation of Novel Rhodanine‐containing Sorafenib Analogs as Potential Antitumor Agents
Author(s) -
Li Wei,
Zhai Xin,
Zhong Zheng,
Li Guangyue,
Pu Yongxiao,
Gong Ping
Publication year - 2011
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201000326
Subject(s) - rhodanine , sorafenib , chemistry , in vitro , cancer cell lines , combinatorial chemistry , a549 cell , cell culture , stereochemistry , pharmacology , biochemistry , cancer cell , cancer , cancer research , biology , genetics , hepatocellular carcinoma
A series of rhodanine‐containing sorafenib analogs was designed, synthesized and evaluated for their in‐vitro antitumor activity against three cancer cell lines (A549, H460 and HT29). Pharmacological data indicated that some of the target compounds possessed marked antiproliferative activity superior to the reference drug sorafenib, especially the most promising compound 7r (with the IC 50 value of 0.8, 1.3 and 2.8 µM against A549, H460 and HT29 cell lines, respectively). The activity was found to strongly depend on the substitution pattern of the rhodanine motif at C‐5″ position. Results suggested that this series of compounds could serve as the bases for the development of novel antitumor agents.