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Design and Synthesis of 2‐Iminothiazolidin‐4‐one Moiety‐Containing Compounds as Potent Antiproliferative Agents
Author(s) -
Zhai Xin,
Li Wei,
Chen Dong,
Lai Ruiwei,
Liu Jun,
Gong Ping
Publication year - 2012
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.201100064
Subject(s) - chemistry , moiety , mtt assay , stereochemistry , sorafenib , a549 cell , cell culture , structure–activity relationship , cancer cell lines , lead compound , cytotoxicity , combinatorial chemistry , cell growth , pharmacology , in vitro , biochemistry , cancer cell , cancer , biology , cancer research , genetics , hepatocellular carcinoma
A new series of 2,5‐diaryliminothiazolidin‐4‐ones were designed and synthesized as potent antiproliferative agents. The antiproliferative activities of the 25 target compounds were evaluated against three cancer cell lines (A549, H460 and HT29) by MTT assay. Pharmacological data indicated that most of the compounds possessed moderate activity, some showed remarkable activity against one or more cell lines. As the most promising compound, 8s (with IC 50 values of 1.1, 0.01 and 1.3 µM against the A549, H460 and HT29 cell lines) was 1.1‐ to 270‐fold more potent than the reference drug sorafenib. Furthermore, preliminary structure–activity relationships (SARs) were summarized to provide guidance for further design and discovery of 2‐iminothiazolidin‐4‐one‐based antiproliferative agents.