In this paper we report the chemical structures of novel derivatives of 3-methyl-4- thiorhodanine which are different in substituents and structures of carbon side chain. Furthermore, in vitro anticancer activity as well as the structure - activity relationships are described. | TAÏP CHÍ PHAÙT TRIEÅN KH&CN, TAÄP 18, SOÁ T1 - 2015 Biological test against breast adenocarcinoma cells (MCF-7) of acylated products of 3-methyl-4 thiorhodanine Lê Hoàng Giàu Nguyễn Tô Nhã Ngô Thị Thùy Dương Tôn Thất Quang Nguyễn Kim Phi Phụng University of Science, VNU-HCM Phạm Nguyễn Kim Tuyến Sai Gon University Fritz Duus Roskilde University, Denmark (Received on January 5 th 2015, accepted on June 22 th 2015) ABSTRACT Rhodanine and its derivatives are not only valued for their interesting chemical properties but also present a wide range of bioactivities and their chemical and pharmacological applications have been investigated. From 3-methyl-4-thiorhodanine we synthesized S-acylated and C-acylated products using (some) carboxylic acid chlorides and the obtained products were studied the anti-proliferative activity by a SRB (sulforhodamine B) assay against a human breast cancer cell line. The results showed that C-acylated products are better inhibitors than S-acylated products. Key words: 3-methyl-4-thiorhodanine, 2-thioxo-1,3-thiazolane-4-one, C-acylated, S-acylated, breast cancer cell line (MCF-7). INTRODUCTION Rhodanine derivatives have been proven to be attractive compounds due to their outstanding biological activities and have undergone rapid development as anticonvulsant, antibacterial, antiviral, and antidiabetic agents. At the same time, these have also been reported as Hepatitis C virus (HCV) protease inhibitors and used as inhibitors of uridine diphospho-Nacetylmuramate/L-alanine ligase. Recently, substituted rhodanines were investigated for the aggregation inhibitor properties. Rhodanines are classified as nonmutagenic and a long-term study on the clinical effects of the rhodanine-based Epalrestat as an anti-diabetic, demonstrated that it is well tolerated. Additionally, rhodanines have been designed as inhibitors of various enzymes such as bacterial -lactamase and Mur ligases. Rhodanine derivatives were found to have marked .
