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Spectral Characteristic and Preliminary Anticancer Activity in vitro of Selected Rhodanine‐3‐carboxylic Acids Derivatives
Author(s) -
Stawoska Iwona,
Tejchman Waldemar,
Mazuryk Olga,
Lyčka Antonín,
NowakSliwinska Patrycja,
Żesławska Ewa,
Nitek Wojciech,
Kania Agnieszka
Publication year - 2017
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.2897
Subject(s) - rhodanine , chemistry , linker , in vitro , carboxylic acid , quenching (fluorescence) , combinatorial chemistry , nitrogen atom , stereochemistry , fluorescence , ring (chemistry) , organic chemistry , biochemistry , physics , quantum mechanics , computer science , operating system
Selected rhodanine‐3‐carboxylic acids derivatives were synthesized to determine the influence of the structure and the length of the linker between the carboxyl group and the nitrogen atom (N‐3) in the 2‐thioxo‐4‐thiazolidinone ring on their activity, monitored via interactions with human serum albumin. Based on fluorescence studies, we concluded that the length of the linker has a limited impact on these interactions. Additionally, we proposed the static mechanism of quenching for all the tested compounds. These derivatives seem to possess an anticancer activity in the nanomolar range with 3 as the most potent compound in both A2780 and A2780cisR cell lines.