1217510-14-9Relevant articles and documents
X-ray crystal structures and anti-breast cancer property of 3-tert -butoxycarbonyl-2-arylthiazolidine-4-carboxylic acids
Jagtap, Rohidas M.,Thorat, Shridhar H.,Gonnade, Rajesh G.,Khan, Ayesha A.,Pardeshi, Satish K.
, p. 1078 - 1086 (2018/02/06)
Diastereomeric '2RS,4R'-2-arylthiazolidine-4-carboxylic acids (ATCAs) were synthesized and their resolution to chiraly pure N-BOC derivatives was attempted by column chromatography. The absolute stereochemistry of the resolved compounds was ascertained by X-ray single crystal structures. Further application of the synthesized compounds was studied for their in vitro anti-breast cancer activity against MCF7 cell line using DOX as a standard by MTT assay method. Cell morphology analysis was carried out by fluorescence microscopy. The compounds containing '2S' absolute configuration in thiazolidine ring and presence of 2-NO2, 2,6-Cl groups on '2R'-aryl substituent showed significant anti-breast cancer activity where some of the compounds were found to be more active than DOX in terms of induced apoptosis mode of MCF7 cell death.
Design, synthesis of 4-aminoquinoline-derived thiazolidines and their antimalarial activity and heme polymerization inhibition studies
Solomon, V. Raja,Haq,Srivastava, Kumkum,Puri, Sunil K.,Katti
, p. 619 - 626 (2013/05/09)
The present study describes the synthesis of a series of new 4-aminoquinoline-derived thiazolidines and evaluation of their antimalarial activity against a NF-54 strain of Plasmodium falciparum in vitro and N-67 strain of Plasmodium yoelii in vivo. Among the series, two compounds, 2-(4-chloro-phenyl)-thiazolidine-4-carboxylic acid [2-(7-chloro-quinolin-4- ylamino)-ethyl]-amide hydrochloride (14) and 2-(2,6-dichloro-phenyl)- thiazolidine-4-carboxylic acid [2-(7-chloro-quinolin-4-ylamino)-ethyl]-amide hydrochloride (22) exhibited significant suppression of parasitaemia in the in vivo assay. All the analogues were found to form strong complex with haematin and inhibited the β-haematin formation in vitro. These results suggest that these compounds act on heme polymerization target.