69739-24-8Relevant academic research and scientific papers
"(3S)- AND (3R)-6,7-BIS(HYDROXYMETHYL)-1H,3H-PYRROLO[1,2-C]THIAZOLES AS P53 ACTIVATORS"
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Page/Page column 15, (2020/01/11)
The present application relates to compounds of formula I, which are (3S)- and (3R)-6,7-bis(Hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles. The present application also relates to pharmaceutical compositions comprising said compounds and the use of these co
Chiral 6,7-bis(hydroxymethyl)-1H,3H-pyrrolo[1,2-c]thiazoles with anti-breast cancer properties
Soares, Maria I.L.,Brito, Ana Filipa,Laranjo, Mafalda,Paixao, Jose A.,Botelho, M.Filomena,Pinho E Melo, Teresa M.V.D.
, p. 254 - 262 (2013/03/29)
The synthesis and biological evaluation of 6,7-bis(hydroxymethyl)-1H,3H- pyrrolo[1,2-c]thiazoles as anticancer agents against MCF7 breast cancer cell lines is reported. The design of the new compounds has been guided considering (3R)-6,7-bis(hydroxymethyl)-5-methyl-3-phenyl-1H,3H-pyrrolo[1,2-c]thiazole as the lead compound due to its good performance against MCF7 breast cancer cell lines (IC50 = 1.0 μM). The structural changes included the removal of the phenyl group at C-3, the replacement of this group by a 3,4,5-trimethoxyphenyl group, the removal of the methyl group at C-5 from the lead scaffold and the replacement of this group by a phenyl substituent. Overall, these studies showed that the combined presence of a phenyl group at C-3 and a methyl group at C-5 in the 1H,3H-pyrrolo[1,2-c]thiazole ring system is essential to ensure high cytotoxicty against MCF7 breast cancer cell lines. To probe whether the absolute configuration of the lead compound might affect the anticancer activity, its enantiomer was prepared and the activity against MCF7 cells was evaluated. (3S)-6,7-Bis(hydroxymethyl)-5-methyl-3-phenyl-1H,3H- pyrrolo[1,2-c]thiazole proved to be the most active compound so far studied, with IC50 value of 0.5 μM.
Conformational analysis, spectral and catalytic properties of 1,3-thiazolidines, ligands for acetophenone hydrosilylation with diphenylsilane
Skvortsov,Uvarov,De Vekki,Studentsov,Skvortsov
scheme or table, p. 2007 - 2021 (2011/02/18)
2-Aryl- and 2-furyl-4-carboxy-1,3-thiazolidines were synthesized. Their spectral properties were studied, and conformational analysis was performed. It was shown that they exist in solution as an equilibrium of neutral and zwitter-ion forms. The influence
