81154-08-7Relevant academic research and scientific papers
A facile synthesis of (Z)-5-(substituted)-2-(methylthio)thiazol-4(5H)-one using microwave irradiation and conventional method
Pansare, Dattatraya N.,Shinde, Devanand B.
, p. 1107 - 1110 (2014)
A new effective approach to the synthesis of some new (Z)-5-(substituted)- 2-thioxothiazolidin-4-one 3a-l and (Z)-5-(substituted)-2-(methylthio)thiazol- 4(5H)-one 5a-l is reported under microwave irradiation as well as conventional conditions.
Copper(II)-complex functionalized magnetite nanoparticles: a highly efficient heterogeneous nanocatalyst for the synthesis of 5-arylidenthiazolidine-2,4-diones and 5-arylidene-2-thioxothiazolidin-4-one
Akhavan, Malihe,Foroughifar, Naser,Pasdar, Hoda,Khajeh-Amiri, Alireza,Bekhradnia, Ahmadreza
, p. 543 - 552 (2017/08/15)
Abstract: Magnetite nanoparticles (MNPs) have proved to be a useful support for heterogeneous catalysis. We have synthesized Fe3O4 MNPs functionalized with a copper(II) complex, and tested the resulting material as a heterogeneous nanocatalyst. The catalyst was tested for aldol condensation reactions between aliphatic/aromatic aldehydes and rhodanine or thiazolidine-2,4-dione (TZD) derivatives under reflux in ethanol, giving the target products in high yield. Environmentally benign chemistry, short reaction times, simple work-up, excellent yields, and the reusability of the new nanocatalyst are beneficial features of the present study. The nanocatalyst was characterized by scanning electron microscopy, vibrating sample magnetometery, thermogravimetry, X-ray diffraction, and energy-dispersive X-ray analyses. The data showed that the magnetic nanoparticles are super-paramagnetic with a size range of 10–20?nm. Graphical Abstract: [Figure not available: see fulltext.].
Thiazolidine derivatives as potent and selective inhibitors of the PIM kinase family
Bataille, Carole J.R.,Brennan, Méabh B.,Byrne, Simon,Davies, Stephen G.,Durbin, Matthew,Fedorov, Oleg,Huber, Kilian V.M.,Jones, Alan M.,Knapp, Stefan,Liu, Gu,Nadali, Anna,Quevedo, Camilo E.,Russell, Angela J.,Walker, Roderick G.,Westwood, Robert,Wynne, Graham M.
supporting information, p. 2657 - 2665 (2017/04/06)
The PIM family of serine/threonine kinases have become an attractive target for anti-cancer drug development, particularly for certain hematological malignancies. Here, we describe the discovery of a series of inhibitors of the PIM kinase family using a high throughput screening strategy. Through a combination of molecular modeling and optimization studies, the intrinsic potencies and molecular properties of this series of compounds was significantly improved. An excellent pan-PIM isoform inhibition profile was observed across the series, while optimized examples show good selectivity over other kinases. Two PIM-expressing leukemic cancer cell lines, MV4-11 and K562, were employed to evaluate the in vitro anti-proliferative effects of selected inhibitors. Encouraging activities were observed for many examples, with the best example (44) giving an IC50 of 0.75 μM against the K562 cell line. These data provide a promising starting point for further development of this series as a new cancer therapy through PIM kinase inhibition.
A facile synthesis of (Z)-5-(substituted)-2-(methylthio)thiazol-4(5H)-one using microwave irradiation and conventional method
Pansare, Dattatraya N.,Shinde, Devanand B.
, p. 1107 - 1110 (2015/02/19)
A new effective approach to the synthesis of some new (Z)-5-(substituted)-2-thioxothiazolidin-4-one 3a-l and (Z)-5-(substituted)-2-(methylthio)thiazol-4(5H)-one 5a-l is reported under microwave irradiation as well as conventional conditions.
Structure-based design of rhodanine-based acylsulfonamide derivatives as antagonists of the anti-apoptotic Bcl-2 protein
Li, Huan-Qiu,Yang, Jing,Ma, Shuhua,Qiao, Chunhua
experimental part, p. 4194 - 4200 (2012/08/28)
A series of novel rhodanine-based acylsulfonamide derivatives were designed, synthesized, and evaluated as small-molecule inhibitors of anti-apoptotic Bcl-2 protein. These compounds exhibit potent antiproliferative activity in three human tumor cell lines
Synthesis and characterization of (Z)-5-arylmethylidenerhodanines with photosynthesis-inhibiting properties
Opletalova, Veronika,Dolezel, Jan,Kralova, Katarina,Pesko, Matus,Kunes, Jiri,Jampilek, Josef
experimental part, p. 5207 - 5227 (2011/08/06)
A series of rhodanine derivatives was prepared. The synthetic approach, analytical and spectroscopic data of all synthesized compounds are presented. Lipophilicity of all the discussed rhodanine derivatives was analyzed using the RP-HPLC method. The compo
