317337-07-8Relevant articles and documents
THE LITTLE MOLECULE COMPOUND WHICH USED FOR PROMOTING THE STEM CELLS HYPERPLASIA AND THE USE THEREOF
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Page/Page column 7, (2012/03/12)
The invention provides small molecule compounds capable of accelerating proliferation of stem cells and uses thereof. The compounds play an important role in the research of stem cell proliferation mechanism. The invention further relates to the uses of the compounds and relevant compounds thereof in the preparation of stem cell proliferation accelerators and the preparation of medicines accelerating stem cell proliferation. The invention also relates to the uses of the compounds in the preparation of medicines for the treatment of various diseases arising from functional cells loss or damage. The diseases arising from stem cell trauma comprise diseases related to the degeneration or damage of nervous system cells, blood system diseases, diseases related to the loss or damage of cardiovascular cells, skin burn and the like.
Synthesis and biological evaluation of a novel human stem/progenitor cells proliferation activator: 4-(4-(5-mercapto-1,3,4-oxadiazol-2-yl)phenyl) thiosemicarbazide (Stemazole)
Sun, Ying,Wang, Wei,Sun, Yuanyuan,Han, Mei
, p. 2930 - 2936 (2011/06/27)
Stem/progenitor cells are crucial for cell-based therapy and regenerative medicine, and their application in clinical and basic research requires a large supply of cells. To identify effective stem/progenitor cell proliferation activators, we synthesised a series of new 4-(4-(5-mercapto-1,3,4-oxadiazol-2- yl)phenyl) thiosemicarbazide (named Stemazole) derivatives. Preliminary evaluation of the structure-activity relationship (SAR) and the biological activities of the compounds were determined with a luminescent cell viability assay. The identified leading compound, Stemazole, exhibited remarkable proliferation-promoting activity in human hippocampal stem/progenitor cells (HSCs) in a time-dependent and concentration-dependent manner. The proliferation-promoting activity of Stemazole was further confirmed against a panel of human stem/progenitor cells derived from each of the three blastoderm layers. In conclusion, Stemazole is a novel activator of stem cells proliferation.
The structure-antituberculosis activity relationships study in a series of 5-aryl-2-thio-1,3,4-oxadiazole derivatives
MacAev, Fliur,Ribkovskaia, Zinaida,Pogrebnoi, Serghei,Boldescu, Veaceslav,Rusu, Ghenadie,Shvets, Nathaly,Dimoglo, Anatholy,Geronikaki, Athina,Reynolds, Robert
experimental part, p. 6792 - 6807 (2011/12/15)
A series of 82 5-aryl-2-thio-1,3,4-oxadiazole derivatives were screened for their anti-mycobacterial activities against Mycobacterium tuberculosis H37Rv. The synthesized compounds 30-37 appeared to be the most active derivatives exhibiting more than 90% inhibition of mycobacterial growth at 12.5 μg/mL. Structure-activity relationships study was performed for the given series by using the electronic-topological method combined with neural networks (ETM-NN). A system for the anti-mycobacterial activity prediction was developed as the result of training associative neural network (ASNN) with weights calculated from projections of a compound and each pharmacophoric fragment found on the elements of the Kohonen's self-organizing maps (SOMs). From the detailed analysis of all compounds under study, the necessary requirements for a compound to possess antituberculosis activity have been formulated. The analysis has shown that any requirement's violation for a molecule implies a considerable decrease or even complete loss of its activity. Molecular docking studies of the compounds allowed shedding light on the binding mode of these novel anti-mycobacterial inhibitors.
