In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Characterization, chemical optimization and anti-tumor activity of a tubulin poison identified by a p53-based phenotypic screen, published in 2008-11-01, which mentions a compound: 2199-44-2, mainly applied to JJ781 derivative antitumor design preparation structure activity p53 tubulin, SDS of cas: 2199-44-2.
A robust p53 cell-based assay that exploits p53’s function as a transcription factor was used to screen a small mol. library and identify bioactive small mols. with potential antitumor activity. Unexpectedly, the majority of the highest ranking hit compounds from this screen arrest cells in mitosis and most of them impair polymerization of tubulin in cells and in vitro. One of these novel compounds, JJ78:1, was subjected to structure-activity relationship studies and optimized leading to the identification of JJ78:12. This mol. is significantly more potent than the original hit JJ78:1, as it is active in cells at two-digit nanomolar concentrations and shows clear antitumor activity in a mouse xenograft model as a single agent. The effects of nocodazole, a well established tubulin poison, and JJ78:12 on p53 levels are remarkably similar, supporting that tubulin depolymerization is the main mechanism by which JJ78:12 treatment leads to p53 activation in cells. In summary, these results identify JJ78:12 as a potential cancer therapeutic, demonstrate that screening for activators of p53 in a cell-based assay is an effective way to identify inhibitors of mitosis progression and highlights p53’s sensitivity to alterations during mitosis.
Compound(2199-44-2)SDS of cas: 2199-44-2 received a lot of attention, and I have introduced some compounds in other articles, similar to this compound(Ethyl 3,5-Dimethyl-2-pyrrolecarboxylate), if you are interested, you can check out my other related articles.
Reference:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com