Design and synthesis of new substituted spirooxindoles as potential inhibitors of the MDM2-p53 interaction was written by Barakat, Assem;Islam, Mohammad Shahidul;Ghawas, Hussien Mansur;Al-Majid, Abdullah Mohammed;El-Senduny, Fardous F.;Badria, Farid A.;Elshaier, Yaseen A. M. M.;Ghabbour, Hazem A.. And the article was included in Bioorganic Chemistry in 2019.Formula: C4H7NO2S This article mentions the following:
The designed compounds, 4a-p, were synthesized using a simple and smooth method with an asym. 1,3-dipolar reaction as the key step. The chem. structures for all synthesized compounds were elucidated and confirmed by spectral anal. The mol. complexity and the absolute stereochem. of 4b and 4e designed analogs were determined by X-ray crystallog. anal. The anticancer activities of the synthesized compounds were tested against colon (HCT-116), prostate (PC-3), and hepatocellular (HepG-2) cancer cell lines. Mol. modeling revealed that the compound 4d binds through hydrophobic-hydrophobic interactions with the essential amino acids (LEU: 57, GLY: 58, ILE: 61, and HIS: 96) in the p53-binding cleft, as a standard p53-MDM2 inhibitor (6SJ). The mechanism underlying the anticancer activity of compound 4d was further evaluated, and the study showed that compound 4d inhibited colony formation, cell migration, arrested cancer cell growth at G2/M, and induced apoptosis through intrinsic and extrinsic pathways. Transactivation of p53 was confirmed by flow cytometry, where compound 4d increased the level of activated p53 and induced mRNA levels of cell cycle inhibitor, p21. In the experiment, the researchers used many compounds, for example, Thiazolidine-4-carboxylic acid (cas: 444-27-9Formula: C4H7NO2S).
Thiazolidine-4-carboxylic acid (cas: 444-27-9) belongs to thiazolidine derivatives. Derivatives, thiazolidines, are known. For example, the drug pioglitazone contains a thiazolidine ring. Another drug that contains a thiazolidine ring is the antibiotic penicillin. Thiazolidine and its composites are key components of many natural products and drugs , and are also present in many synthetic compounds such as anticancer, anti-inflammatory, antitubercular, antifungal, antiviral, anti-HIV, cytotoxicity, antitrypanosomal, antinociceptive and anti-hypernociceptive compounds.Formula: C4H7NO2S
Referemce:
Thiazolidine – Wikipedia,
Thiazolidine – ScienceDirect.com