Synthetic Route of 64359-81-5, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 64359-81-5, Name is 4,5-Dichloro-2-octylisothiazol-3(2H)-one, SMILES is O=C1N(CCCCCCCC)SC(Cl)=C1Cl, belongs to thiazoles compound. In a article, author is Bkhaitan, Majdi, introduce new discover of the category.
Synthesis and Antiproliferative Activity of 4 beta-O-Substituted, 4 beta-N-Substituted Deoxypodophyllotoxin Derivatives, and 4 beta-OH-4 ‘-O-Substituted Podophyllotoxin
Podophyllotoxin (PPT) and its derivatives possess various biological activities and particularly against numerous cancers. The high toxicity and side effects of this therapeutic class are behind the restricted deployment in clinical applications. Here, we have identified and reported the synthesis of 4 beta-O-substituted 4′-O-demethylpodphyllotoxin derivatives, 4 beta-N-substituted 4′-O-demethyl-4- deoxypodophyllotoxin derivatives and 4 beta-OH- 4′-O-substituted podophyllotoxin derivative (series a, e and p) respectively. These derivatives are either esters or amides of various heterocyclic moieties which include imidazole, thiazole, pyrazole, and indole. Their synthesis was carried out in one step reaction and obtained in good yield. We tested all prepared compounds against T47D, MDA231, Caco-2, and MCF-7 cancer cell lines. They have been shown to possess significant biological activity, where series a has been demonstrated to be the most potent one. Compound 3 a exhibits potential activity in the micromolar range scoring 11 mu M against Caco-2 and 18 mu M against MDA231. Consequently, all synthesized compounds have been evaluated for their safety profile and tested against PCS201012 which are normal skin fibroblast cell lines showing noticeable safety. The biological results demonstrate that the presence of an aromatic heterocycle ring in position 4 and 4’ lead to derivatives less toxic compared to podophyllotoxin and epipodophyllotoxin. Also, they are less potent. However, the results obtained will have, in future work, an important impact on the development of more potent and less toxic leads.
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Reference:
Thiazole | C3H3NS – PubChem,
,Thiazole | chemical compound | Britannica