First Synthesis for Bis-Spirothiazolidine Derivatives as a Novel Heterocyclic Framework and Their Biological Activity.

Autor:	Flefel EM; Department of Photochemistry, Chemical Industries Research Division, National Research Centre, 33 EL-Bohouth St., Dokki 12622, Giza, Egypt.; Department of Chemistry, College of Science, Taibah University, Al-Madinah Al-Monawarah 1343, Saudi Arabia., El-Sofany WI; Department of Photochemistry, Chemical Industries Research Division, National Research Centre, 33 EL-Bohouth St., Dokki 12622, Giza, Egypt.; Department of Chemistry, College of Science, Hail University, Hail, Saudi Arabia., Awad HM; Department of Tanning Materials and Leather Technology, Chemical Industries Research Division, National Research Centre, 33 EL-Bohouth St., Dokki 12622, Giza, Egypt., El-Shahat M; Department of Photochemistry, Chemical Industries Research Division, National Research Centre, 33 EL-Bohouth St., Dokki 12622, Giza, Egypt.
Jazyk:	angličtina
Zdroj:	Mini reviews in medicinal chemistry [Mini Rev Med Chem] 2020; Vol. 20 (2), pp. 152-160.
DOI:	10.2174/1389557519666190920114852
Abstrakt:	Background: Spirothiazolidines are versatile synthetic scaffold possessing wide spectrum of biological interests involving potential anticancer activity. Objective: To report the first synthesis of Bis Spiro-thiazolidine as a novel heterocyclic ring system. Methods: One-pot three-component reaction including condensation of p-phenyllene diamine; cyclohexanone and thioglycolic acid produced Spiro-thiazolidine 4, which underwent further condensation with cyclohexanone and thioglycolic acid with equimolar ratio to introduce Bis-Spiothiazolidine 5 as the first synthesis. Also, bis spiro-thiazolidine arylidene derivatives 6-13 were synthesized by the reaction of Bis-Spiothiazolidine 5 with different aromatic benzaldehydes. Results: Four compounds 13, 12, 9 and 11 have shown highly significant anticancer activity compared to Doxorubicin® (positive control) against Human liver carcinoma (HepG2) and Human Normal Retina pigmented epithelium (RPE-1) cell lines. Conclusion: The novel bis-spirothiazolidine deriviatives have been synthesized for the first time and showed excellent anticancer activities compare with the corresponding spirothiazolidine derivatives. (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)
Databáze:	MEDLINE
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