Synthesis and antitumor activity evaluation of some N-heterocycles derived from pyrazolyl-substituted 2(3H)-furanone

Abou-Elmagd, W.S.I. ; El-Ziaty, Ahmed ; Elzahar, M.I. ; Ramadan, S.K. ; Hashem, A.I. ; Ramadan, Sayed 


Abstract


© 2016, Copyright © Taylor & Francis Group, LLC. Pyrazolyl-substituted 2(3H)-furanone was allowed to react with different nitrogen nucleophiles such as hydrazine hydrate, ethylenediamine, ethanolamine, and anthranilic acid to give pyrrolone and benzoxazinone derivatives. The acid hydrazide 3 was reacted with some carbonyl compounds such as 4-chlorobenzaldehyde, chloroacetyl chloride, and acetic anhydride to give thiazolidinone, oxadiazole, and pyridazinone derivatives. Selected examples of the synthesized compounds were evaluated as anticancer agents against three types of carcinoma cell lines (HePG 2, HCT116, and PC3), using Doxorubicin as a reference drug. The result revealed that some of the new compounds showed high activities. Compound 6a was more potent than the standard drug. A docking study using MOE 2008.10 program was performed.


Other data

Issue Date 2016
Journal Synthetic Communications 
URI http://research.asu.edu.eg/123456789/872
DOI 14
1197
http://www.scopus.com/inward/record.url?eid=2-s2.0-84978524975&partnerID=MN8TOARS
46
10.1080/00397911.2016.1193755


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