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Synthesis and antitumor activity of some new pyrazolo[1,5-α]pyrimidines

Synthesis and antitumor activity of some new pyrazolo[1,5-α]pyrimidines

作     者:Ashraf S.Hassan Mohamed F.Mady Hanem M.Awad Taghrid S.Hafez 

作者机构:Department of Organometallic and Organometalloid Chemistry National Research Centre Dokki 12622 CairoEgypt Department of Green Chemistry National Research Centre Dokki 12622 Cairo Egypt Department of Mathematics and Natural Science Faculty of Science and Technology University of Stavanger N-4036 Stavanger Norway Department of Tanning Materials and Leather Technology National Research Centre Dokki 12622 Cairo Egypt 

出 版 物:《Chinese Chemical Letters》 (中国化学快报(英文版))

年 卷 期:2017年第28卷第2期

页      面:388-393页

核心收录:

学科分类:1007[医学-药学(可授医学、理学学位)] 10[医学] 

主  题:5-Amino-1H-pyrazole Pyrazolo[1 5-α]pyrimidine Schiff bases MIT assay Anticancer activity Structure activity relationship 

摘      要:New series of pyrazolo[1,5-α]pyrimidine derivatives 7a-i,11a-c and Schiff bases 13a-c were synthesized and screened for their in vitro antitumor activity against three human carcinoma cell lines,namely colorectal carcinoma(HCT116),prostate adenocarcinoma(PC-3) and liver carcinoma(HepG-2) using MTT cytotoxicity assay at 100 μg/*** of the tested compounds displayed good anticancer activities against HCT-116 and PC-3 ***,compounds 7d and 11 a showed better antitumor activity than the rest of the compounds against both cell lines.A structure-activity relationship(SAR) has been discussed and structures of the newly synthesized compounds were confirmed by different spectral data(MS,IR,^1H NMR and ^13C NMR) and elemental analysis.

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