Design, Synthesis and Antitumor Evaluation of Novel Pyrazolopyrimidines and Pyrazoloquinazolines

被引：48

作者：

El-Naggar, Mohamed ^{[1
]}

Hassan, Ashraf S. ^{[2
]}

Awad, Hanem M. ^{[3
]}

Mady, Mohamed F. ^{[4
,5
]}

机构：

[1] Univ Sharjah, Fac Sci, Chem Dept, Sharjah 27272, U Arab Emirates

[2] Natl Res Ctr, Organometall & Organometalloid Chem Dept, Cairo 12622, Egypt

[3] Natl Res Ctr, Dept Tanning Mat & Leather Technol, Cairo 12622, Egypt

[4] Natl Res Ctr, Dept Green Chem, Cairo 12622, Egypt

[5] Univ Stavanger, Fac Sci & Technol, Dept Chem Bio Sci & Environm Technol, N-4036 Stavanger, Norway

来源：

MOLECULES | 2018年 / 23卷 / 06期

关键词：

pyrazolopyrimidines; pyrazoloquinazolines; synthesis; antitumor activity; cell cycle analysis; SRC KINASE INHIBITORS; IN-VITRO; BIOLOGICAL EVALUATION; SCHIFF-BASES; ANTIOXIDANT ACTIVITY; CYTOTOXIC ACTIVITY; DERIVATIVES; ANTICANCER; MOIETY; THIOGLYCOSIDES;

D O I：

10.3390/molecules23061249

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

k A series of N-aryl-7-aryl-pyrazolo[1,5-a]pyrimidines 18a-u and N-aryl-pyrazolo[1,5-a]quinazolines 25a-c were designed and synthesized via the reaction of 5-aminopyrazoles 11a-c with enaminones 12a-g or 19, respectively. The new compounds were screened for their in vitro antitumor activity toward liver (HepG-2) and breast (MCF-7) human cancer cells using 3-[4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide MTT assay. From the results, it was found that all compounds showed dose-dependent cytotoxic activities against both HepG-2 and MCF-7 cells. Two compounds 18o and 18a were selected for further investigations. Cell cycle analysis of liver (HepG-2) cells treated with 18o and breast (MCF-7) cells treated with 18a showed cell cycle arrest at G2/M phase and pro-apoptotic activity as indicated by annexin V-FITC staining.

引用

页数：20

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