4-Substituted-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine Derivatives: Design, Synthesis, Antitumor and EGFR Tyrosine Kinase Inhibitory Activity

被引：18

作者：

Abbas, Safinaz E. -S. ^{[1
]}

Aly, Enayat I. ^{[1
]}

Awadallah, Fadi M. ^{[1
]}

Mahmoud, Walaa R. ^{[1
]}

机构：

[1] Cairo Univ, Dept Pharmaceut Chem, Fac Pharm, Cairo 11562, Egypt

来源：

CHEMICAL BIOLOGY & DRUG DESIGN | 2015年 / 85卷 / 05期

关键词：

antitumor; EGFR-TK inhibition; molecular modeling; pyrazolo[3; 4-d]pyrimidines; synthesis; ANTIPROLIFERATIVE ACTIVITY; CANCER; AGENTS; STRATEGY; DOCKING; CELLS; A431;

D O I：

10.1111/cbdd.12451

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：

Four series of some 4-substituted-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine derivatives 5a-f, 6a-f, 8a-f, and 9a-f were designed to be screened for their antitumor activity. All compounds were evaluated against breast (MCF-7) and lung (A-549) cell lines. Six compounds 5a, 5b, 6b, 6e, 9e, and 9f displaying activity against both cell lines were further estimated for their EGFR-TK inhibitory activity where they revealed 41-91% inhibition and compound 6b elicited the highest activity (91%). A docking study of these compounds into the ATP-binding site of EGFR-TK demonstrated their binding mode where H-bonding interaction with Met793 through N-1 of pyrimidine or N-2 of pyrazole was observed.

引用

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页码：608 / 622

页数：15

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