A QSAR Study on Some Series of Anticancer Tyrosine Kinase Inhibitors

被引：5

作者：

Anwer, Zaihra ^{[1
]}

Gupta, Satya P. ^{[1
,2
]}

机构：

[1] Meerut Inst Engn Technol, Dept Pharmaceut Technol, Meerut 250005, Uttar Pradesh, India

[2] Meerut Inst Engn Technol, Dept Appl Sci, Meerut 250005, Uttar Pradesh, India

来源：

MEDICINAL CHEMISTRY | 2013年 / 9卷 / 02期

关键词：

Quantitative structure-activity relationship; Tyrosine kinase inhibitors; Lck inhibitors; Endothelial growth factor receptor (EGFR); 4-alkynylquinazolines; 4-alkenylquinazolines; N-4,6-pyrimidine-N-alkyl-N -phenyl ureas; RECEPTOR; EGFR;

D O I：

10.2174/1573406411309020005

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A quantitative structure-activity relationship (QSAR) study has been made on two different series of anticancer tyrosine kinase inhibitors, namely a series of 4-alkynyl and 4-alkenyl-quinazolines and a series of N-4,6-pyrimidine-N-alkyl-N'-phenyl ureas. For the first series, QSAR results indicate that the activity is controlled by the hydrophobicity of the molecules and molecular connectivity index of the substituent, whereas for the second series of compounds the activity is found to be controlled by the molecular connectivity index of the substituent and some indicator variables.

引用

页码：203 / 212

页数：10

共 19 条

[1] Oncogenic kinase signalling [J].

Blume-Jensen, P ;

Hunter, T .

NATURE, 2001, 411 (6835) :355-365

[2]

Dobrusin EM, 1992, ANNU REP MED CHEM, V27, P169

[3] Comparing antibody and small-molecule therapies for cancer [J].

Imai, Kohzoh ;

Takaoka, Akinori .

NATURE REVIEWS CANCER, 2006, 6 (09) :714-727

[4] NEU(C-ERBB2/HER2) AND THE EPIDERMAL GROWTH-FACTOR RECEPTOR (EGFR) IN BREAST-CANCER [J].

JARDINES, L ;

WEISS, M ;

FOWBLE, B ;

GREENE, M .

PATHOBIOLOGY, 1993, 61 (5-6) :268-282

[5] GENERAL DEFINITION OF VALENCE DELTA-VALUES FOR MOLECULAR CONNECTIVITY [J].

KIER, LB ;

HALL, LH .

JOURNAL OF PHARMACEUTICAL SCIENCES, 1983, 72 (10) :1170-1173

[6]

Kier LB., 1976, Molecular connectivity in chemistry and drug research

[7] Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: Identification of new scaffolds for potent EGFR tyrosine kinase inhibitors [J].

Kitano, Yasunori ;

Suzuki, Tsuyoshi ;

Kawahara, Eiji ;

Yamazaki, Takahisa .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2007, 17 (21) :5863-5867

[8] TYROSINE KINASE INHIBITION - AN APPROACH TO DRUG DEVELOPMENT [J].

LEVITZKI, A ;

GAZIT, A .

SCIENCE, 1995, 267 (5205) :1782-1788

[9]

LIU XQ, 1994, RECENT PROG HORM RES, V49, P149

[10] Development of N-4,6-pyrimidine-N-alkyl-N′-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase [J].

Maier, Jennifer A. ;

Brugel, Todd A. ;

Sabat, Mark ;

Golebiowski, Adam ;

Laufersweiler, Matthew J. ;

VanRens, John C. ;

Hopkins, Corey R. ;

De, Biswanath ;

Hsieh, Lily C. ;

Brown, Kimberly K. ;

Easwaran, Vijayasurian ;

Janusz, Michael J. .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (14) :3646-3650

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