Design and Synthesis of Novel 2-Substituted-Benzyl-5-(2-Methylbenzofuran-3-yl)-2H-Tetrazoles: Anti-Proliferative Activity

被引：1

作者：

Mokenapelli, Sudhakar ^{[1
]}

Gutam, Madhu ^{[1
]}

Yerrabelli, Jayaprakash Rao ^{[1
]}

Irlapati, Vamshi Krishna ^{[2
]}

Gorityala, Neelima ^{[2
]}

Sagurthi, Someswar Rao ^{[2
]}

Chitneni, Prasad Rao ^{[1
]}

机构：

[1] Osmania Univ, Dept Chem, Nat Prod Lab, Hyderabad 500007, Telangana, India

[2] Osmania Univ, Dept Genet & Biotechnol, Hyderabad 500007, Telangana, India

来源：

RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY | 2020年 / 46卷 / 05期

关键词：

benzofuran; tetrazoles; anti-proliferative activity; molecular docking; SAR studies; BENZOFURAN DERIVATIVES; ANTIINFLAMMATORY EVALUATION; CYTOTOXIC ACTIVITY; TETRAZOLE; INHIBITORS; POTENT; AGENTS; PART; TOXICITY;

D O I：

10.1134/S1068162020050179

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：

A new series of 2,5-regioselective benzofuran-tetrazole hybrids (XIIIa-XIIIp) were synthesised from 2H-chromene-3-carbonitriles (IXa), (IXb) in multi steps approach under mild reaction conditions in good yields and evaluated their anti-proliferative activity against HCT116 and Miapaca2 cell lines. Wherein compounds (XIIIe) (IC50: 3.19 mu M) and (XIIIm) (IC50: 2.25 mu M) were displayed highest anti-proliferative activity in both cell lines. Molecular docking and SAR studies revealed the in vitro results with target Proto-oncogene tyrosine kinase Src protein.

引用

页码：845 / 855

页数：11

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