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

A new series of 2,5-regioselective benzofuran-tetrazole hybrids ( XIIIa – XIIIp ) were synthesised from 2 H -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 cel...

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Bibliographic Details
Published in:Russian journal of bioorganic chemistry 2020-09, Vol.46 (5), p.845-855
Main Authors: Sudhakar Mokenapelli, Gutam, Madhu, Yerrabelli, Jayaprakash Rao, Irlapati, Vamshi Krishna, Gorityala, Neelima, Sagurthi, Someswar Rao, Chitneni, Prasad Rao
Format: Article
Language:English
Subjects:
Antiproliferatives
Biochemistry
Biomedical and Life Sciences
Biomedicine
Bioorganic Chemistry
Biotechnology
Kinases
Life Sciences
Molecular docking
Organic Chemistry
Tetrazoles
Tyrosine
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Summary:A new series of 2,5-regioselective benzofuran-tetrazole hybrids ( XIIIa – XIIIp ) were synthesised from 2 H -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 ) (IC 50 : 3.19 μM) and ( XIIIm ) (IC 50 : 2.25 μM) 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.
ISSN:1068-1620
1608-330X
DOI:10.1134/S1068162020050179