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Synthesis and structure-activity relationships of novel pyrimido[1,2-b]indazoles as potential anticancer agents against A-549 cell lines.

Abstract：

:A series of novel pyrimido[1,2-b]indazoles 5, 7 have been prepared from 3-trifluoromethyl-5-phenyl-2,6-dicyano anilines 1 via novel indazole regioisomers 3 and 4 through a facile strategy. Specific examples were evaluated for anticancer activity in vitro and found to exhibit promising activity against A-549 cell lines and are more effective than Etoposide. QSAR models were developed and validated by cross-validation method. The results of the best QSAR model were further compared with the crystal structure of tubulin protein. The binding energies estimated were found to have a good correlation with the experimental inhibitory potencies.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Yakaiah T,Lingaiah BP,Narsaiah B,Shireesha B,Ashok Kumar B,Gururaj S,Parthasarathy T,Sridhar B

doi

10.1016/j.bmcl.2007.03.087

subject

Has Abstract

pub_date

2007-06-15 00:00:00

pages

3445-53

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00385-X

journal_volume

17

pub_type

杂志文章

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