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Synthesis and structure guided evaluation of estrogen agonist and antagonist activities of some new tetrazolyl indole derivatives.

Abstract：

:Several regioisomeric tetrazolyl indole derivatives with structurally modified alkyl substituents at the tetracyclic indole nitrogen containing N-ethyl amino tetrazole moiety have been synthesized and screened for their ER binding affinity, agonist (estrogenic), antagonist (antiestrogenic) and anti-implantation activities. N-2 regioisomers were found to be moderately antagonists and one compound showed 100% contraceptive efficacy at 10 mg/kg dose. Molecular docking studies carried out in comparison to estradiol and raloxifene showed different binding modes of the two regioisomers to the binding site.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Singh US,Shankar R,Yadav GP,Kharkwal G,Dwivedi A,Keshri G,Singh MM,Moulik PR,Hajela K

doi

10.1016/j.ejmech.2007.10.035

subject

Has Abstract

pub_date

2008-10-01 00:00:00

pages

2149-58

issue

10

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(07)00430-8

journal_volume

43

pub_type

杂志文章

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