Synthesis and Evaluation of a Dimer of 2‐(4‐Pyridylmethyl)‐1‐Indanone as a Novel Nonsteroidal Aromatase Inhibitor | Zendy

Gupta Ranju | Zendy; Jindal Dharam Paul | Zendy; Jit Birinder | Zendy; Narang Gaurav | Zendy; Palusczak Anja | Zendy; Hartmann Rolf W. | Zendy

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Synthesis and Evaluation of a Dimer of 2‐(4‐Pyridylmethyl)‐1‐Indanone as a Novel Nonsteroidal Aromatase Inhibitor

Author(s) -

Gupta Ranju,

Jindal Dharam Paul,

Jit Birinder,

Narang Gaurav,

Palusczak Anja,

Hartmann Rolf W.

Publication year - 2004

Publication title -

archiv der pharmazie

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.468

H-Index - 61

eISSN - 1521-4184

pISSN - 0365-6233

DOI - 10.1002/ardp.200400853

Subject(s) - aromatase , dimer , chemistry , aminoglutethimide , stereochemistry , pyridine , aromatase inhibitor , aldol condensation , medicinal chemistry , biochemistry , cancer , organic chemistry , medicine , catalysis , breast cancer

A novel dimer of 2‐(4‐pyridylmethyl)‐1‐indanone ( 2 ) was obtained while carrying out aldol condensation of 1‐indanone with pyridine‐4‐carboxaldehyde in potas sium hydroxide. The structure of dimer 3 has been established using various spectral techniques and was screened for its ability to inhibit the cytochrome P 450 enzyme aromatase. The dimer showed strong inhibition of human placental aromatase and was found 3 times more potent (RP = 3, IC 50 = 10.2 μM) as compared to aminoglutethimide (RP = 1, IC 50 = 18.5 μM

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