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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