Synthesis and evaluation of a dimer of 2-(4-pyridylmethyl)-1-indanone as a novel nonsteroidal aromatase inhibitor.
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 potassium 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 microM) as compared to aminoglutethimide (RP = 1, IC(50) = 18.5 microM.
Gupta
Ranju
R
University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India. ranju29in@yahoo.co.in
Jindal
Dharam Paul
DP
Jit
Birinder
B
Narang
Gaurav
G
Palusczak
Anja
A
Hartmann
Rolf W
RW
D047072:Aromatase Inhibitors; D006801:Humans; D066298:In Vitro Techniques; D007189:Indans / Q000138:chemical synthesis* / Q000494:pharmacology; D008861:Microsomes / Q000187:drug effects / Q000201:enzymology; D010920:Placenta / Q000187:drug effects / Q000201:enzymology
C492795:2-(4-pyridylmethyl)-1-indanone; D047072:Aromatase Inhibitors; D007189:Indans