title: Synthesis and evaluation of a dimer of 2-(4-pyridylmethyl)-1-indanone as a novel nonsteroidal aromatase inhibitor.
abstract: 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.
authors.affiliation: University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India. ranju29in@yahoo.co.in
authors.forename: Ranju
authors.initials: R
authors.lastname: Gupta
authors.forename: Dharam Paul
authors.initials: DP
authors.lastname: Jindal
authors.forename: Birinder
authors.initials: B
authors.lastname: Jit
authors.forename: Gaurav
authors.initials: G
authors.lastname: Narang
authors.forename: Anja
authors.initials: A
authors.lastname: Palusczak
authors.forename: Rolf W
authors.initials: RW
authors.lastname: Hartmann
mesh_terms: 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
chemical_list: C492795:2-(4-pyridylmethyl)-1-indanone; D047072:Aromatase Inhibitors; D007189:Indans