64334-93-6Relevant academic research and scientific papers
Synthesis and pharmacological evaluation of new cysLT1 receptor antagonists
Griera,Armengol,Reyes,Alvarez,Palomer,Cabre,Pascual,Garcia,Mauleon
, p. 547 - 570 (2007/10/03)
This paper describes the synthesis and pharmacological evaluation of three series of compounds 4a-b, 13a-k and 19, structurally related to the known potent cysLT1 receptor antagonists RG-12553, IC1-204219 and ONO-1078, respectively. The common structural feature of these new series is the presence of a 4-quinolone nucleus acting as a template for substitution of the aromatic nucleus present in the prototype antagonists. We describe the evolution of these series leading to antagonists with potency at nanomolar concentrations in vitro.
Synthesis and antitumor properties of bis (quinaldine) derivatives
Sinha,Philen,Sato,Cysyk
, p. 1528 - 1531 (2007/10/04)
A series of 7-nitro. and amino-N,N'-bis(4-quinaldinyl)-αω-diaminoalkanes related to the 6-amino derivative was synthezied and tested in the mouse P-388 lymphocytic leukemia screen. Three of the 7-nitro derivatives were found to have moderate activity (T/C 140-150%), while other nitro derivatives were devoid of any antitumor properties. All five 7-amino compounds were moderately to strongly active (T/C 134-196%). In addition, binding of amino derivatives 2-6 to DNA was examined by their ability to (1) stabilize DNA to thermal denaturation and (2) inhibit the DNA-dependent RNA polymerase reaction in vitro. T(m) data suggest that these compounds bind to DNA and are strong inhibitors of the polymerase reaction (I50 = 6-9 X 10-6 M).
