| 摘要 |
<p>PURPOSE:To obtain the subject derivative comprising a 2-aryl-4-quinolinol derivative, exhibiting an excellent antitumor effect on its oral administration, inhibiting the aggregation of tubulin as a functional mechanism, capable of overcoming multiple resistance, and useful for anticancer chemotheraby, etc. CONSTITUTION:The objective 2-aryl-4-quinolinol derivative of formula II (R<1> is cyano, ethynyl, (substituted)alkyl, aminomethyl, etc.; Ar is 5-6 membered aromatic hetero ring, naphthyl, (substituted)phenyl, etc.; A is H, lower alkoxycarbonyl) and useful as an active ingredient for antitumor agents, etc., is produced by reacting an aniline derivative (e.g. p-dimethylaminoaniline) with an N-p-alkoxyphenyl aromatic acyl acetoamide (e.g. N-p-methoxyphenylbenzoyl acetic amide) and subsequently subjecting the produced beta-arylamino-betaarylacrylic acid ester of formula I [R<4> is the same as R<1>; Ar<1> is the same as Ar; Z is alkoxy, benzyl, etc.] to a thermal ring-closing reaction.</p> |
