Novel water-soluble c-ring analogues of 20(S)-camptothecin

Novel water-soluble c-ring analogues of 20(S)-camptothecin

  • CN 1,221,421 A
  • Filed: 04/22/1997
  • Published: 06/30/1999
  • Est. Priority Date: 06/05/1996
  • Status: Abandoned Application
First Claim
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1. formula 1 compound, R wherein 1, R 2, R 3And R 4Identical or different separately, expression hydrogen, hydroxyl, lower alkoxy, aryloxy, lower alkane acyl group, nitro, cyano group, halogen, carboxyl, carbonyl oxygen base, amino, substituted-amino, low alkyl group, replacement low alkyl group or R 2And R 3Expression-O-(CH combines 2) n-O-, wherein n=1 or 2;

  • R 5Expression hydrogen, low alkyl group, replace low alkyl group, rudimentary aralkyl, methylol, carboxymethyl, aminomethyl, wherein amino is one or dibasic replacement aminomethyl, two substituting groups independence or be combined together to form 5 or 6 yuan of member ring systems separately wherein, described member ring systems contains carbon and arbitrariness and contains one or two and be selected from oxygen, the heteroatoms of nitrogen and sulphur, R represents hydrogen, low alkyl group, low-grade alkenyl, the lower alkane acyl group, replace low alkyl group, replace the lower alkane acyl group, replace low-grade alkenyl, elementary alkoxy carbonyl, phenyl, benzyl or benzoyl, wherein phenyl can be not and to replace or replace;

    And R 6Expression hydrogen, hydroxyl, lower alkoxy or COOR '"'"', wherein R '"'"' expression hydrogen, low alkyl group or rudimentary aralkyl;

    Acid amides or amino, wherein amino can be not replacement or one or dibasic, two substituting groups independence or be combined together to form the member ring systems that contains 3 to 8 atoms separately wherein, described member ring systems contains carbon and arbitrariness contains the heteroatoms that one or two is selected from oxygen, nitrogen and sulphur;

    Phenoxy group, phenyl, benzoyl or benzyl, wherein phenyl can be and not replace or replaced by one, two or three substituting group, and described substituting group is selected from halogen, hydroxyl, lower alkoxy, cyano group, carboxyl, nitro, amido, amino or substituted-amino, low alkyl group, replacement low alkyl group;

    Cycloalkyl or cycloalkyl low-grade alkyl, wherein to be 3 yuan to 7 yuan all be the member ring systems of carbon atom to ring;

    By the low alkyl group of one or more heterocyclic substituted, wherein heterocyclic system has 3 to 7 atoms, comprises carbon and is selected from the heteroatoms of oxygen, nitrogen and sulphur with at least one;

    Lower alkane acyl group, low alkyl group;

    Replace low alkyl group, wherein substituting group can be halogen, hydroxyl, alkoxyl group, aryloxy, carboxyl, cyano group, sulfo-, alkylthio, thioaryl, aryl, heteroaryl, nitro, amido or amino, wherein amino can be not replacement or one or dibasic, two substituting groups independence or be combined together to form the member ring systems that contains 3 to 8 atoms separately wherein, described member ring systems contains carbon and arbitrariness contains the heteroatoms that one or two is selected from oxygen, nitrogen and sulphur.

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