Azaindole-indole coupled derivatives, preparation methods and uses thereof
AssigneeJingcai Cheng
InventorsJingcai Cheng, Qizheng Yao, Zhaohui Wang, Weiyi Hua
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Abstract
A novel class of azaindole-indole coupled derivatives, their preparation methods, pharmaceutical compositions containing the same and the uses thereof. The common structural feature of these derivatives is that they are coupled by azaindole and indole bi-molecule at different positions, forming extended pi-conjugated systems. Such derivatives inhibited cell growth and proliferation by various mechanisms. The present compounds have improved solubility, increased bioavailability, and thus have enhanced drug actions, and reduced medical dosages and undesired responses.
Claims11
An azaindole-indole coupled derivative represented by the formula (IG) or the pharmaceutically acceptable salts thereof:
- Y═Z (IG)
- wherein,
- Y is an azaindole group represented by formula (Y1) or (Y2);
- Z is an indole group represented by formula (Z1) or (Z2);
- “═” represents the double bond which is located between the 3-position of the azaindole group (Y) and the 2′- or 3′-position of the indole group (Z);
- in the above Y1, Y2, Z1 and Z2, R1 and R1′ independently represent H or the following groups which may be unsubstituted or substituted by 1 to 3 substituents:
- C1-C6 alkyl, aryl, aralkyl, acyl, aroyl, glycosyl or biosyl protected by acyl, glycosyl or biosyl;
- wherein said substituents are selected from:
- halogen, hydroxyl, C1-C3 alkyl, nitro or amino;
- R2, R3, R4, R2′, R3′, R4′ and R5′ independently represent H, halogen, hydroxyl, sulfhydryl, or the following groups which may be unsubstituted or substituted by 1 to 3 substituents:
- C1-C4 alkyl, nitro, amino, amido, amide, C1-C4 alkoxy, methylthio, phenyl, phenoxy, aryl, aralkyl, trifluoromethyl, acyl, aroyl, sulfonic group, sulfamoyl, isocyanate, or alkyl isocyanate;
- wherein said substituents are selected from:
- halogen, hydroxyl, C1-C3 alkyl having, nitro or amino;
- R represents oxygen, sulfur, selenium, or a NR6 or NOR6 group, wherein R6 is H, or the following groups which may be unsubstituted or substituted by 1 to 3 substituents:
- C1-C6 straight-chain or branched-chain alkyl, aryl, aralkyl, C3-C6 alicyclic group, acyl, aroyl, sulfonyl or phosphoryl;
- wherein said substituents are selected from:
- halogen, hydroxyl, C1-C3 alkyl, nitro or amino.
Dependencies are inferred from the claim text.