Abstract: This present invention discloses a heterocyclic substituted acardite derivate and application thereof, namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole or pyrimidine, and the substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound of the present invention and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.

Abstract: Provided is the composition of a peptide and its mutagenic version, or other derivatives with the same 3-D structure with activity to bind the extracellular domain of PDGFR-?, or -?, but does not dimerize by itself, wherein said peptide comprises the sequence shown as SEQ ID NO: 1, 2 or 3. Also provided is the composition of the nucleotide sequence encoding said peptide and its derivatives, and the usage of said peptide and derivatives of the peptide in preparation of medicine for the prevention and treatment of fibrosis diseases, such as liver, kidney, and lung fibrosis, primary cancer, and cancer metastasis, especially stomach cancer, liver cancer, breast cancer, and lung cancer.

Abstract: This present invention discloses a heterocyclic substituted acardite derivate and application thereof, namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole or pyrimidine, and the substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound of the present invention and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.

Abstract: Provided is the composition of a peptide and its mutagenic version, or other derivatives with the same 3-D structure with activity to bind the extracellular domain of PDGFR-?, or -?, but does not dimerize by itself, wherein said peptide comprises the sequence shown as SEQ ID NO: 1, 2 or 3. Also provided is the composition of the nucleotide sequence encoding said peptide and its derivatives, and the usage of said peptide and derivatives of the peptide in preparation of medicine for the prevention and treatment of fibrosis diseases, such as liver, kidney, and lung fibrosis, primary cancer, and cancer metastasis, especially stomach cancer, liver cancer, breast cancer, and lung cancer.

Abstract: The invention relates to pseudolaric acid-B derivatives of general formula (I), wherein (a) R1 is cyano, heterocyclyl, COXR? or CON(R?)2, wherein X is O or NH, R? is H, cycloalkyl, alkyl, heterocyclic alkyl or arylalkyl, each R? is independently alkyl, cycloalkyl or heterocyclicalkyl; (b) R2 is H, alkylacyl, arylalkylacyl, arylacyl or heterocyclylacyl; (c) R3 is COXY, amino or halogen, wherein X is O or NH, Y is H, NH2, hydroxy, alkyl, cycloalkyl, heterocyclicalkyl, hetroatom-substituted alkyl, tertiary amino-substituted ammonioalkyl, aryl, arylalkyl or polyhydroxyalkyl. The invention also relates to processes for preparing such derivatives and antitumor or antifungal pharmaceutical compositions containing the same.

Abstract: The invention relates to pseudolaric acid-B derivatives of general formula (I), wherein (a) R1 is cyano, heterocyclyl, COXR′ or CON(R′)2, wherein X is O or NH, R′ is H, cycloalkyl, alkyl, heterocyclic alkyl or arylalkyl, each R″ is independently alkyl, cycloalkyl or heterocyclicalkyl; (b) R2 is H, alkylacyl, arylalkylacyl, arylacyl or heterocyclylacyl; (c) R3 is COXY, amino or halogen, wherein X is O or NH, Y is H, NH2, hydroxy, alkyl, cycloalkyl, heterocyclicalkyl, hetroatom-substituted alkyl, tertiary amino-substituted ammonioalkyl, aryl, arylalkyl or polyhydroxyalkyl. The invention also relates to processes for preparing such derivatives and antitumor or antifungal pharmaceutical compositions containing the same.