Synthesis and antitumour activity of new dendritic polyamines-(imide-DNA-intercalator) conjugates: potent Lck inhibitors.
A series of dendritic polyamines-(imide-DNA-intercalators) conjugates with different connectivity in their basic chain were synthesised and evaluated as antitumour compounds. Although their antiproliferative activity against HT-29 was not significant, conjugates 13 and 16 showed a promising profile as inhibitors of Lck.
Braña
Miguel F
MF
Departamento de Química Orgánica y Farmacéutica, Facultad de Ciencias Experimentales y Técnicas, Universidad San Pablo-CEU, Boadilla del Monte 28668, Madrid, Spain. mfbrana@ceu.es
Domínguez
Gema
G
Sáez
Beatriz
B
Romerdahl
Cynthia
C
Robinson
Simmon
S
Barlozzari
Teresa
T
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D007094:Imides / Q000138:chemical synthesis / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007364:Intercalating Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / Q000037:antagonists & inhibitors; D011073:Polyamines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D007094:Imides; D007364:Intercalating Agents; D011073:Polyamines; D019860:Lymphocyte Specific Protein Tyrosine Kinase p56(lck)