2,4-Diamino-9H-pyrimido[4,5-b]indol-5-ols: synthesis, in vitro cytotoxic activity, and QSAR investigations.
A series of novel 2,4-diaminopyrimido[4,5-b]indol-6-ols has been synthesized and the in vitro cytotoxic activities were evaluated against four human cancer cell lines originating from solid tumors. An increase in activity was observed when a heteroaromatic ring was annulated on side g of the pyrimido[4,5-b]indole system to give compounds with activities comparable to ellipticine and cisplatin. To understand the experimental cytotoxic activities, QSAR investigations were performed, which showed a very good linearity between the experimental and predicted IC(50).
Dotzauer
Bernd
B
Institut für Pharmazie und Lebensmittelchemie, Emil Fischer Centrum, Friedrich-Alexander-Universität, Schuhstr. 19, D-91052 Erlangen, Germany.
Grünert
Renate
R
Bednarski
Patrick J
PJ
Lanig
Harald
H
Landwehr
Jens
J
Troschütz
Reinhard
R
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D021281:Quantitative Structure-Activity Relationship; D013055:Spectrophotometry, Infrared
D000970:Antineoplastic Agents; D011743:Pyrimidines