2005

Fused pyridine derivatives

R 0450 Synthesis and in vitro Cytotoxic Evaluation of 1,4-Bisubstituted and 1,3,9-Trisub-
stituted β-Carboline Derivatives. — A variety of bi- and trisubstituted β-carboline
27- 149 derivatives are synthesized via Pictet—Spengler reaction of tryptophan (I) and evalu-
ated for their cytotoxic activity. The 1,3,9-trisubstituted β-carboline derivatives such as
(VII) and (VIII) show higher cytotoxic activities in vitro than the corresponding
1,3-disubstituted β-carbolines (V). N-Pentafluorobenzylcarboline (VIIIc) proves to be
the most active compound of this series. — (CAO, R.; PENG, W.; CHEN, H.; HOU,
X.; GUAN, H.; CHEN, Q.; MA, Y.; XU*, A.; Eur. J. Med. Chem. 40 (2005) 3,
249-257; Dep. Biochem., Cent. Biopharm. Res., Coll. Life Sci., Sun Yat-Sen Univ.,
Guangzhou 510275, Peop. Rep. China; Eng.) — R. Staver