Synthesis, in vitro and in vivo Cytotoxicity of 6,7‐Diaryl‐2,3,8,8a‐tetrahydroindolizin‐5(1H)‐ones.

Abstract

Fused pyridine derivatives R 0450 Synthesis, in vitro and in vivo Cytotoxicity of 6,7-Diaryl-2,3,8,8a-tetrahydroindolizin-5(1H)-ones. -A library of title compounds [cf. (VI)] is prepared according to the scheme. The lead substance exhibits the most potent cytotoxicity toward HCT-116 colon cancer cells. -(KIMBALL, F. S.; TUNOORI, A. R.; VICTORY, S. F.; DUTTA, D.; WHITE, J. M.; HIMES, R. H.; GEORG*, G. I.; Bioorg. Med. Chem. Lett. 17 (2007) 16, 4703-4707; Dep. Med. Chem., Univ. Kans., Lawrence, KS 66045, USA; Eng.) -M. Paetzel 52-143

Total Syntheses and Cytotoxicity of (R)- and (S)-Boehmeriasin A

“…We had become interested in this natural product because of the promising anticancer activity reported and our interest in this class of compounds. , We now report the total synthesis of both boehmeriasin A enantiomers and data concerning their in vitro anticancer activity. In a retrosynthetic sense (Scheme ), boehmeriasin A ( 1 ) was to be derived from an intramolecular biaryl coupling of intermediate 2 , which itself was to be accessed from a palladium-mediated cross-coupling reaction.…”