Synthesis of novel 2-cyanothiazolocarbazoles analogues of ellipticine
✍ Scribed by Hadjila Chabane; Christelle Lamazzi; Valérie Thiéry; Gérald Guillaumet; Thierry Besson
- Publisher
- Elsevier Science
- Year
- 2002
- Tongue
- French
- Weight
- 111 KB
- Volume
- 43
- Category
- Article
- ISSN
- 0040-4039
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📜 SIMILAR VOLUMES
Original 1,4-benzoxazine analogues of ellipticine were prepared using a general synthetic route that relied on an anionic ring annulation as the key transformation. The interest of this approach lies on the possibility of an easy entrance to a wide range of derivatives from the phenol intermediate.
Two new ellipticine analogues were synthetized as potential non nucleoside inhibitors of reverse transcriptase and were tested on Moloney leukaemia virus reverse transcriptase in vitro. Both derivatives (9a,b) showed considerable inhibitory effect; IDs0 was found to be in the range of 2.8 to 4.5 x 1