Phorboid 20-homovanillates modified on ring C to mimic the constitution and conformation of the ultrapotent vanilloid resiniferatoxin (RTX) and on the AB ring system to suppress the tumour-promoting potential of the terpenoid core were prepared. Several unexpected reactions were discovered, and the structure-activity relationships for this class of vanilloid ligands were expanded.
Synthesis and biological evaluation of phorbol-resiniferatoxin (RTX) hybrids / R. Annunziata, G. Appendino, A. Bertolino, A. Minassi, A. Szallasi, L. De Petrocelli, V. Di Marzo. - In: EUROPEAN JOURNAL OF ORGANIC CHEMISTRY. - ISSN 1434-193X. - 2004:16(2004), pp. 3413-3421. [10.1002/ejoc.200400122]
Synthesis and biological evaluation of phorbol-resiniferatoxin (RTX) hybrids
R. AnnunziataPrimo
;
2004
Abstract
Phorboid 20-homovanillates modified on ring C to mimic the constitution and conformation of the ultrapotent vanilloid resiniferatoxin (RTX) and on the AB ring system to suppress the tumour-promoting potential of the terpenoid core were prepared. Several unexpected reactions were discovered, and the structure-activity relationships for this class of vanilloid ligands were expanded.
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