Triterpenoids as new promising anticancer drugs.
Triterpenoids are structurally diverse organic compounds, characterized by a basic backbone modified in multiple ways, allowing the formation of more than 20 000 naturally occurring triterpenoid varieties. Several triterpenoids, including ursolic and oleanolic acid, betulinic acid, celastrol, pristimerin, lupeol, and avicins possess antitumor and anti-inflammatory properties. To improve antitumor activity, some synthetic triterpenoid derivatives have been synthesized, including cyano-3,12-dioxooleana-1,9 (11)-dien-28-oic (CDDO), its methyl ester (CDDO-Me), and imidazolide (CDDO-Im) derivatives. Of these, CDDO, CDDO-Me, and betulinic acid have shown promising antitumor activities and are presently under evaluation in phase I studies. Triterpenoids are highly multifunctional and the antitumor activity of these compounds is measured by their ability to block nuclear factor-kappaB activation, induce apoptosis, inhibit signal transducer, and activate transcription and angiogenesis.
Petronelli
Alessia
A
Department of Hematology, Istituto Superiore di Sanità, Viale Regina Elena 299, 00161 Rome, Italy.
Pannitteri
Gaetano
G
Testa
Ugo
U
D020533:Angiogenesis Inhibitors / Q000494:pharmacology; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002454:Cell Differentiation / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D002986:Clinical Trials as Topic; D016503:Drug Delivery Systems; D006801:Humans; D015394:Molecular Structure; D051267:NF-E2-Related Factor 2 / Q000096:biosynthesis; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*
D020533:Angiogenesis Inhibitors; D000972:Antineoplastic Agents, Phytogenic; D051267:NF-E2-Related Factor 2; D014315:Triterpenes