The Royal Institution for the Advancement of Learning / Mcgill University

Pharma Mar, S.a.

Junichi Tanaka

Dolores Garcia Gravalos

Tatsuo Higa

Marie-Ève Bordeleau

Robert Francis

Jerry Pelletier

Lisa Lindqvist

The present invention relates to a anti-proliferative target for designing chemotherapeutic agents, which comprises a EIF4A protein having an amino acid sequence, as defined in claim

Chemotherapeutic agents for inhibition of protein translation

Compounds of formula (I) wherein Ris selected from H, C(&#x2550;O)R', P(&#x2550;O)R&#x2032;R&#x2033;, S(&#x2550;O)R&#x2032;R&#x2033;, substituted or unsubstituted C-Calkyl, substituted or unsubstituted C-Calkenyl, substituted or unsubstituted C-Calkynyl, or substituted or unsubstituted aryl; or Rtogether with Rforms a saturated or unsaturated heterocyclic ring; Rand Rare each, independently, selected from H, C(&#x2550;O)R&#x2032;, P(&#x2550;O)R&#x2032;R&#x2033;, S(&#x2550;O)R&#x2032;R&#x2033;, substituted or unsubstituted C-Calkyl, substituted or unsubstituted C-Calkenyl, substituted or unsubstituted C-Calkynyl, or substituted or unsubstituted aryl; or one of Ror Rtogether with Rforms a saturated or unsaturated heterocyclic ring; or Rand Rtogether form a saturated or unsaturated heterocyclic ring; Ris selected from H, C(&#x2550;O)R&#x2032;, P(&#x2550;O)R&#x2032;R&#x2033;, S(&#x2550;O)R&#x2032;R&#x2033;, substituted or unsubstituted C-Calkyl, substituted or unsubstituted C-Calkenyl, substituted or unsubstituted C-C, alkynyl, or substituted or unsubstituted aryl, wherein R&#x2032; is selected from the group consisting of H, OH, NO, NH, SH, CN, halogen, C(&#x2550;O)H, C(&#x2550;O)CH, COH, COCH, substituted or unsubstituted C-Calkyl, substituted or unsubstituted C-Calkenyl, substituted or unsubstituted C-Calkynyl, substituted and unsubstituted aryl; R&#x2033; is selected from the group consisting of H, OH, NO, NH, SH, CN, halogen, &#x2550;O, C(&#x2550;O)H, C(&#x2550;O)CH, COH, COCH, substituted or unsubstituted C-Calkyl, substituted or unsubstituted C-Calkenyl, substituted or unsubstituted C-Calkynyl, substituted and unsubstituted aryl; wherein X, XXon formula I are independently placed in any particular position of the chain and independently selected from H, OH, OR&#x2032;, SH, SR&#x2032;, SOR&#x2032;, SOR&#x2032;, NO, NH, NHR&#x2032;, N(R&#x2032;), NHC(O)R&#x2032;, CN, halogen, &#x2550;O, C(&#x2550;O)H, C(&#x2550;O)CH, COH, COCH, substituted or unsubstituted C-Calkyl, substituted or unsubstituted C-Calkenyl, substituted or unsubstituted C-Calkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, wherein substituent groups defined by R&#x2032; are each independently selected from the group consisting of H, OH, OR&#x2032;, SH, SR&#x2032;, SOR&#x2032;, SOR&#x2032;, NO, NH, NHR&#x2032;, N(R&#x2032;), NHC(O)R&#x2032;, CN, halogen, &#x2550;O, C(&#x2550;O)H, C(&#x2550;O)CH, COH, COCH, substituted or unsubstituted C-Calkyl, substituted or unsubstituted C-Calkenyl, substituted or unsubstituted C-Calkynyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaromatic; wherein x is 6 to 20; and wherein the dotted lined is one or several optional double bonds placed in any particular position of the side chain; or pharmaceutically acceptable salts thereof are useful as antitumor compounds and include compound IK-8-73-4 of structure (a) which was isolated from a spongesp.

Oxy-and amino-substituted tetrahydrofuryl derivatives with antitumour activity

Growing community of inventors

Okinawa, Japan

Junichi Tanaka