Pharma Mar, S.a.

Ignacio Rodriguez

Ignacio Manzanares

Carmen Cuevas

Simon Munt

Pilar Gallego

Concepción Polanco

Felix Cuevas

Paloma Mendez

Jose Luis Aceña

Javier Adrio

Paloma Mandez

Concepcion Polanco

The invention relates to aplidine derivatives of the general formula: which are useful for the treatment of tumors.

Synthetic methods for aplidine and new antitumoral derivatives, methods of making and using them

New spisulosine derivatives of use in treating tumors are of the formula (I) wherein: each X is the same or different, and represents H, OH, OR', SH, SR&#x2032;, SOR&#x2032;, SOR&#x2032;, NO, NH, NHR&#x2032;, N(R&#x2032;), CN, halogen, C(&#x2550;O)H, C(&#x2550;O)CH, COH, COCH, substituted or unsubstituted C&#x2013;Calkyl, substituted or unsubstituted C&#x2013;Calkenyl, substituted or unsubstituted C&#x2013;Calkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups X may together form &#x2550;O; Y is NR, OR, PR, SR, or halogen, wherein the number of substituents Ris selected to suit the valency and each Ris independently selected of H, OH, C(&#x2550;O)R&#x2032;, P(&#x2550;O)R&#x2032;R&#x2033;, substituted or unsubstituted C&#x2013;Calkyl, substituted or unsubstituted C&#x2013;Calkenyl, substituted or unsubstituted C&#x2013;Calkynyl, substituted or unsubstituted aryl, and wherein the dotted line indicates an optional double bond; each Z is the same different, and represents H, OH, OR&#x2032;, SH, SR&#x2032;, SOR&#x2032;, SOR&#x2032;, NO, NH, NHR&#x2032;, N(R&#x2032;), NHC(O)R&#x2032;, CN, halogen, C(&#x2550;O)H, C(&#x2550;O)CH, COH, COCH, substituted or unsubstituted C&#x2013;Calkyl, substituted or unsubstituted C&#x2013;Calkenyl, substituted or unsubstituted C&#x2013;Calkenyl, substituted or unsubstituted C&#x2013;Calkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups Z may together form &#x2550;O; z is 0 to 25; y is to 0 to 20; Ris H, C(&#x2550;O)R&#x2032;, P(&#x2550;O)R&#x2032;R&#x2033;, S(&#x2550;O)R&#x2032;R&#x2033;, S(&#x2550;O)R&#x2032;, substituted or unsubstituted C&#x2013;Calkyl, substituted or unsubstituted C&#x2013;CAlkenyl, substituted or unsubstituted C&#x2013;Calkynyl, substituted or unsubstituted aryl; Ris H, C(&#x2550;O)R&#x2032;, P(&#x2550;O)R&#x2032;R&#x2033;, S(&#x2550;O)R&#x2032;R&#x2033;, S(&#x2550;O)R&#x2032;, substituted or unsubstituted C&#x2013;Calkyl, substituted or unsubstituted C&#x2013;Calkenyl, substituted or unsubstituted C&#x2013;Calkynyl, substituted or unsubstituted aryl; each of the R&#x2032;, R&#x2033; groups is independently selected from the group consisting of H, OH, NO, NH, SH, CN, halogen, &#x2550;O, C(&#x2550;O)H, C(&#x2550;O)CH, COH, CO, substituted or unsubstituted C&#x2013;Calkyl, substituted or unsubstituted C&#x2013;Calkoxy, substituted or unsubstituted C&#x2013;Calkenyl, substituted or unsubstituted C&#x2013;Calkynl, substituted or unsubstituted aryl; there may be one or more unsaturations in the hydrocarbon backbone defined by the chain (II) and salts thereof; with the exception of a C&#x2013;C2-amino-3-hydroxyalkane or a C&#x2013;C2-amino-3-hydroxyalkene 

Antitumoral compounds

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Madrid, Spain

Ignacio Rodriguez