Pharma Mar, S.a.

Juan Jose Gonzalez

Ignacio Manzanares

Carmen Cuevas

Simon Munt

Andres Francesh

Regan James Anderson

Jonathan Charles Morris

Carlos Del Pozo

Modesto Remuiñan

Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X, R, R, R, R, R, and Rare each independently selected from the group consisting of H, OH, OR', SH, SR&#x2032;, SOR&#x2032;, SOR&#x2032;, NO, NH, NHR&#x2032;, N(R&#x2032;), NHCOR&#x2032;, NHSOR&#x2032;, CN, halogen, &#x2550;O, C(&#x2550;O)H, C(&#x2550;O)R&#x2032;, COH, COR&#x2032;, carboxyalkyl, C-Calkyl, C-Calkenyl, C-Calkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R&#x2032; groups is independently selected from the group consisting of H, OH, SH, NO, NH, CN, halogen, &#x2550;O, C(&#x2550;O)H, C(&#x2550;O)CH, COH, COCH, C-Calkyl, C-Calkenyl, C-Calkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups of Rand R, Rand R, Rand R, Rand R, or Rand Rmay be joined into a carbocyclic or heterocyclic ring system.

Variolin derivatives and their use as antitumor agents

Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X, R, R, R, R, Rand Rare each independently selected from the group consisting of H, OH, OR', SH, SR&#x2032;, SOR&#x2032;, SOR&#x2032;, NO, NH, NHR&#x2032;, N(R&#x2032;), NHCOR&#x2032;, NHSOR&#x2032;, CN, halogen, &#x2550;O, C(&#x2550;O)H, C(&#x2550;O)R&#x2032;, COH, COR&#x2032;, carboxyalkyl, C-Calkyl, C-Calkenyl, C-Calkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R&#x2032; groups is independently selected from the group consisting of H, OH, SH, NO, NH, CN, halogen, &#x2550;O, C(&#x2550;O)H, C(&#x2550;O)CH, COH, COCH, C-Calkyl, C-Calkenyl, C-Calkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups Rand R, Rand R, Rand R, Rand R, or Rand Rmay be joined into a carbocyclic or heterocyclic ring system. 

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Madrid, Spain

Juan Jose Gonzalez