CAMBIO DE DISCURSO : LA SECOND-LINE SCLC-ES TRAS EL FIASCO DE LA FASE III LAGOON YA MEJOR NI NOMBRARLA...CAMBIAMOS DISCURSO A MANTENIMIENTO EN FIRTS-LINE Y PASAMOS DEL VIAL DE 4 Mg AI VIAL DE 2 Mg .//. JazzPharma TO WITHDRAW LURBINECTEDIN WITH US_FDA IN SECOND-LINE SCLC-ES...EN ESPAÑA NO SE HAN ENTERADO AÚN...SI NO EXISTIERA IMFORTE...AHORA MISMO PHARMAMAR ESTARÍA ANTE UNA GRAVE SITUACIÓN ... 2 DE OCTUBRE DE 2028 ... ES LA FECHA MÁS TEPMPRANA PARA LA POSIBLE ENTRADA DE GENÉRICOS .
23 mayo 2007
22 mayo 2007
Synthesis and Structure-Activity Relationship of Cytotoxic Marine Cyclodepsipeptide IB-01212 Analogues. 18 / 5 / 2007 .
2007 May 18
Cruz LJ, Francesch A, Cuevas C, Albericio F.
Institute for Research in Biomedicine, Barcelona Science Park, University of Barcelona, 08028-Barcelona, Spain, Fax: (+34) 93-403-71-26.
Several recently discovered marine products have remarkable in vitro and in vivo anticancer profiles against a wide range of tumor cell lines. Some of these compounds are currently in clinical trials. These compounds show complex structures and mechanisms of action of interest. Herein, we describe the preparation of a series of totally synthetic molecules that are structurally related to the natural marine product IB-01212 and evaluated them as antitumor agents. For this, total solid-phase syntheses of the products were performed in parallel by two distinct routes: linear synthesis and convergent synthesis. Structural modifications were introduced in several residue positions to afford 21 IB-01212 analogues for structure-relationship studies. An increase in the number of methyl groups in the macrocycle enhanced cytotoxic activity. Also, the replacement of an ester bond by an amide bond favored antitumor activity against several human cell lines. In addition, the L configuration analogues were more active against all the tumor cell lines than those containing the D configuration. A significant increase in the size and asymmetry of the macrocycle diminished biological activity with respect to that of IB-01212. These results are of great value for the discovery of new and more effective anticancer agents.
Cruz LJ, Francesch A, Cuevas C, Albericio F.
Institute for Research in Biomedicine, Barcelona Science Park, University of Barcelona, 08028-Barcelona, Spain, Fax: (+34) 93-403-71-26.
Several recently discovered marine products have remarkable in vitro and in vivo anticancer profiles against a wide range of tumor cell lines. Some of these compounds are currently in clinical trials. These compounds show complex structures and mechanisms of action of interest. Herein, we describe the preparation of a series of totally synthetic molecules that are structurally related to the natural marine product IB-01212 and evaluated them as antitumor agents. For this, total solid-phase syntheses of the products were performed in parallel by two distinct routes: linear synthesis and convergent synthesis. Structural modifications were introduced in several residue positions to afford 21 IB-01212 analogues for structure-relationship studies. An increase in the number of methyl groups in the macrocycle enhanced cytotoxic activity. Also, the replacement of an ester bond by an amide bond favored antitumor activity against several human cell lines. In addition, the L configuration analogues were more active against all the tumor cell lines than those containing the D configuration. A significant increase in the size and asymmetry of the macrocycle diminished biological activity with respect to that of IB-01212. These results are of great value for the discovery of new and more effective anticancer agents.
21 mayo 2007
18 mayo 2007
17 mayo 2007
Alzheimer es actualmente la patología más devastadora y de mayor crecimiento en los Estados Unidos .
16/05/2007 12:55:00 -
El CEO de la farmacéutica norteamericana Wyeth, Robert Essner, en una exposición ante la comisión de Salud, Educación, Trabajo y Pensiones del Senado norteamericano, subrayó que el Alzheimer es actualmente la patología más devastadora y de mayor crecimiento en los Estados Unidos, al tiempo que solicitó el compromiso de la Cámara de la misma manera que se iniciaron iniciativas para detener el SIDA en la década de los ochenta.
El CEO de la farmacéutica norteamericana Wyeth, Robert Essner, en una exposición ante la comisión de Salud, Educación, Trabajo y Pensiones del Senado norteamericano, subrayó que el Alzheimer es actualmente la patología más devastadora y de mayor crecimiento en los Estados Unidos, al tiempo que solicitó el compromiso de la Cámara de la misma manera que se iniciaron iniciativas para detener el SIDA en la década de los ochenta.
16 mayo 2007
15 mayo 2007
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