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El cáncer es una enfermedad crónica caracterizada por la aparición de células
anormales que se comportan irregularmente, pierden el control de su crecimiento, lo que
conduce a una proliferación desordenada.
El desarrollo de nuevos agentes antitumorales es de primordial importancia,
principalmente el desarrollo de fármacos que interrumpan la fase del ciclo celular, más
concretamente la mitosis.
Las kinesinas son proteínas motoras que intervienen en la formación del huso
mitótico y el monastrol actúa como un inhibidor selectivo para la proteína motora
Kinesina-5 (KSP, denominado también Eg5).
Siendo así el objetivo es crear análogos de monastrol para observar si hay
diferencias en la potencia de acción, ya que el monastrol es un inhibidor débil de la
kinesina KSP. Dentro de los cuatro compuestos enviados para la bioactividad, el que
presto mejor resultado fue el compuesto 9, presentando un IC50 para concentraciones
100 μM.
Cancer is a chronic disease characterized by the appearance of abnormal cells that behave erratically, losing control of its growth, which leads to a disordered proliferation. The development of new antitumor agents is of paramount importance, particularly the development of drugs that disrupt the cell cycle phase, more specifically mitosis. Kinesins are motor proteins involved in the formation of the spindle and acts as an inhibitor monastrol selective kinesin motor protein-5 (KSP, also called Eg5). The objective is to create analogues of monastrol to see if there are differences in potency of action, as the monastrol is a weak inhibitor of the kinesin KSP. Within four compounds sent for bioactivity, which presto best result was compound 9, showing an IC50 of 100 μM concentrations.
Cancer is a chronic disease characterized by the appearance of abnormal cells that behave erratically, losing control of its growth, which leads to a disordered proliferation. The development of new antitumor agents is of paramount importance, particularly the development of drugs that disrupt the cell cycle phase, more specifically mitosis. Kinesins are motor proteins involved in the formation of the spindle and acts as an inhibitor monastrol selective kinesin motor protein-5 (KSP, also called Eg5). The objective is to create analogues of monastrol to see if there are differences in potency of action, as the monastrol is a weak inhibitor of the kinesin KSP. Within four compounds sent for bioactivity, which presto best result was compound 9, showing an IC50 of 100 μM concentrations.
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Mª de la Concepción Pérez Melero