Elesclomol

Definition

ChEBI: A carbohydrazide obtained by formal condensation of the carboxy groups of malonic acid with the hydrino groups of two molar equivalents of N-methylbenzenecarbothiohydrazide

Biological Activity

elesclomol (also known as sta-4783), originally identified in a cell-based phenotypic screen for proapoptotic activity, is a novel small-molecule that potently induces apoptosis of cancer cells through the rapid generation of reactive oxygen species (ros) and the induction of unmanageable levels of oxidative stress. elesclomol exhibits autitumor activity against a broad spectrum of types of cancer cell in human tumor xengograft models due to its excessive ros production and elevated levels of oxidative stress leading to the death of cancer cells. elesclomol is currently being studies as a novel cancer therapeutic, in which it has demonstrated ability to prolong progression-free survival in study subjects.ronald k. blackman, kahlin cheung-ong, marinella gebbia, david a. proia, suqin he, jane kepros, aurelie jonneaux, philippe marchetti, jerome kluza, patricia e. rao, yumiko wada, guri giaever, corey nislow. mitochondrial electron transport is the cellular target of the oncology drug elesclomol. plos one 2012; 7(1): e29798jessica r. kirshner, suqin he, vishwasenani balasubramanyam, jane kepros, chin-yu yang, mei zhang, zhenjian du, james barsoum, and john bertin. elesclomol induces cancer cell apoptosis through oxidative stress. mol cancer ther 2008; 7:2319-2327