Syntheses and antitumor activities of N¡ä1,N¡ä3-dialkyl-N¡ä1,N¡ä3-di-(alkylcarbonothioyl) malonohydrazide: The discovery of elesclomol
文摘
A series of N¡ä1,N¡ä3-dialkyl-N¡ä1,N¡ä3-di(alkylcarbonothioyl) malonohydrazides have been designed and synthesized as anticancer agents by targeting oxidative stress and Hsp70 induction. Structure-activity relationship (SAR) studies lead to the discovery of STA-4783 (elesclomol), a novel small molecule that has been evaluated in a number of clinical trials as an anticancer agent in combination with Taxol.