488832-69-5 Usage
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
Check Digit Verification of cas no
The CAS Registry Mumber 488832-69-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,8,8,8,3 and 2 respectively; the second part has 2 digits, 6 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 488832-69:
(8*4)+(7*8)+(6*8)+(5*8)+(4*3)+(3*2)+(2*6)+(1*9)=215
215 % 10 = 5
So 488832-69-5 is a valid CAS Registry Number.
InChI:InChI=1/C19H20N4O2S2/c1-22(18(26)14-9-5-3-6-10-14)20-16(24)13-17(25)21-23(2)19(27)15-11-7-4-8-12-15/h3-12H,13H2,1-2H3,(H,20,24)(H,21,25)
488832-69-5Relevant articles and documents
Facile and convenient synthesis of N ′1, N ′3-dialkyl- N ′1, N ′3-bis(arylcarbonothioyl)malonohydrazides via propylphosphonic anhydride coupling
Xia, Zhiqiang,Jiang, Jun,Sun, Lijun,Tatsuta, Noriaki,Koya, Keizo,Zhang, Junyi,Bohnert, Gary,Chen, Shoujun
, p. 3394 - 3398 (2015/01/09)
A facile and convenient synthetic method for the anticancer agent elesclomol and its analogues, N′1,N′3-dialkyl-N′1,N′3-bis(arylcarbonothioyl)malonohydrazides, by the direct coupling of N-alkyl-N-(substituted)be
Syntheses and antitumor activities of N′1, N′3-dialkyl-N′1,N′3-di- (alkylcarbonothioyl) malonohydrazide: The discovery of elesclomol
Chen, Shoujun,Sun, Lijun,Koya, Keizo,Tatsuta, Noriaki,Xia, Zhiqiang,Korbut, Timothy,Du, Zhenjian,Wu, Jim,Liang, Guiqing,Jiang, Jun,Ono, Mitsunori,Zhou, Dan,Sonderfan, Andrew
, p. 5070 - 5076 (2013/09/12)
A series of N′1,N′3-dialkyl- N′1,N′3-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.
PROCESS FOR PREPARING BIS(THIOHYDRAZIDE AMIDES)
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Page/Page column 36-37, (2009/07/17)
Disclosed herein are methods of preparing a bis(thio-hydrazide amides) compounds of the following structural formula (I), wherein R1., R3 and Y are defined herein.
