- Semicarbazide derivatives and pharmaceutical compositions and uses thereof
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The invention relates to a selenosemicarbazone derivative, and a pharmaceutical composition and an application thereof. Specifically, the invention relates to a compound shown as a formula I or an isomer thereof, a pharmaceutically acceptable salt, a composition comprising the compound shown as the general formula I or the isomer thereof, the pharmaceutically acceptable salt and a pharmaceutically acceptable vector, and applications of the compound shown as the general formula I or the isomer thereof and the pharmaceutically acceptable salt in preparing drugs for resisting tumor or treating diseases or symptoms related to the tumor. The formula I is shown in the description.
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Paragraph 0149; 0152-0154; 0163-0164
(2020/05/11)
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- Novel 1,3,4-Selenadiazole-Containing Kidney-Type Glutaminase Inhibitors Showed Improved Cellular Uptake and Antitumor Activity
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Kidney-type glutaminase [KGA/isoenzyme glutaminase C (GAC)] is becoming an important tumor metabolism target in cancer chemotherapy. Its allosteric inhibitor, CB839, showed early promise in cancer therapeutics but limited efficacy in in vivo cancer models. To improve the in vivo activity, we explored a bioisostere replacement of the sulfur atom in bis-2-(5-phenylacetamido-1,2,4-thiadiazol)ethyl sulfide and CB839 analogues with selenium using a novel synthesis of the selenadiazole moiety from carboxylic acids or nitriles. The resulting selenadiazole compounds showed enhanced KGA inhibition, more potent induction of reactive oxygen species, improved inhibition of cancer cells, and higher cellular and tumor accumulation than the corresponding sulfur-containing molecules. However, both CB839 and its selenium analogues show incomplete inhibition of the tested cancer cells, and a partial reduction in tumor size was observed in both the glutamine-dependent HCT116 and aggressive H22 liver cancer xenograft models. Despite this, tumor tissue damage and prolonged survival were observed in animals treated with the selenium analogue of CB839.
- Chen, Zhao,Li, Di,Xu, Ning,Fang, Jinzhang,Yu, Yan,Hou, Wei,Ruan, Haoqiang,Zhu, Panpan,Ma, Renchao,Lu, Shiying,Cao, Danhui,Wu, Rui,Ni, Mowei,Zhang, Wei,Su, Weike,Ruan, Benfang Helen
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supporting information
p. 589 - 603
(2019/01/10)
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- An efficient one-pot synthesis of 2-amino-1,3,4-selenadiazoles
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An efficient one-pot synthesis of 2-amino-1,3,4-selenadiazoles from isoselenocyanates, hydrazine hydrate and aromatic aldehydes has been developed. This approach provides a simple, mild and facile way to construct various derivatives in moderate to good y
- Li, Xue,Gan, Bin,Xie, Tinghui,Yang, Ping,Xie, Yuanyuan
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p. 178 - 181
(2016/04/20)
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- Phenolic thio- and selenosemicarbazones as multi-target drugs
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A series of isosteric phenolic thio- and selenosemicarbazones have been obtained by condensation of naturally-occurring phenolic aldehydes and thio(seleno)semicarbazides. Title compounds were designed as potential multi-target drugs, and a series of struc
- Calcatierra, Verónica,López, óscar,Fernández-Bola?os, José G.,Plata, Gabriela B.,Padrón, José M.
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- One-pot synthesis of 5-arylamino-1,3,4-selenadiazol-2(3H)-ones from arylisoselenocyanates
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A one-pot reaction of arylisoselenocyanates, hydrazine and bis(trichloromethyl) carbonate, in the presence of a base provides an efficient route for the synthesis of 5-arylamino-1,3,4-selenadiazol-2(3H)-ones in good to excellent yields. A plausible mechan
- Xie, Yuanyuan,Yang, Ping,Chen, Xiaodong
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experimental part
p. 421 - 424
(2012/09/22)
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- Selective synthesis of novel 2-imino-1,3-selenazolidin-4-ones and 2-amino-1,3,4-selenadiazin-5-ones from isoselenocyanates
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An efficient and regioselective synthesis of 2-imino-1,3-selenazolidin-4- ones and 2-amino-1,3,4-selenadiazin-5-ones was achieved via one-pot reaction of isoselenocyanates, hydrazines, and ethyl chloroacetate or chloroacetyl chloride, respectively. Plausi
- Xie, Yuanyuan,Liu, Junli,Li, Jianjun
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supporting information; experimental part
p. 932 - 935
(2011/03/21)
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