- Synthesis and cytotoxic evaluation of quinazolin-4(3H)-one derivatives bearing thiocarbamate, thiourea or N-methyldithiocarbamate side Chains
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We have previously found that the dithiocarbamate derivatives of quinazolin-4(3H)-one could act as cytotoxic agents against a panel of human tumor cell lines. To investigate the contribution of dithiocarbamate moiety to the cytotoxic activity, three series of novel quinazolin-4(3H)-one derivatives bearing thiocarbamate, thiourea or Nmethyldithiocarbamate side chains were synthesized and tested for their cytotoxic activity against human cancer cell lines A549, MCF-7, HeLa, HT29 and HCT-116 by MTT assay. The results showed that transformation of the dithiocarbamate moiety in lead compound I to thiocarbamate or thiourea led to a decrease or loss of cytotoxic activity. Some N-alkylated analogs of lead compound II preferentially inhibited the proliferation of A549 cells, although their potencies were not improved in comparison with the unalkylated counterparts. The structure-activity relationship obtained in this research will be beneficial for further synthesis and discovery of effective cytotoxic agents.
- Cao, Sheng-Li,Xu, Hong,Wang, Yao,Liao, Ji,Zhang, Jing-Jing,Li, Zhong-Feng,Guo, Yan-Wen,Li, Xiao-Rong,Cui, Xue-Mei,Xu, Xingzhi
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experimental part
p. 163 - 173
(2012/07/31)
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- Antimicrobial volatile glucosinolate autolysis products from Hornungia petraea (L.) Rchb. (Brassicaceae)
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Plant samples of Hornungia petraea were analyzed for glucosinolate (GLS) autolysis metabolites for the first time. GC-MS analysis of the autolysate and the synthesis of a series (12 compounds) of possible glucosinolate breakdown products revealed/corroborated the presence of glucoaubrietin, glucolimnanthin, glucolepigramin and glucotropaeolin in this species as the most likely "mustard oil" precursors. GLS degradation products identified in the autolysate of H. petraea, benzyl isothiocyanate, 3- and 4-methoxybenzyl isothiocyanate, along with several other structurally related compounds were evaluated for antimicrobial activity in order to possibly pinpoint the role of the latter secondary metabolites in the plant tissues. The assays showed a very high antibacterial activity of the tested isothiocyanates against Sarcina lutea and an antifungal effect against Aspergillus fumigatus and Candida albicans with MIC values in the order of 1 μg/ml value.
- Radulovi?, Niko S.,Deki?, Milan S.,Stojanovi?-Radi?, Zorica Z.
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experimental part
p. 351 - 357
(2012/07/16)
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- Selective Alpha 2B/2C Agonists
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Described herein are compounds useful as agonists of alpha 2B/2C receptors. Pharmaceutical compositions including the presently described compounds and methods of treatment of diseases and conditions with the presently described compounds also are disclos
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Page/Page column 10-11
(2011/02/25)
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- A new efficient synthesis of isothiocyanates from amines using di-tert-butyl dicarbonate
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Alkyl and aryl amines are converted smoothly to the corresponding isothiocyanates via the dithiocarbamates in good to excellent yields using di-tert-butyl dicarbonate (Boc2O) and 1-3 mol % of DMAP or DABCO as catalyst. As most of the byproducts are volatile, the work-up involves simple evaporation of the reaction mixture.
- Munch, Henrik,Hansen, Jon S.,Pittelkow, Michael,Christensen, J?rn B.,Boas, Ulrik
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p. 3117 - 3119
(2008/09/20)
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- 2-IMINO-1,3-THIAZINE DERIVATIVES
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A compound of the formula (I) of the present invention selectively binds to a cannabinoid type 2 receptor (CB2R) and exhibits an antagonistic activity or agonistic activity to CB2R. wherein R1 is optionally substituted alkylene; R2 i
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