70362-07-1Relevant articles and documents
Piperazine-Coumarin based fluorescence probe with enhanced brightness and solubility for bio-thiol detection and esophageal carcinoma diagnosis
Ma, Junyan,Xu, Yaoyu,Wang, Yaxin,Li, Junkuo,Liu, Lin,Si, Weijie,Hou, Jingli,Zhang, Zhenxing
supporting information, (2021/10/05)
The development of novel fluorescent dyes for bio-thiol is of great importance in biological, clinical and pharmaceutical sciences. Given the importance of bio-thiol anticipating in numerous physiological processes, there is a great need to construct fluo
Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells
Draoui, Nihed,Schicke, Olivier,Fernandes, Antony,Drozak, Xavier,Nahra, Fady,Dumont, Amélie,Douxfils, Jonathan,Hermans, Emmanuel,Dogné, Jean-Michel,Corbau, Romu,Marchand, Arnaud,Chaltin, Patrick,Sonveaux, Pierre,Feron, Olivier,Riant, Olivier
, p. 7107 - 7117 (2013/11/06)
Under hypoxia, cancer cells consume glucose and release lactate at a high rate. Lactate was recently documented to be recaptured by oxygenated cancer cells to fuel the TCA cycle and thereby to support tumor growth. Monocarboxylate transporters (MCT) are the main lactate carriers and therefore represent potential therapeutic targets to limit cancer progression. In this study, we have developed and implemented a stepwise in vitro screening procedure on human cancer cells to identify new potent MCT inhibitors. Various 7-substituted carboxycoumarins and quinolinone derivatives were synthesized and pharmacologically evaluated. Most active compounds were obtained using a palladium-catalyzed Buchwald-Hartwig type coupling reaction, which proved to be a quick and efficient method to obtain aminocarboxycoumarin derivatives. Inhibition of lactate flux revealed that the most active compound 19 (IC 50 11 nM) was three log orders more active than the CHC reference compound. Comparison with warfarin, a conventional anticoagulant coumarin, further showed that compound 19 did not influence the prothrombin time which, together with a good in vitro ADME profile, supports the potential of this new family of compounds to act as anticancer drugs through inhibition of lactate flux.
Benzofurylpyrone derivatives
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, (2008/06/13)
There is provided benzofuryl-α-pyrone derivative represented by the following structural formula (I): wherein R1represents a hydrogen atom or an alkyl group of 1 to 5 carbons; R2represents hydrogen, —CO—R5or —SO2/sub