133544-77-1Relevant academic research and scientific papers
NQO1-activated 6 -diazyl -5 - oxo - L -n-leucine prodrug and preparation method and application thereof
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Paragraph 0078-0079, (2021/10/05)
The invention discloses NQO1-activated 6 -diazyl -5 - oxo - L - n-leucine prodrug and a preparation method and application thereof. Due to the high expression NQO1 in most tumor cells, the introduced NQO1 activated quinic acid group can achieve the tumor
Syntheses and antibacterial activity of N -acylated ciprofloxacin derivatives based on the trimethyl lock
Ji, Cheng,Miller, Patricia A.,Miller, Marvin J.
supporting information, p. 707 - 710 (2015/06/23)
Several N-acyl ciprofloxacin quinone derivatives based on a trimethyl lock structure were synthesized, and their in vitro antibacterial activity against a panel of clinically relevant bacteria was evaluated. A few new analogues displayed enhanced activity
Anti-tumuor agents
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Page column 22, (2010/01/30)
The invention concerns anti-tumour agents of formula (I) wherein each of R1, R2and R3has the meanings defined in the specification including hydrogen, (1-4C)alkyl, (3-4)alkenyl, (3-4C)alkynyl, amino, (1-4C)alkylamino and (
Reductive and Bioreductive Activation is Controlled by Electronic Properties of Substituents in Conformationally-Constrained Anticancer Drug Delivery Systems
Weerapreeyakul, Natthida,Visser, Petra,Brummelhuis, Mathijn,Gharat, Laxmikant,Chikhale, Prashant J.
, p. 148 - 163 (2007/10/03)
Conformationally-constrained, anticancer drug delivery systems (TDDS) containing the methyl ester of melphalan (as a model drug) were synthesized using electron-withdrawing or electron-donating functional groups to modulate reductive and bioreductive activation. The electronic nature of substituents in TDDS was found to control reductive and bioreductive activation of TDDS, thus influencing drug delivery from TDDS.
Reductive activation of conformationally-constrained, anticancer drug delivery systems
Gharat, Laxmikant,Visser, Petra,Brummelhuis, Mathijn,Guiles, Ronald,Chikhale, Prashant
, p. 444 - 456 (2007/10/03)
Redox-active substituents were used to modulate reduction potentials in conformationally-constrained, drug delivery systems. The extent of drug delivery was proportional to the degree of reductive activation, which was influenced by the electronic properties of the substituents. Such reductively-activated carrier systems can be used to achieve controlled drug delivery to bioreductive regions in hypoxic solid tumors.
