Design, Synthesis, and Evaluation of DuocarmycinO-Amino Phenol Prodrugs Subject to Tunable Reductive Activation

نویسندگان
چکیده

برای دانلود باید عضویت طلایی داشته باشید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Synthesis and Biological Evaluation of Mutual Prodrugs of 2- {[3-(trifluoromethyl)phenyl]amino}benzoic Acid

For reducing the gastrointestinal (GI) toxicity associated with flufenamic acid (FA), its carboxylic group was masked by synthesizing its mutual prodrugs with propyphenazone by direct coupling and by using spacer technique. The structures of the synthesized mutual prodrugs (FE and FG) were confirmed by IR, H NMR, C NMR, mass spectroscopy and their purity were established by elemental analysis. ...

متن کامل

Design, synthesis and biological evaluation of phosphorodiamidate prodrugs of antiviral and anticancer nucleosides.

We herein report the application of the phosphorodiamidate phosphate prodrug approach to a series of thirteen nucleoside analogs with antiviral or anticancer activity. Twenty-five symmetrical phosphorodiamidates were synthesized, bearing esterified l-Alanine (and in one case d-Alanine) in the prodrug moiety, each as single stereoisomer. The presence of an achiral phosphorus represents a potenti...

متن کامل

Bioreduction activated prodrugs of camptothecin: molecular design, synthesis, activation mechanism and hypoxia selective cytotoxicity.

Several water-soluble derivatives (CPT3, CPT3a-d) of camptothecin (CPT) were synthesized, among which CPT3 bearing an N,N'-dimethyl-1-aminoethylcarbamate side-chain was further conjugated with reductively eliminating structural units of indolequinone, 4-nitrobenzyl alcohol and 4-nitrofuryl alcohol to produce novel prodrugs of camptothecin (CPT4-6). All CPT derivatives were of lower cytotoxicity...

متن کامل

Design, Synthesis and Biological Evaluation of Brain-Targeted Thiamine Disulfide Prodrugs of Ampakine Compound LCX001.

Ampakine compounds have been shown to reverse opiate-induced respiratory depression by activation of amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) glutamate receptors. However, their pharmacological exploitations are hindered by low blood-brain barrier (BBB) permeability and limited brain distribution. Here, we explored whether thiamine disulfide prodrugs with the ability of "lock-i...

متن کامل

Design, synthesis and evaluation of diclofenac-antioxidant mutual prodrugs as safer NSAIDs

Diclofenac has been conjugated with different antioxidants having antiulcerogenic activity with the objective of obtaining diclofenac-antioxidant mutual prodrugs as safer NSAIDs devoid of ulcerogenic side-effects. The synthesized derivatives are screened for their antiinflammatory, analgesic and antiulcer activity. The mutual prodrugs show retention of antiinflammatory activity with reduced ulc...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

ژورنال

عنوان ژورنال: Journal of Medicinal Chemistry

سال: 2010

ISSN: 0022-2623,1520-4804

DOI: 10.1021/jm1010397