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Synthesis and biological activity of alpha-bromoacryloyl lexitropsin conjugates

Romagnoli, Romeo and Baraldi, Pier Giovanni and Iaconinoto, Maria Antonietta and Carrion, Maria Dora and Tabrizi, Mojgan Aghazadeh and Gambari, Roberto and Borgatti, Monica and Heilmann, Jörg (2005) Synthesis and biological activity of alpha-bromoacryloyl lexitropsin conjugates. European journal of medicinal chemistry 40 (11), pp. 1123-1128.

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Abstract

The design, synthesis and biol. evaluation of lexitropsins bearing mixed heterocyclic and benzoheterocyclic moieties and tethered to an alpha-bromo acrylic moiety acting as alkylating moiety are reported, and structure-activity relationships detd. For example, indolecarboxylic acid I reacted with pyrrole deriv. II to give analog III (X = Y = CH, Z = NMe) in 63% yield. With respect to ...

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Item Type:Article
Date:2005
Additional information (public):CAN 144:23119 34-3 Amino Acids, Peptides, and Proteins 636-47-5 (Distamycin A); 132244-47-4; 287734-07-0 Role: PAC (Pharmacological activity), BIOL (Biological study) (prepn. of alpha -bromoacryloyl lexitropsin conjugates, their human antitumor activity, and structure-activity relationship); 870476-34-9P; 870476-35-0P; 870476-36-1P; 870476-37-2P; 870476-38-3P; 870476-39-4P; 870476-40-7P; 870476-41-8P; 870476-42-9P Role: PAC (Pharmacological activity), SPN (Synthetic preparation), BIOL (Biological study), PREP (Preparation) (prepn. of alpha -bromoacryloyl lexitropsin conjugates, their human antitumor activity, and structure-activity relationship); 207845-97-4; 245358-71-8; 561318-70-5; 870476-43-0; 870476-44-1; 870476-45-2 Role: RCT (Reactant), RACT (Reactant or reagent) (prepn. of alpha -bromoacryloyl lexitropsin conjugates, their human antitumor activity, and structure-activity relationship)
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann)
Identification Number:
ValueType
2005:1119440Other
Keywords:Structure-activity relationship (antitumor prepn. of alpha -bromoacryloyl lexitropsin conjugates, their antitumor activity, and structure-activity relationship) Antitumor agents Cytotoxicity Leukemia (prepn. of alpha -bromoacryloyl lexitropsin conjugates, their antitumor activity, and structure-activity relationship) Human (prepn. of alpha -bromoacryloyl lexitropsin conjugates, their human antitumor activity, and structure-activity relationship) bromoacryloyl lexitropsin conjugate prepn antitumor structure activity lexitropsin heterocyclic benzoheterocyclic bromoacryloyl prepn antitumor structure activity human antitumor lexitropsin bromoacryloyl structure activity
Subjects:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Owner: Prof. Dr. Joerg Heilmann
Deposited On:18 Oct 2010 12:50
Last Modified:18 Oct 2010 12:50
Item ID:17226
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