Literature DB >> 22041059

Synthesis and growth regulatory activity of a prototype member of a new family of aminothiol radioprotectors.

Richard R Copp1, Daniel D Peebles, William E Fahl.   

Abstract

The synthesis, growth inhibition and radioprotective activity of the PrC-210 aminothiol, 3-(methylamino)-2-((methylamino)methyl)propane-1-thiol, and its polyamine and thiolated polyamine progenitors are reported. All of the molecules significantly inhibited growth of cultured normal human fibroblasts. The combination of an ROS-scavenging thiol group and a positively charged alkyl-amine backbone provided the most radioprotective aminothiol molecule.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 22041059      PMCID： PMC3254260          DOI： 10.1016/j.bmcl.2011.10.011

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  12 in total

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Journal:  J Med Chem       Date:  2001-02-01       Impact factor: 7.446

4.  Antiproliferative properties of polyamine analogues: a structure-activity study.

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Journal:  J Med Chem       Date:  1994-10-14       Impact factor: 7.446

5.  Polyamine depletion in human melanoma cells leads to G1 arrest associated with induction of p21WAF1/CIP1/SDI1, changes in the expression of p21-regulated genes, and a senescence-like phenotype.

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8.  Prophylaxis and management of acute radiation-induced skin reactions: a systematic review of the literature.

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  11 in total

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Authors:  Daniel D Peebles; Cheryl M Soref; Richard R Copp; Allen L Thunberg; William E Fahl
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2.  Significant Suppression of CT Radiation-Induced DNA Damage in Normal Human Cells by the PrC-210 Radioprotector.

Authors:  Frank Jermusek; Chelsea Benedict; Emma Dreischmeier; Michael Brand; Michael Uder; Justin J Jeffery; Frank N Ranallo; William E Fahl
Journal:  Radiat Res       Date:  2018-05-21       Impact factor: 2.841

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5.  Radioprotective efficacy and toxicity of a new family of aminothiol analogs.

Authors:  Richard R Copp; Daniel D Peebles; Cheryl M Soref; William E Fahl
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6.  Determination of plasma levels of the active thiol form of the direct-acting PrC-210 ROS-scavenger using a fluorescence-based assay.

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8.  Reduction of X-ray-induced DNA damage in normal human cells treated with the PrC-210 radioprotector.

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9.  Significant reduction of ischemia-reperfusion cell death in mouse myocardial infarcts using the immediate-acting PrC-210 ROS-scavenger.

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10.  Polycysteine as a new type of radio-protector ameliorated tissue injury through inhibiting ferroptosis in mice.

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