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Literature DB >> 30108953

Synthesis and radioprotective effects of novel benzyl naphthyl sulfoxide (sulfone) derivatives transformed from Ex-RAD.

Lin Tang¹, Tao Peng¹, Gang Wang¹, Xiaoxue Wen¹, Yunbo Sun¹, Shouguo Zhang¹, Shuchen Liu¹, Lin Wang¹.

Abstract

In this work, a series of novel benzyl naphthyl sulfoxides (sulfones) derived from Ex-RAD were designed and synthesized as potential radioprotective agents. Some of the compounds considerably protected HUVECs against 60Co γ-irradiation, accompanied by the absence of cytotoxicity. Compared to Ex-RAD, compound 8n not only exhibited a significant protective effect on cell survival and radiation-induced DNA damage, but also remarkably enhanced the survival (100%) of mice in 30 days after being exposed to irradiation. The results suggested that some target compounds are valuable for further research as promising radioprotectors.

Entities: Chemical Disease Species

Year: 2018 PMID： 30108953 PMCID： PMC6072350 DOI： 10.1039/c7md00573c

Source DB: PubMed Journal: Medchemcomm ISSN： 2040-2503 Impact factor: 3.597

12 in total

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Journal: Crit Care Clin Date: 1999-04 Impact factor: 3.598

2. Amifostine, a radioprotectant agent, protects rat brain tissue lipids against ionizing radiation induced damage: an FTIR microspectroscopic imaging study.

Authors: Gulgun Cakmak; Lisa M Miller; Faruk Zorlu; Feride Severcan
Journal: Arch Biochem Biophys Date: 2012-03-03 Impact factor: 4.013

3. Radioprotective effects of ON 01210.Na upon oral administration.

Authors: Shubhankar Suman; Kamal Datta; Kathryn Doiron; Chen Ren; Ramesh Kumar; David R Taft; Albert J Fornace; Manoj Maniar
Journal: J Radiat Res Date: 2012-05-11 Impact factor: 2.724

4. Subcutaneous administration of amifostine during fractionated radiotherapy: a randomized phase II study.

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Journal: J Clin Oncol Date: 2000-06 Impact factor: 44.544

5. Effects of formulation and route of administration on the systemic availability of Ex-RAD®, a new radioprotectant, in preclinical species.

Authors: Amy W Chun; Robert E Freshwater; David R Taft; Amanda M Gillum; Manoj Maniar
Journal: Biopharm Drug Dispos Date: 2011-01-14 Impact factor: 1.627

6. Radiation protection by a new chemical entity, Ex-Rad: efficacy and mechanisms.

Authors: Sanchita P Ghosh; Michael W Perkins; Kevin Hieber; Shilpa Kulkarni; Tzu-Cheg Kao; E Premkumar Reddy; M V Ramana Reddy; Manoj Maniar; Thomas Seed; K Sree Kumar
Journal: Radiat Res Date: 2009-02 Impact factor: 2.841

7. Administration of ON 01210.Na after exposure to ionizing radiation protects bone marrow cells by attenuating DNA damage response.

Authors: Shubhankar Suman; Manoj Maniar; Albert J Fornace; Kamal Datta
Journal: Radiat Oncol Date: 2012-01-20 Impact factor: 3.481

Synthesis and radioprotective effects of novel benzyl naphthyl sulfoxide (sulfone) derivatives transformed from Ex-RAD.

Review 1. Radiation injuries.

2. Amifostine, a radioprotectant agent, protects rat brain tissue lipids against ionizing radiation induced damage: an FTIR microspectroscopic imaging study.

3. Radioprotective effects of ON 01210.Na upon oral administration.

4. Subcutaneous administration of amifostine during fractionated radiotherapy: a randomized phase II study.

5. Effects of formulation and route of administration on the systemic availability of Ex-RAD®, a new radioprotectant, in preclinical species.

6. Radiation protection by a new chemical entity, Ex-Rad: efficacy and mechanisms.

7. Administration of ON 01210.Na after exposure to ionizing radiation protects bone marrow cells by attenuating DNA damage response.

Review 8. Radiation countermeasure agents: an update (2011-2014).

9. Amelioration of radiation-induced hematopoietic and gastrointestinal damage by Ex-RAD(R) in mice.

10. ON01210.Na (Ex-RAD®) mitigates radiation damage through activation of the AKT pathway.

1. Protective effects of new aryl sulfone derivatives against radiation-induced hematopoietic injury.

2. Synthesis and antitumor effects of novel benzyl naphthyl sulfoxide/sulfone derivatives derived from Rigosertib.

3. Design, Synthesis, and Biological Evaluation of a Novel Aminothiol Compound as Potential Radioprotector.