التفاصيل البيبلوغرافية
| العنوان: |
Synthesis and Cytotoxic Evaluation of Arimetamycin A and Its Daunorubicin and Doxorubicin Hybrids |
| المؤلفون: |
Eric D. Huseman (11172057), Jo Ann W. Byl (9542402), Scott M. Chapp (11172060), Nathan D. Schley (1863295), Neil Osheroff (16602), Steven D. Townsend (1903363) |
| سنة النشر: |
2021 |
| المجموعة: |
Smithsonian Institution: Digital Repository |
| مصطلحات موضوعية: |
Biophysics, Biochemistry, Medicine, Microbiology, Molecular Biology, Pharmacology, Biotechnology, Chemical Sciences not elsewhere classified, Physical Sciences not elsewhere classified, daunorubicin, IC 50, Cytotoxic Evaluation, supercoiled DNA, parent anthracyclines, Doxorubicin Hybrids, arimetamycin, topoisomerase II α, cytotoxicity, acyl donor, steffimycin B, deoxy-amino disaccharide, anthracycline aglycones |
| الوصف: |
The arimetamycin A glycan governs the compound’s cytotoxicity (IC 50 ). To study this branched, deoxy-amino disaccharide, we designed and synthesized a modified acyl donor that underwent glycosylation with three anthracycline aglycones: steffimycinone, daunorubicinone, and doxorubicinone. The result of the approach was a synthesis of arimetamycin A and two novel hybrid anthracyclines. Each molecule exhibited enhanced cytotoxicity in comparison to the parent anthracyclines, steffimycin B, daunorubicin, and doxorubicin. An orienting mechanistic evaluation revealed that the daunorubicin hybrid inhibits the ability of human topoisomerase IIα to relax negatively and positively supercoiled DNA. |
| نوع الوثيقة: |
article in journal/newspaper |
| اللغة: |
unknown |
| Relation: |
https://figshare.com/articles/journal_contribution/Synthesis_and_Cytotoxic_Evaluation_of_Arimetamycin_A_and_Its_Daunorubicin_and_Doxorubicin_Hybrids/15036357 |
| DOI: |
10.1021/acscentsci.1c00040.s001 |
| الاتاحة: |
https://doi.org/10.1021/acscentsci.1c00040.s001 |
| Rights: |
CC BY-NC 4.0 |
| رقم الانضمام: |
edsbas.7DB65752 |
| قاعدة البيانات: |
BASE |