Data on synthesis of methylene bisphosphonates and screening of their inhibitory activity towards HIV reverse transcriptase
| Autor: | Sergey N. Kochetkov, A. N. Korovina, N.N. Usanov, Marina K. Kukhanova, Olga A. Khomich, Elina Puljula, Jouko Vepsäläinen, Dmitry V. Yanvarev |
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| Přispěvatelé: | Faculty of Health Sciences, School of Pharmacy, Activities |
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
lcsh:Computer applications to medicine. Medical informatics Inhibitory postsynaptic potential 01 natural sciences Chemical synthesis 03 medical and health sciences chemistry.chemical_compound Urea page Methylene lcsh:Science (General) Data Article Phosphorolysis chemistry.chemical_classification Multidisciplinary 010405 organic chemistry Thymidine analogue Reverse transcriptase 3. Good health 0104 chemical sciences 030104 developmental biology Enzyme Biochemistry chemistry lcsh:R858-859.7 hormones hormone substitutes and hormone antagonists lcsh:Q1-390 |
| Zdroj: | Data in Brief, Vol 8, Iss, Pp 1157-1167 (2016) Data in Brief |
| ISSN: | 2352-3409 |
| DOI: | 10.1016/j.dib.2016.07.039 |
| Popis: | Article Inorganic pyrophosphate (PPi) mimetics designed on a basis of methylenediphosphonic acid backbone are promising inhibitors of two key HIV replication enzymes, IN [1] and RT [2]. Herein, we present chemical synthesis of eleven methylenebisphosphonates (BPs) with their NMR and HRMS analysis synthesized via five different ways. Also, we present data on inhibition of HIV RT catalyzed phosphorolysis and polymerization by synthesized BPs using two methods based on denaturing urea PAGE. Tests were also performed for thymidine analogue mutations reverse transcriptase (TAM RT), which was expressed and purified for that. Structure–activity relationships and inhibitory activity data of synthesized BPs are presented in “Methylene bisphosphonates as the inhibitors of HIV RT phosphorolytic activity” [2]. published version http://purl.org/eprint/status/PeerReviewed |
| Databáze: | OpenAIRE |
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