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Data on synthesis of methylene bisphosphonates and screening of their inhibitory activity towards HIV reverse transcriptase.

Data on synthesis of methylene bisphosphonates and screening of their inhibitory activity towards HIV reverse transcriptase.
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Yanvarev DV, Korovina AN, Usanov NN, Khomich OA, Vepsäläinen J, Puljula E, Kukhanova MK, Kochetkov SN,


Yanvarev DV, Korovina AN, Usanov NN, Khomich OA, Vepsäläinen J, Puljula E, Kukhanova MK, Kochetkov SN, (click to view)

Yanvarev DV, Korovina AN, Usanov NN, Khomich OA, Vepsäläinen J, Puljula E, Kukhanova MK, Kochetkov SN,

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Data in brief 2016 07 268() 1157-67 doi 10.1016/j.dib.2016.07.039

Abstract

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].

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