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. 2016 Jul 26:8:1157-67.
doi: 10.1016/j.dib.2016.07.039. eCollection 2016 Sep.

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

D V Yanvarev  1 , A N Korovina  1 , N N Usanov  1 , O A Khomich  1 , J Vepsäläinen  2 , E Puljula  2 , M K Kukhanova  1 , S N Kochetkov  1
Affiliations

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

D V Yanvarev et al. Data Brief. .

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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Figures

Fig. 1.
Fig. 1
The bisphosphonates synthesized for this publication.
Fig. 2.
Fig. 2
Bisphosphonates synthesized previously and studied as HIV RT inhibitors.
Fig. 3.
Fig. 3
PAGE of RT catalyzed pyrophosphorolysis inhibited by 2, 5, 10, 20, 50, and 100 μM of BPs 1, 12, 13 and 20, 50, 100, 200, and 500 μM of BP 3.
Fig. 4.
Fig. 4
PAGE of RT catalyzed (A) pyrophosphorolysis inhibited by 2, 5, 20, 50, and 100 μM of BPs 12 and 13; (B) elongation inhibited by 20, 50, 100, 200, and 500 μM of BPs 12 and 13.
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References

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