172957-71-0Relevant academic research and scientific papers
Specific features of HIV-1 integrase inhibition by bisphosphonate derivatives
Agapkina, Julia,Yanvarev, Dmitry,Anisenko, Andrey,Korolev, Sergey,Veps?l?inen, Jouko,Kochetkov, Sergey,Gottikh, Marina
, p. 73 - 82 (2014)
The integration of viral DNA into the cell genome is one of the key steps in the replication cycle of human immunodeficiency virus type 1 (HIV-1). Therefore, the viral enzyme integrase (IN) catalyzing this process is of great interest as a target for new
Methylene bisphosphonates as the inhibitors of HIV RT phosphorolytic activity
Yanvarev,Korovina,Usanov,Khomich,Veps?l?inen,Puljula,Kukhanova,Kochetkov
, p. 153 - 162 (2016/06/13)
The structure-function analysis of 36 methylenebisphosphonates (BPs) as inhibitors of the phosphorolytic activity of native and drug-resistant forms of HIV-1 reverse transcriptase (RT) was performed. It was shown that with the increase of the inhibitory potential of BPs towards the phosphorolytic activity raises their ability to inhibit the RT-catalyzed DNA elongation. Herein, we report the impact of the thymidine analog mutations (TAM) on the activity of bisphosphonates, as well as some structural features of the BPs, allowing them to maintain the inhibitory activity on the enzyme resistant to nucleoside analog therapy. We estimated the Mg2+-coordinating group structure, the linker and the aromatic pharmacophore influence on the inhibitory potential of the BPs. Based on the 31 BPs SAR, several BPs with improved inhibitory properties were designed and synthesized.
Herbicidal aza bisphosphonic acids and compositions containing the same
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, (2008/06/13)
Herbicidal compositions containing a bisphosphonic acid compound of the formula STR1 wherein n is 0, 1, 2, 3, 4, 5 or 6, or an agrochemically acceptable salt or hydrolyzable ester thereof and methods of controlling undesirable plant growth using these bis
