39861-21-7Relevant articles and documents
Small molecule inhibition of microRNA-21 expression reduces cell viability and microtumor formation
Ankenbruck, Nicholas,Kumbhare, Rohan,Naro, Yuta,Thomas, Meryl,Gardner, Laura,Emanuelson, Cole,Deiters, Alexander
supporting information, p. 3735 - 3743 (2019/07/03)
MicroRNAs (miRNAs) are short, non-coding RNA molecules estimated to regulate expression of a large number of protein-coding genes and are implicated in a variety of biological processes such as development, differentiation, proliferation, and cell surviva
Structure-guided design and development of novel benzimidazole class of compounds targeting DNA gyraseB enzyme of Staphylococcus aureus
Janupally, Renuka,Jeankumar, Variam Ullas,Bobesh, Karyakulam Andrews,Soni, Vijay,Devi, Parthiban Brindha,Pulla, Venkat Koushik,Suryadevara, Priyanka,Chennubhotla, Keerthana Sharma,Kulkarni, Pushkar,Yogeeswari, Perumal,Sriram, Dharmarajan
, p. 5970 - 5987 (2015/01/08)
The gyraseB subunit of Staphylococcus aureus DNA gyrase is a well-established and validated target though less explored for the development of novel antimicrobial agents. Starting from the available structural information in PDB (3TTZ), we identified a novel series of benzimidazole used as inhibitors of DNA gyraseB with low micromolar inhibitory activity by employing structure-based drug design strategy. Subsequently, this chemical class of DNA gyrase inhibitors was extensively investigated biologically through in vitro assays, biofilm inhibition assays, cytotoxicity, and in vivo studies. The binding affinity of the most potent inhibitor 10 was further ascertained biophysically through differential scanning fluorimetry. Further, the most potent analogues did not show any signs of cardiotoxicity in Zebra fish ether-a-go-go-related gene (zERG), a major breakthrough among the previously reported cardiotoxic gyraseB inhibitors.
Succinate derivative compounds useful as cysteine protease inhibitors
-
, (2008/06/13)
Disclosed are novel succinate derivative compounds of the formula(I)/(Ia): wherein R1, R2, R3, R4, R5, R6, R7, X and A are defined herein. The compounds are useful as inhibitors of cysteine proteases. Also disclosed are methods of using and methods of making such compounds.
Novel succinate derivative compounds useful as cysteine protease inhibitors
-
, (2008/06/13)
Disclosed are novel succinate derivative compounds of the formula (I)/(Ia): wherein R1, R2, R3, R4, R5, R6, R7, X and A are defined herein. The compounds are useful as inhibitors of cysteine proteases. Also disclosed are methods of using and methods of making such compounds.
SYNTHESIS AND STRUCTURE OF MONOCHLORO DERIVATIVES OF 2-(4-AMINOPHENYL)-5(6)-AMINOBENZIMIDAZOLE
Shchel'tsyn, V. K.,Frolova, T. I.,Grudtsyn, Yu. D.,Vandysheva, E. A.,Kaminskii, A. Ya.,Leonova, V. V.
, p. 2132 - 2142 (2007/10/02)
Methods for the production of the monochloro derivatives of 2-(4-aminophenyl)-5(6)-aminobenzimidazole from chloronitrobenzanilides or by the condensation of 1,2,4-triaminobenzene with chloroaminobenzoic acid were investigated.It was established that the nitration of o-chlorobenzanilides takes place selectively in a mixture of acetic acid, acetic anhydride, and chloroform, while the nitration of 4(7)- or 5(6)-chlorobenzimidazoles takes place in sulfuric acid.The effect of the chlorine atoms and the nitro (amino) group on the IR and PMR spectra of the benzanilides and benzimidazoles is determined by their mutual position and by the position in relation of the amide bridge or the condensed imidazole ring.Analysis of the PMR spectra of the chlorodiaminophenylbenzimidazoles indicated that the amino group was localized at position 6 of the benzimidazole ring.
