308846-64-2Relevant academic research and scientific papers
Synthesis and antiviral activities of novel acylhydrazone derivatives targeting HIV-1 capsid protein
Tian, Baohe,He, Meizi,Tang, Shixing,Hewlett, Indira,Tan, Zhiwu,Li, Jiebo,Jin, Yinxue,Yang, Ming
scheme or table, p. 2162 - 2167 (2009/12/25)
HIV-1 capsid protein (CA) plays important roles in the viral replication cycle. A number of acylhydrazone derivatives that act as inhibitors of HIV-1 CA assembly, were designed and synthesized. The synthesized compounds were tested for their antiviral activities and cytotoxicities using CEM cells. Some derivatives also were assayed for their ability to inhibit HIV-1 CA assembly in vitro. Among them, compounds 14f and 14i display the most promising potency with EC50 values of 0.21 and 0.17 μΜ, respectively.
Constrained analogues of procaine as novel small molecule inhibitors of DNA methyltransferase-1
Castellano, Sabrina,Kuck, Dirk,Sala, Marina,Novellino, Ettore,Lyko, Frank,Sbardella, Gianluca
, p. 2321 - 2325 (2008/12/22)
Constrained analogues of procaine were synthesized, and their inhibiting activity against DNMT1 was tested. Among them, the most potent compound, derivative 3b, was also able to induce a recognizable demethylation of chromosomal satellite repeats in HL60 human myeloid leukemia cells and thus represents a lead compound for the development of a novel class of non-nucleoside DNMT1 inhibitors.
