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Distinct Effects of Two HIV-1 Capsid Assembly Inhibitor Families That Bind the Same Site within the N-Terminal Domain of the Viral CA Protein
The development of an in vitro capsid assembly assay based on the association of CA-NC subunits on immobilized oligonucleotides is described and demonstrated that inhibitors that bind within the same site on CA can have distinct binding modes and mechanisms of action. Expand
Discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly.
Replacement of the enamine functionality of the hit series with either an imidazole or a pyrazole ring led to compounds that inhibited both capsid assembly and reverse transcriptase, leading to lead compound 48, a pure capsidAssembly inhibitor with improved antiviral activity. Expand
Identification of EZH2 and EZH1 small molecule inhibitors with selective impact on diffuse large B cell lymphoma cell growth.
These compounds represent a structurally distinct EZH2 inhibitor chemotype for the exploration of the role of Polycomb Repressive Complex 2-mediated H3K27 methylation in various biological contexts. Expand
Thiotetrazole alkynylacetanilides as potent and bioavailable non-nucleoside inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases.
A series of aryl thiotetrazolylacetanilides were synthesized and found to be potent inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases, with one inhibitor having good oral bioavailability in rats. Expand
Investigation on the role of the tetrazole in the binding of thiotetrazolylacetanilides with HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases.
The replacement of the tetrazole by a pyrazolyl group led to reversal of selectivity, providing inhibitors with excellent potency against the double mutant reverse transcriptase. Expand
Inhibition of HIV-1 capsid assembly: optimization of the antiviral potency by site selective modifications at N1, C2 and C16 of a 5-(5-furan-2-yl-pyrazol-1-yl)-1H-benzimidazole scaffold.
A uHTS campaign led to the discovery of a 5-(5-furan-2-ylpyrazol-1-yl)-1H-benzimidazole series that inhibits assembly of HIV-1 capsid. Synthetic manipulations at N1, C2 and C16 positions improved theExpand
Direct N-cyclopropylation of cyclic amides and azoles employing a cyclopropylbismuth reagent.
The direct cyclopropyl transfer reaction onto cyclic amides, isatins, oxindoles, imides, and carbamates employing a nonpyrophoric cycloprostylbismuth reagent is reported, developing an expedient method to N-cyclopropylate azoles and amides. Expand
Arylcyclopropanes: Properties, Synthesis and Use in Medicinal Chemistry
Introduction ............................................................................................. 2 1. Conjugative, Physical and Conformational Properties ............................... 3Expand
Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2.
A concise and modular synthesis enabled the rapid development of structure-activity relationships, which led to the identification of 44 as a potent, SAM-competitive inhibitor of EZH2 that dose-dependently decreased global H3K27me3 in KARPAS-422 lymphoma cells. Expand
Discovery, design, and synthesis of indole-based EZH2 inhibitors.
The discovery and optimization of a series of small molecule EZH2 inhibitors is described, which demonstrates nanomolar levels of biochemical potency, cellular potency, and afforded tumor regression when dosed in an EZh2 dependent tumor xenograft model. Expand