TABLE 4.

Putative Tat antagonists that significantly reduce HIV transcription^a

Compound(s)	Infection stage(s) tested	Cell type(s)	Screen	Development status	Reference(s)
VRX496 (Lexgenleucel-T)	Acute, chronic	CD4+ T cells, CD34+ hematopoietic stem cells	NA	Phase 2	121, 171, 174 – 178
Rev-TD-anti-TAR	Acute, chronic	CD4+ T cells	NA	Phase 1/2	172, 173
dCA	Acute, chronic	HeLa-CD4, T-cell lines, PBMCs, primary CD4+ T cells	NA	Preclinical	158 – 160, 164
Durhamycin A	Acute	HeLa-CD4, T-cell lines	LTR-reporter	Preclinical	179
WM5	Acute, chronic	HeLa, T-cell lines, PBMCs	SAR	Preclinical	180 – 183
NM13	Acute	T-cell line	SAR	Preclinical	184, 185
HM13N	Acute, chronic, latent	T-cell lines, monocytic cell lines, PBMCs	SAR	Preclinical	186
Temacrazine	Acute, chronic, latent	T-cell line, monocytic cell lines	NA	Preclinical	187
NeoR	Acute, chronic	T-cell line, promonocytic cell line, PBMCs	SAR	Preclinical	188
3-(4-Chlorophenyl)-5-methyl-N-(3-pyridinyl-methyl)pyrazolo[1,5-a]pyrimidin-7-amine (compound 791), N-{[2-(2-hydroxybenzoyl)hydrazine]carbonothiol}-4-biphenylcarboxamide (compound 833), 2-hydroxy-N′-(3-hydroxy-4-methoxybenzylidene)benzohydrazide (compound 892)	Acute, chronic, latent	T-cell lines, CEM-GXR, PBMCs, HeLa HIVrtTAΔMls (189)	SMN2 minigene reporter	Preclinical	168

^aBased on data from reference 157. Abbreviations: NA, not available; SAR, structure-activity relationship; PBMCs, peripheral blood mononuclear cells.