Anti-HIV-activity

Gold Complexes with Anti-arthritic, Anti-tumour and Anti-HIV Activity 

Prospects for Gold-Based Anti-Cancer Drugs 

Tepperman and colleagues have found that A CN) - is taken up into H9 cells, a continuous T-cell line that is susceptible to HIV infection. At concentrations as low as 20ppb, it retards the proliferation of HIV in these cells. The concentration used is well tolerated in arthritis patients, which suggests that Au(CN)2 may have promise as a complement for existing HIV treatments.  

in The Columbia University Complete Home Medical Guide, ed. D.F. Tapley, T.Q. Morris, L.P. Rowland and R.J. Wiess, Crown, New York, 1989, pp. 602-625. 

In the context of treating AIDS, there has been recent excitement from the research of anti-HIV properties of gold complexes. Reverse transcriptase (RTase) is an enzyme 

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Heterocyclic sulfone derivatives with anti-HIV activity 97F321. 

Naphtho[l, 2 4,5]thiazolo[3,2-h][l,2,4]triazines 1052 were prepared by cyclocondensation of aminoiminonaphthothiazole 1051 with an acetylenedicarboxylate. Methyl ester 1052 was tested in vitro for anti-HIV activity and was inactive (91MI6). 

Ivanova G, Arzumanov A A, Turner JJ et al (2006) Anti-HIV activity of steric block oligonucleotides. Ann NY Acad Sci 1082 103-115... 

Wang J, Jin Y, Rapp KL, Schinazi RF, Chu CK (2007) D- and L-2, 3 -didehydro-2, 3 -dideoxy-3 -fluoro-carbocyclic nucleosides synthesis, anti-HIV activity and mechanism of resistance. J Med Chem 50 1828-1839... 

Ji C, Brandt M, Dioszegi M, Jekle A, Schwoerer S, ChaUand S, Zhang J, Chen Y, Zautke L, Achhammer G, Baehner M, Kroetz S, HeUek-Snyder G, Schumacher R, Cammack N, Sankuratri S (2007) Novel CCR5 monoclonal antibodies with potent and broad-spectrum anti-HIV activities. Antiviral Res 74 125-137... 

CD26/DPP1V 3-70 Inc. CK on CCRl CCR5/keep anti-HIV activity Proost et al. (2000)... 

Part 2 lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity. Eioorg. Med. Chem. Lett. 2001, 11, 2741-2745. 

Gao, Y., Katsuraya, K., Kaneko, Y., Mimura, T., Nakashima, H., and Uryu, T., Synthesis, enzymatic hydrolysis, and anti-HIV activity of AZT-spacer-curdlan sulfates, Macromolecules, 32, 8319, 1999. 

In addition, HIV-1 infection also induces the secretion of certain metallo-proteinases (MMP-2, MMP-9) that are capable of cleaving the N-terminus of SDF-1 but not that of the P-chemokines, and this decreases SDF-1 affinity for CXCR4 binding (227-229). Proteolytic modification of SDF-1 by a serum factor(s) that is different from CD26 and MMPs, which results in reduced anti-HIV activity, has been described as well (230). How SDF-1 proteolytic... 

Struyf S, Proost P, Schols D, et al. CD26/dipeptidyl-peptidase IV down-regulates the eosinophil chemotactic potency, but not the anti-HIV activity of human eotaxin by affecting its interaction with CC chemokine receptor 3. J Immunol 1999 162 4903 1909. 

The HEPT and TIBO derivatives were discovered as the result of a systematic evaluation for anti-HIV activity in cell culture. They were later found to achieve their anti-HIV-1 activity through an interaction with the HIV-1 RT. In contrast, nevirapine, pyridinone, and BHAP emerged from a screening program for HIV-1 RT inhibitors. The anti-HIV-1 activity of these compounds was subsequently confirmed in cell culture. Like the HEPT and TIBO derivatives, the 2, 5 -bis-0-(tert-butyldimethylsilyl)-3 -spiro-5" -(4" -amino-1", 2" -oxathiole-2", 2" -dioxide)-pyrimidine (TS AO) derivatives (Fig. 9) [65,66] and a-anilinophenylacetamides (a-APA) (Fig. 10) [67] were discovered through the evaluation of their anti-HIV activity in cell culture. Subsequently, they were found to act as specific inhibitors of HIV-1 RT. 

De Clercq E. Anti-HIV activity of sulfated polysaccharides. In Yalpani M, ed. Carbohydrates and Carbohydrate Polymers, Analysis, Biotechnology,... 

Barzu T, Level M, Petitou M, Lormeau J-C, J. Choay J, Schols D, Baba M, Pauwels R, Witvrouw M, De Clercq E. Preparation and anti-HIV activity of O-acylated heparin and dermatan sulfate derivatives with low anticoagulant effect. J Med Chem 1993 36 3546-3555. 

Balzarini J, Van Aerschot A, Pauwels R, Baba M, Schols D, Herdewijn P, De Clercq E. 5-Halogeno-3 -fluoro-2, 3 -dideoxyuridines as inhibitors of human immunodeficiency virus (HIV) potent and selective anti-HIV activity of 3 -fhroro-2, 3 -dideoxy-5-chlorouridine. Mol Pharmacol 1989 35 571-577. 

Shaw, C. Gold Complexes with Anti-arthritic, Anti-tumour and Anti-HIV Activity In Uses of Inorganic Chemistry in Medicine, Farrell, N., Ed. The Royal Society of Chemistry Cambridge, 1999, pp 26-57. 

T. Dutta and N. K. Jain, Targeting potential and anti-HIV activity of lamivudine loaded mannosylated poly(propyleneimine) dendrimer, Biochim. Biophys. Acta Gen. Subj., 1770 (2007) 681-686. 

Pyridine- and pyran-fused benzothiepin-SS-dioxide derivatives of types 74 and 75 (X = SO2) have been prepared by standard annelation procedures from the benzothiepin ketone derivatives. A number of the bis-fused derivatives showed good anti-cancer and moderate anti-HIV activity <00ZN(B)417>. 

The new heterocyclic system represented by compounds of type 147 (eg. R = Cl), and containing a bis-fused [l,3,4]thiadiazepine moiety, was prepared by cyclocondensation of 1-aminobenzimidazoIe-2-thione with 6-chloropyrimidine-5-carboxaldehydes. Some representatives of the system (e.g. 147, R = NMe2> showed anti-HIV activity <00SC3719>. 

A dimeric cyclam (biscyclam) 8 [ 12], with two cyclam moieties linked by a 3,6-dioxaoctane-l,8-diyl group at the C(6) positions, showed a remarkably improved anti-HIV activity after 4 days with the EC50 value... 

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