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Document Figure 9 Chemical structures of reported inhibitors of HIV-1 integrase. (I) aurintricarboxylic acid monomer; (II) cosalane; (III) dihydronaphthoquinone or DHNQ; (IV) primaquine; (V) caffeic acid phenethyl ester or CAPE; (VI) quercetin; (VII) quercetagetin; (VIII) AG1717; (IX) β-conidendrol; (X) suramin; (XI) curcumin. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_105.html (1 of 2) [4/5/2004 4:52:14 PM] Page 105
Document Page 106 on the same ring or can potentially be positioned close together in three-dimensional space if rings stack on top of each other. More recently it was shown that cosalane (II), a steroid-substituted derivative of (I), was no better in inhibiting integrase in vitro than the parent compound, but showed promise in HIV cytopathicity cell-culture assays [45]. Although cosalane and a number of related analogues inhibit both HIV protease and integrase in vitro, the primary site of action is believed to be inhibition of gp120 binding to CD4 receptors. In 1993, the effects of selected topoisomerase II inhibitors, antimalarial agents, DNA binders, naphthoquinones, and various other agents on integrase activity in vitro were investigated [46]. Although certain effective topoisomerase inhibitors are also good HIV integrase inhibitors, this is not a generalizable correlation. Since many topoisomerase inhibitors also bind DNA, it is difficult to assess whether the observed in vitro effects result from specific interaction with integrase or from the sequestering or distorting of the DNA substrate. However, several compounds were identified that are not known to be DNA binders but that inhibited integrase with reasonable IC 50 values. These included dihydroxynaphthoquinone (III), primaquine (IV), caffeic acid phenethyl ester (CAPE, V), and quercetin (VI). Motivated by the structural similarities between compounds III–VI, a more intensive structure-function study of flavones was undertaken in which approximately 50 related compounds were screened for inhibition of in vitro integrase activity [47]. Flavones are planar compounds containing three aromatic rings substituted with various polar groups such as hydroxy substituents. General trends were observed relating structure to inhibitory effectiveness; for example, inhibition required at least three hydroxy groups, the most favorable arrangement being when they were located ortho to one another. The most effective compound, quercetagetin (VII), is a potent topoisomerase II inhibitor and a known DNA intercalator. It was noted by the authors that many flavones are not integrase-specific; rather, they inhibit a broad range of enzymes including DNA polymerases, ATPases, and NAPDH-monooxygenases. They are also, in general, capable of DNA intercalation. It has not been established that their inhibitory effects are due to direct interactions with integrase. A subsequent detailed structure-activity relationship study of CAPE (V) revealed that while the ortho hydroxys were important for in vitro integrase inhibition, both the caffeic acid and phenethyl moieties could be substantially modified [48]. Ortho hydroxyl groups in the context of other classes of compounds also confer anti-integrase potency. For example, several semisynthetic compounds derived from arctigenin, a topoisomerase I inhibitor that itself is not active against integrase, have been shown to inhibit HIV integrase [49]. More compelling evidence of the importance of ortho hydroxyl groups was provided by the tyrphostins, a group of synthetic compounds that are tyrosine kinase inhibitors. Several of these also inhibit integrase in the submicromolar range http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_106.html [4/5/2004 4:52:16 PM]
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Structure-based Drug Design 14 Stru
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Document Analysis of various HIV-1
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Document Page 54 Table 2) [12,54].
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Document Table 3 HIV-1 RT Amino Aci
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Page 85 and 86: Document Chris Tantillo. The work i
Page 87 and 88: Document Page 72 16. Goldman ME, Nu
Page 89 and 90: Document 30. Coffin JM. HIV populat
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Page 101 and 102: Document 122. Marshall WS, Beaton G
Page 103 and 104: Document dine) and didanosine (dide
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Page 107 and 108: Document 163. Lacey SF, Larder BA.
Page 109 and 110: Document Figure 1 Retroviral lifecy
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Page 117 and 118: Document Page 92 The role of the N-
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Page 139 and 140: Document cubation of phosphotyrosin
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Page 149 and 150: Document 4 Bradykinin Receptor Anta
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Page 169 and 170: Document Figure 6 Rat and human B2
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Document Table 1 Inhibition Data fo
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Document Page 166 As predicated, th
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Document 6 Structural Implications
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Document Table 1 Known Three-Dimens
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Document Page 398 with growth hormo
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Document All effects of the IL-1 fa
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Document Page 405 strands constitut
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Document 17 Structure and Functiona
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Document Table 1 Approval Indicatio
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Document Page 438 proteins. One pot
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Document II. Type IFNs A great deal
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Document Page 443 that allowed for
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Document Figure 6 Proposed receptor
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Document Page 462 strains of influe
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Document B. Protein Structure Page
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Document Page 471 molecules in the
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Document Page 476 nM, respectively.
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Document A. The Canyon Page 491 The
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Document Subsequent studies have sh
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Document Page 495 of the RNA and pr
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Document Figure 4 A ribbon diagram
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Document Figure 5 Some compounds wh
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Document Figure 7 HRV14 VP1 hydroph
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Document D ddI, 152 tumour necrosis
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Document antistasin peptides, 281 c
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Document Phosphoglycerate kinase (P
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Document [Protease targets] serinyl
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