J Med Chem.2006 49 727 739
Loteprednol Etabonate_82034-46-6_DataSheet_MedChemExpress
Product Name:Loteprednol Etabonate CAS No.:82034-46-6Cat. No.:HY-17358Product Data SheetMWt:466.95Formula:C24H31ClO7Purity :>98%Solubility:DMSO 90 mg/mL; Water <1 mg/mL y Mechanisms:Biological Activity:Loteprednol Etabonate is an anti inflammatory corticosteroid used in optometry and ophthalmologyPathways:GPCR/G protein; Target:Glucocorticoid Receptor g gLoteprednol Etabonate is an anti-inflammatory corticosteroid used in optometry and ophthalmology.IC50 Value:Target: Glucocorticoid Receptorin vitro:in vivo: Intravenous administration of loteprednol etabonate (5 mg/kg) to dogs revealed a terminal half-life of 2.8 h, a volume of distribution of 3.7 L/kg, and a total body clearance of 0.9 L/h/kg. Intact loteprednol etabonate was not detectable in the urine. After oral administration of the drug (5 mg/kg)to dogs, only metabolites, but no intact drug, were found in the plasma, an indication for a high first-pass effect. A pronounced binding of the drug to plasma protein (> 90%) and a high erythrocyte-References:[1]. Noble S, Goa KL. Loteprednol etabonate: clinical potential in the management of ocularinflammation. BioDrugs. 1998 Oct;10(4):329-39.[2]. Szelenyi I, Hochhaus G, Heer S et al. Loteprednol etabonate: a soft steroid for the treatment of p p g g p p ()g y ybuffer partition coefficient of 7.8 were determined in vitro....allergic diseases of the airways. Drugs Today (Barc). 2000 May;36(5):313-20.[3]. Howes JF. Loteprednol etabonate: a review of ophthalmic clinical studies. Pharmazie. 2000Mar;55(3):178-83.[4]. Pavesio CE, Decory HH. Treatment of ocular inflammatory conditions with loteprednoletabonate. Br J Ophthalmol. 2008 Apr;92(4):455-9.[5]. Comstock TL, Decory HH. Advances in corticosteroid therapy for ocular inflammation:loteprednol etabonate. Int J Inflam. 2012;2012:789623.[6]. Loteprednol Caution: Not fully tested. For research purposes onlyMedchemexpress LLC18 W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S AE m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m。
LetPub_JCR2015_top500
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5.794 5.855 5.209 5.056 4.098 9.9169.4949.64710.02510.99210.77710.5397.559 5.5000.0000.0000.0000.0000.000 10.1109.57110.35510.30811.0499.6217.2448.8688.9018.1158.479 6.5627.1197.1959.4668.9879.6638.2887.6897.5057.111 11.77112.6900.0000.0000.0000.0000.000 9.5759.2518.9879.3969.2939.2969.653 9.1437.436 6.4757.758 6.9188.2847.510 9.2848.6507.8568.2347.5437.5147.672 8.5190.0000.0000.0000.0000.0000.000 7.572 5.2650.0000.0000.0000.0000.000 9.2678.9517.375 6.153 6.397 5.0290.000 8.6018.3147.5250.0000.0000.0000.000 10.2269.9159.4579.2309.4909.6038.568 9.3707.230 6.284 6.000 5.368 4.209 5.022 9.8088.4347.9107.500 6.894 6.1387.618 0.0000.0000.0000.0000.0000.0000.000 10.15410.4008.8337.4670.0000.0000.000 9.197 6.982 6.414 5.759 5.262 5.838 5.151 8.8169.1149.55912.31212.5819.412 6.435 8.8088.2788.0267.8367.479 6.878 6.954 14.30810.353 5.550 5.5109.8727.280 6.4387.8587.1897.3557.822 6.9077.0997.4508.385 6.7110.0000.0000.0000.0000.0008.9059.5999.6467.6008.250 6.110 5.2369.1329.50014.82917.18211.56812.02910.722 9.4169.3749.1548.1868.1958.266 6.750 7.8148.6009.04810.4040.0000.0000.000 10.2849.4408.6509.0157.7917.8048.147 6.306 5.484 4.260 2.683 3.343 3.624 2.137 9.8979.4399.45510.3407.755 6.3067.725 8.1937.8377.7427.338 6.747 6.488 6.250 8.2269.6309.402 5.3710.0000.0000.000 8.1097.5127.2940.0000.0000.0000.000 8.305 6.828 6.544 6.844 6.979 5.907 6.519 8.2457.79510.3338.8330.0000.0000.000 10.1888.8337.2278.0487.581 6.3647.732 0.0000.0000.0000.0000.0000.0000.000 8.5207.916 6.606 6.105 6.193 6.418 4.922 8.3127.6047.4047.8827.365 6.646 6.2628.3687.9437.092 4.7500.0000.0000.0009.1418.681 6.931 6.338 5.967 6.143 5.705 6.5527.480 6.962 5.759 4.857 3.462 3.500 6.111 6.3757.5007.0007.765 5.625 6.333 8.73611.41012.89713.54014.15312.54313.444 8.5597.357 6.3737.4147.1357.216 6.440 8.6078.4868.8008.2737.467 6.592 5.843 8.1319.58310.70010.2288.6568.9077.264 8.5707.7358.0877.141 6.7187.3497.851 7.0188.1457.3688.1367.2317.881 3.3917.5147.8238.3497.333 6.171 6.525 6.408 10.4599.1589.4477.8788.7838.2058.6897.2070.0000.0000.0000.0000.0000.0008.5358.2387.286 6.397 5.368 5.046 4.8837.188 6.3297.4927.4747.9008.4607.4468.5628.376 6.840 6.5257.0417.069 6.226 8.3038.2498.3128.0178.1727.043 6.014 8.755 5.855 5.800 6.434 4.489 3.158 3.788 8.1227.396 6.659 5.503 4.605 3.728 1.357 8.3858.3718.8499.0508.2407.5488.254 8.2500.0000.0000.0000.0000.0000.000 8.4747.8958.2868.8898.5058.3988.261 8.224 6.910 6.862 6.346 5.561 5.876 4.786 7.8277.8060.0000.0000.0000.0000.000 6.852 6.828 6.320 5.472 5.836 4.542 4.836 9.3137.9767.3889.297 5.814 4.3570.000 7.859 6.8707.038 5.862 5.086 5.5697.821 7.343 6.606 6.619 5.947 5.777 5.077 5.446 7.431 6.531 5.750 5.203 5.636 4.734 5.059 7.0297.2607.036 6.087 6.191 6.123 5.636 7.7199.7977.7567.7849.08211.7657.803 7.0957.975 6.624 6.556 6.368 5.371 3.862 7.7687.1497.905 6.886 6.263 5.579 4.803 7.390 6.846 6.043 6.378 6.9617.5868.0336.534 6.648 5.627 5.286 5.642 6.068 5.4657.1357.339 6.594 5.833 6.942 6.558 4.310 9.3858.4559.2729.43110.3338.6889.189 7.5849.0339.3809.88611.68510.2837.264 10.08311.87510.09111.23510.20012.1887.556 8.636 6.1698.1208.651 5.675 5.333 3.074 7.8717.4777.8668.435 4.1520.0000.000 6.482 5.379 6.274 5.216 5.479 2.9710.000 5.810 5.5787.65510.12510.2168.3068.933 8.0537.73510.4619.09110.62311.50710.896 7.2617.633 5.7327.164 5.949 5.690 4.756 0.000 6.736 6.645 6.516 6.033 5.178 5.249 7.1177.475 6.827 6.325 4.7670.0000.000 7.125 6.355 5.895 5.922 5.527 5.545 5.349 6.466 6.024 6.054 6.811 5.295 4.729 4.539 9.6967.712 5.789 5.627 4.702 2.652 2.179 8.5687.4708.0869.3818.9879.67710.150 0.0000.0009.1279.0798.9789.1259.336 0.0000.0008.6949.5439.5328.8838.721 7.7287.9437.3707.6217.3287.180 6.944 1.3390.6210.7410.0000.0000.0000.000 7.132 5.854 5.250 6.519 6.360 5.154 4.143 7.8678.7719.52210.14110.88110.4559.325 9.478 6.5837.208 4.875 3.773 2.545 3.375 6.687 6.585 6.2130.0000.0000.0000.000。
RepSox_446859-33-2_DataSheet_MedChemExpress
Caution: Not fully tested. For research purposes only Medchemexpress LLC
m o c . s s e r p x e m e h c d e m . w w w : b e AW Sm Uo , 0 c 4. 5s 8s 0e r p Jx Ne ,m n e oh t c e d ce nm i r P @ o , f yn a i Wl : ni a om s E n i k l i W 8 1
Product Data Sheet
Product Name: CAS No.: Cat. No.: MWt: Formula: Purity :
RepSox 446859-33-2 HY-13012 287.32 C17H13N5 >98%
Solubilithanisms: Pathways:TGF-beta/Smad ; Target:TGF-beta/Smad g Activity: y Biological Description: IC50 Value: N/A RepSox can efficiently replace transgenic Sox2 in the absence of VPA and cMyc, as well as in both embryonic and adult fibroblasts, we chose to further characterize E-616452 and named it RepSox, for Replacement of Sox2. in vitro: Pretreated MEFs with RepSox, applying the chemical for three days, and then removed it at the time of transduction with Oct4, Klf4, and cMyc. In these experiments, no Oct4+GFP+ colonies were formed, suggesting that RepSox does not act on the initial somatic cells to replace Sox2. Consistent with this result, we did not detect a significant increase in the expression of endogenous Sox2or closely related Sox family members upon RepSox treatment [1]. RepSox did increase by 5fold the expression of L-Myc, a close homolog of cMyc that can functionally replace it in References: [1]. Ichida JK, Blanchard J, Lam K, A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog. Cell Stem Cell. 2009 Nov 6;5(5):491-503.
Ebrotidine_100981-43-9_DataSheet_MedChemExpress
Product Name:Ebrotidine CAS No.:100981-43-9Cat. No.:HY-15538Product Data SheetMWt:477.42Formula:C14H17BrN6O2S3Purity :>98%Solubility:DMSOy Mechanisms:Biological Activity:Ebrotidine(FI 3542)is a competitive H2receptor antagonist (Ki=1275nM)with a potent Pathways:GPCR/G protein; Target:Histamine Receptor Ebrotidine(FI 3542) is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potentantisecretory activity and evidenced gastroprotection. IC50 Value: 127.5 nM (Ki)[1]; 0.21mg/kg (ED50, histamine- stimulated acid secretion) [2]Target: H2 receptor in vitro: Ebrotidine displaced 3H-thiotidine specific binding to histamine H2-receptors (Ki: 127.5nmol/l), showing a higher affinity (p < 0.05) than ranitidine (Ki: 190.0 nmol/l) and cimetidine (Ki:246.1 nmol/l) [1]. in vivo: Following intravenous administration to rats, ebrotidine inhibited histamine- and pentagastrin-stimulated acid secretion in a dose-dependent manner, ED50 being 0.21 and 0.44References:[1]. Agut J, Sánchez JC, Sacristán A, Action of ebrotidine, ranitidine and cimetidine on the specificbinding to histamine H1- and H2-receptors. Arzneimittelforschung. 1997 Apr;47(4A):447-9.[2]. Palop D, Agut J, Márquez M, Histamine H2-receptor antagonist action of ebrotidine. Effects on p g p ,gmg/kg, respectively [2]. The mean number of gastric erosions seen at endoscopy after treatment with ebrotidine plus ASA (2.0 +/- 0.3) was significantly lower than that after placebo plus ASA (3.7+/- 0.2). This reduction ...gastric acid secretion, gastrin levels and NSAID-induced gastrotoxicity in the rat.Arzneimittelforschung. 1997 Apr;47(4A):439-46.[3]. Konturek SJ, Kwiecien N, Sito E, Effects of ebrotidine on aspirin-induced gastric mucosaldamage and blood flow in humans. Scand J Gastroenterol. 1993 Dec;28(12):1047-50.[4]. Piotrowski J, Yamaki K, Morita M, Ebrotidine--a new H2-receptor antagonist with mucosalstrengthening activity. Biochem Int. 1992 Mar;26(4):659-67.Caution: Not fully tested. For research purposes onlyMedchemexpress LLC18 W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S AE m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m。
Atipamezole_104054-27-5_DataSheet_MedChemExpress
Product Name:Atipamezole CAS No.:104054-27-5Cat. No.:HY-12380A MWt:212.29Formula:C14H16N2Purity :>98%Solubility:Mechanisms:Biological Activity:References:Caution: Not fully tested. For research purposes onlyMedchemexpress LLC[1]. Jager LP, et al. Effects of atipamezole, detomidine and medetomidine on release of steroid hormones byporcine adrenocortical cells in vitro. Eur J Pharmacol. 1998 Apr 3;346(1):71-6.[2]. Biegon A, et al. Quantitative in vitro and ex vivo autoradiography of the alpha 2-adrenoceptor antagonist[3H]atipamezole. Eur J Pharmacol. 1992 Nov 24;224(1):27-38.[3]. Virtanen R, et al. Highly selective and specific antagonism of central and peripheral alpha 2-adrenoceptors by atipamezole. Arch Int Pharmacodyn Ther. 1989 Jan-Feb;297:190-204.Atipamezole(MPV1248) is an alpha-adrenoceptor antagonist with high affinity and selectivity for the alpha 2-receptor.IC50 value:Target: alpha2-adrenoceptor antagonist in vitro: The alpha2-adrenoceptor antagonist atipamezole was a potent inhibitor of aldosterone release (range 10-1000 nM) [1]. In receptor binding studies [( 3H]-clonidine and [3H]-prazosin displacement) an alpha2/alpha 1 selectivity ratio of 8526 was obtained for atipamezole, while idazoxan and yohimbine showed ratios of 27 and 40, respectively. Atipamezole had also about a 100 times higher affinity on alpha 2-adrenoceptorsthan the reference compounds [3].in vivo: In vivo studies of [3H]atipamezole demonstrated good penetration into the brain (0.3-1.8% injected dose/g at 5 min, depending upon brain region). In addition, [3H]atipamezole displayed rapid in vivo clearance of nonspecific binding such...Pathways:GPCR/G protein; Target:Adrenergic Receptor Product Data SheetDMSO18W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S AE m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m。
Fluvoxamine maleate_61718-82-9_DataSheet_MedChemExpress
Product Name:Fluvoxamine maleate CAS No.:61718-82-9Cat. No.:HY-B0103AProduct Data SheetMWt:434.41Formula:C19H25F3N2O6Purity :>98%Solubility:DMSO 87 mg/mL; Water <1y Mechanisms:Biological Activity:Fluvoxamine maleate is an antidepressant which functions pharmacologically as a selectivePathways:Neuronal Signaling; Target:SSRIs g ;mg/mL; Ethanol 87 mg/mLFluvoxamine maleate is an antidepressant which functions pharmacologically as a selectiveserotonin reuptake inhibitor.Target: SSRIs Fluvoxamine (maleate) is the maleate salt form of fluvoxamine, which is effective in inhibiting 5-HT uptake by blood platelets and brain synaptosomes. The antagonism by fluvoxamine of the reserpine-induced lowering of the pentamethylenetetrazole convulsive threshold can be regarded as due to an effect upon 5-HT uptake. In contrast to the effects of desmethylimipramine and imipramine, no stimulatory effects are found in rats when rapidly acting reserpine-like compounds are given following a dose of fluvoxamine [1]. fluvoxamine appears to improve combat-related PTSD References:[1]. Claassen, V., et al., Fluvoxamine, a specific 5-hydroxytryptamine uptake inhibitor. Br JPharmacol, 1977. 60(4): p. 505-16.[2]. Escalona, R., et al., Fluvoxamine treatment in veterans with combat-related post-traumatic g []pp psymptoms but not depressive symptoms. The high attrition rate and lack of a placebo group limits the conclusions of our study. Controlled studies of fluvoxamine in the treatmen...stress disorder. Depress Anxiety, 2002. 15(1): p. 29-33.[3]. Ginsburg, B.C., J.W. Pinkston, and R.J. Lamb, The potency of fluvoxamine to reduce ethanol self-administration decreases with concurrent availability of food. Behav Pharmacol, 2012. 23(2): p.134-42.Caution: Not fully tested. For research purposes onlyMedchemexpress LLC18W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S AE m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m。
Voreloxin_175414-77-4_DataSheet_MedChemExpress
Product Name:Voreloxin CAS No.:175414-77-4Product Data SheetCat. No.:HY-10534MWt:401.44Formula:C18H19N5O4S Purity :>98%Solubility:Mechanisms:Biological Activity:Pathways:Cell Cycle/DNA Damage; Target:Topoisomerase DMSOg y Voreloxin is a small molecule and a naphthyridine analogue with antineoplastic activity. Vosaroxin intercalates into DNA in a site-specific manner and blocks the re-ligation process carried out by topoisomerase II during DNA replication. As a result, inhibition of DNA replication, RNA and protein synthesis occurs, followed by cell cycle arrest at G2 phase and induced p53-independent apoptosis.This agent shows a favorable toxicity profile in several aspects: it does not generate reactive oxygen species, as do anthracyclines, reducing the risk of cardiotoxicity; it is not a P-glycoprotein (P-gp)substrate, and thereby evades the common mechanism for multidrug resistance; and it has limited distribution to normal tissues and a more chemically stable molecular structure....References:[1]. Scatena, Caroline D.; Kumer, Jeffrey L.; Arbitrario, Jennifer P. et al. Voreloxin, a first-in-class anticancer quinolone derivative, acts synergistically with cytarabine in vitro and induces bonemarrow aplasia in vivo. Cancer Chemotherapy and Pharmacology (2010), 66(5), 881-888.[2]. Advani, Ranjana H.; Hurwitz, Herbert I.; Gordon, Michael S. et al. Voreloxin, a First-in-Class y[]jAnticancer Quinolone Derivative, in Relapsed/Refractory Solid Tumors: A Report on Two DosingSchedules. Clinical Cancer Research (2010), 16(7), 2167-2175.[3]. J E Lancet, F Ravandi, R M Ricklis et al. A phase Ib study of vosaroxin, an anticancer quinolonederivative, in patients with relapsed or refractory acute leukemia. Leukemia (2011) 25, 1808-1814[4]. Voreloxin [5]. Abbas JA, Stuart RK. Vosaroxin : a novel antineoplastic quinolone. Expert Opin Investig Drugs.2012 Aug;2...Caution: Not fully tested. For research purposes onlyMedchemexpress LLC18 W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S AE m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c om。
Cryptotanshinone-Cryptotanshinon-DataSheet-MedChemExpress
体内研究
Cryptotanshinone reverses the ovarian IR and significantly increases 2-deoxy-D-[1,2-3H]-glucose uptake in all examined tissues from the DEX-treated mice. Cryptotanshinone significantly reduces the ovulation rate and plasma E2 and P levels [2]. Cryptotanshinone administration significantly reduces the body weight and food intake of ob/ob mice (C57BL/6J-Lepob) and diet-induced obese (DIO) mice in a dose-dependent manner. Cryptotanshinone causes noticeably less fat in the adipose tissues, significant reductions of serum triglycerides and cholesterol levels, and 2.5- to 3-fold higher AMPK activity of the skeletal muscles than in the control mice. Oral administration of Cryptotanshinone at 600 mg/kg/day produces dramatic reductions in blood glucose levels of ob/ob mice (C57BL/6J-Lepob), db/db mice (C57BL/KsJ-Leprdb), and ZDF rats, which occur after 3 days and persist over the entirety of the monitoring period [4].
GSK 650394_890842-28-1_DataSheet_MedChemExpress
Product Name:GSK 650394CAS No.:890842-28-1Cat. No.:HY-15192MWt:382.45Formula:C25H22N2O2Purity :>98%Solubility:Mechanisms:Biological Activity:References:Caution: Not fully tested. For research purposes onlyMedchemexpress LLC[1]. Sherk AB, et al. Development of a small-molecule serum- and glucocorticoid-regulated kinase-1antagonist and its evaluation as a prostate cancer therapeutic. Cancer Res. 2008 Sep 15;68(18):7475-83.[2]. Mansley MK, et al. Effects of nominally selective inhibitors of the kinases PI3K, SGK1 and PKB on theinsulin-dependent control of epithelial Na+ absorption. Br J Pharmacol. 2010 Oct;161(3):571-88.[3]. Peng HY, et al. Spinal SGK1/GRASP-1/Rab4 is involved in complete Freund's adjuvant-inducedinflammatory pain via regulating dorsal horn GluR1-containing AMPA receptor trafficking in rats. Pain. 2012Dec;153(12):2380-92.[4]. Peng HY, et al. Spinal serum-inducible and glucocorticoid-inducible kinase 1 mediates neuropathic pain via kalirin and downstream PSD-95-dependent NR2B phosphorylation in rats. J Neurosci. 2013 Mar20;33(12):5227-40....GSK650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assayrespectively.IC50 Value: 62 nM (SGK1); 103 nM (SGK2) [1]Target: SGK in vitro: GSK650394 inhibited the enzymatic activity of SGK1 and SGK2 in the SPA assay with IC50 values of 62 nM and 103 nM, respectively. GSK650394 is relatively non-toxic, with LC50 values of 41 μM in M1 cells (68 times its activity IC50) and a LC50 greater than 100 μM in HeLa cells in XTT assays, which measure mitochondrial enzymatic activity. GSK650394 inhibited SGK1-mediated epithelial transport with an IC50 of 0.6 μM in the SCC assay. The selectivity of GSK650394 for SGK1 over that of Akt and other related kinases proved to be greater than 30-fold, while GSK650394 was more than 60-fold selective for SGK1 over the upstream AGC kinase PDK1 [1]. GSK650394 had no effect on cell survival or growth i...Pathways:Others; Target:SGK Product Data SheetDMSO > 40 mg/ml18 W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S AE m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m。
AG-490_133550-30-8_DataSheet_MedChemExpress
Product Name:AG-490CAS No.:133550-30-8Cat No :HY 12000Product Data SheetCat. No.:HY-12000MWt:294.30Formula:C17H14N2O3Purity :>98%DMSO 57mg/mLWaterSolubility:Mechanisms:Pathways:JAK/STAT; Target:EGFRPathways:JAK/STAT; Target:JAKPathways:Protein Tyrosine Kinase/RTK; Target:EGFR Pathways:Protein Tyrosine Kinase/RTK;Target:JAKDMSO ≥57mg/mL Water <1.2mg/mL Ethanol ≥8mg/mLBiological Activity:AG-490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). Inhibitor of JAK2, JAK3/STAT, JAK3/AP-1 and JAK3/MAPKpathways and potently inhibits cytokine-independent cell growth in vitro and tumor cell invasion in vivo.Pathways:Protein Tyrosine Kinase/RTK; Target:JAK References:[1]. Luan HF, Zhao ZB, Zhao QH, Zhu P, Xiu MY, Ji Y.Hydrogen sulfide postconditioning protects isolated rat hearts against ischemia and reperfusion injury mediated by the JAK2/STAT3 survivalpathway.Braz J Med Biol Res. 2012 Oct;45(10):898-905.[2]Grimm S Ott C H?rlacher M Weber D Hoehn A Grune T Advanced glycation end products [2]. Grimm S, Ott C, H?rlacher M, Weber D, Hoehn A, Grune T.Advanced glycation end products-induced formation of immunoproteasomes: involvement of the receptor for AGEs andJak2/STAT1.Biochem J. 2012 Aug 15.[3]. Ferlazzo A, Carvalho ES, Gregorio SF, Power DM, Canario AV, Trischitta F, Fuentes J.Prolactin regulates luminal bicarbonate secretion in the intestine of the sea bream (Sparus auratus L.).J ExpBiol. 2012 Aug 1.[4]. Chang HH, Huang YM, Wu CP, Tang YC, Liu CW, Huang CH, Ho LT, Wu LY, Kuo YC, Kao YH.Endothelin-1 stimulates suppressor of cytokine signaling-3 gene expression in adipocytes.Gen Comp Endocrinol....Caution: Not fully tested. For research purposes onlyMedchemexpress LLCp18 W i l k i n s o n W a y , P r i n c e t o n , N J 08540,U S AE m a i l : i n f o @m e d c h e m e x p r e s s .c o m W e b : w w w .m e d c h e m e x p r e s s .c o m。
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Structure-ActivityRelationshipStudiesofNovelBenzophenonesLeadingtotheDiscoveryofaPotent,NextGenerationHIVNonnucleosideReverseTranscriptaseInhibitor
KarenR.Romines,†,*GeorgeA.Freeman,†LeeT.Schaller,†JillR.Cowan,†SteveS.Gonzales,†JeffreyH.Tidwell,†ClarenceW.Andrews,III,†DavidK.Stammers,‡RichardJ.Hazen,†RobertG.Ferris,†StevenA.Short,†JosephH.Chan,†andLawrenceR.Boone†
GlaxoSmithKlineInc.,ResearchTrianglePark,NorthCarolina27709,andUniVersityofOxford,Oxford,UKReceiVedJuly14,2005Despitetheprogressofthepasttwodecades,thereisstillconsiderableneedforsafe,efficaciousdrugsthattargethumanimmunodeficiencyvirus(HIV).ThisisparticularlytrueforthegrowingnumberofpatientsinfectedwithvirusresistanttocurrentlyapprovedHIVdrugs.Ourhighthroughputscreeningeffortidentifiedabenzophenonetemplateasapotentialnonnucleosidereversetranscriptaseinhibitor(NNRTI).Thismanuscriptdescribesourextensiveexplorationofthebenzophenonestructure-activityrelationships,whichculminatedintheidentificationofseveralcompoundswithverypotentinhibitionofbothwildtypeandclinicallyrelevantNNRTI-resistantmutantstrainsofHIV.Thesepotentinhibitorsinclude70h(GW678248),whichhasinvitroantiviralassayIC50valuesof0.5nMagainstwild-typeHIV,1nMagainsttheK103Nmutantassociated
withclinicalresistancetoefavirenz,and0.7nMagainsttheY181Cmutantassociatedwithclinicalresistancetonevirapine.Compound70hhasalsodemonstratedrelativelylowclearanceinintravenouspharmacokineticstudiesinthreespecies,anditistheactivecomponentofadrugcandidatewhichhasprogressedtophase2clinicalstudies.
IntroductionTheuseofcombinationtherapy,orhighlyactiveantiretroviraltherapy(HAART),fortreatmentofhumanimmunodeficiencyvirus(HIV)infectionhasdramaticallyimpactedthedisease.Diligentuseofavailableanti-retroviraldrugscancontrolanHIVinfectionforseveralyears,andasaconsequence,thedeathrateofHIVpatientsinthedevelopedworldfelldramaticallyinthemidtolate1990s.Nonnucleosidereversetranscriptaseinhibitors(NNRTI’s),includingnevirapineandefavirenz,areprovingtobeimportantcomponentsofHAART.Inparticular,theuseofefavirenzincombinationwithtwonucleosides(e.g.,lamivudineandzidovudine)isanexcellentfirst-linetherapyforHIVpatients,andithasbeenusedextensivelyinrecentyears.1Aswithallantiretroviraldrugsdevelopedtodate,theuseoftheNNRTI’shasledtotheappearanceofclinicalresistancetothisclassofdrugs.Unfortunately,thegeneticbarrierofallcurrentNNRTI’sisrelativelylow,andasinglemutationcanbegintoreducethesusceptibilityofvirustodrug.Furthermore,crossresistancebetweentheapprovedNNRTI’s(efavirenz,nevirapine,anddelavirdine)isquitecommon,andpatientsaregenerallyforcedtoabandontheapprovedNNRTI’saltogetheroncetheyhavedevelopedresistancetooneofitsmembers.2,3Tomakethesituationevenworse,theappearanceofdrug-resistantvirusisnotlimitedtoNNRTI-experiencedpatients.RecentstudiesindicatethenumberofnewlyinfectedpatientswithNNRTI-resistantvirusisincreasing.4InoneU.S.cohort
whichincludedantiretroviralnaı¨vepatientsfrom44cities,18%haddecreasedphenotypicsensitivitytoatleastoneNNRTI,andone-thirdofthesehaddecreasedphenotypicsensitivitytoallcurrentlyusedNNRTI’s.5EfavirenzandnevirapinearethemostwidelyusedNNRTI’s.Althoughresistancepatternsinthepresenceofthemultidrug
regimensofHIVcarearecomplex,it’sclearthateachoftheseNNRTI’sisassociatedwithasinglepointmutationthattriggersthedevelopmentofclinicalresistance.Forefavirenz,itistheK103Nmutation.Fornevirapine,itistheY181Cmutation.2Consequently,thesemutantviruseshavebeenafocalpointinoursearchforanextgenerationNNRTI.OureffortstodiscoveranNNRTIefficaciousagainstresistantviralstrainsoriginatedinahighthroughputscreeningeffortwhichidentifiedthebenzophenone1(Figure1).6Theinitial
optimizationworkforthistemplatewaspublishedin1995.Thefindingthatresistantvirusesreadilygeneratedinthepresenceoftheleadinganalogue2werecross-resistanttonevaripineledtodecreasedinterestinfurtheroptimizationofthebenzophe-nonesatthattime,andworkinthiscompoundserieswasbrieflystopped.Becauseoftheimportanceofthisdrugclass,however,weturnedourattentiononcemoretothebenzophenonesinthelate1990s,asoneofseveralpotentialtemplatesfortargeting
*Correspondingauthor.Phone:9194834749.Fax:9193152141.E-mail:Karen.r.romines.@gsk.com.†GlaxoSmithKlineInc.
‡UniversityofOxford.
Figure1.InitialbenzophenoneNNRTIleadstructures.
727J.Med.Chem.2006,49,727-73910.1021/jm050670lCCC:$33.50©2006AmericanChemicalSocietyPublishedonWeb12/24/2005