Proteasome inhibition by peptide-semicarbazones.

abstract：:A QSAR methodology that involves multilinear (Hansch-type) and nonlinear (ANN backpropagation) approaches was developed to correlate the antiplatelet activity of 60 benzoxazinone derivatives against factor Xa. The statistical characteristics provided by multilinear model (R2 = 0.821) indicated satisfactory stability a...

journal_title：Bioorganic & medicinal chemistry

authors： Katritzky AR,Pacureanu LM,Slavov S,Dobchev DA,Karelson M

更新日期：2006-11-15 00:00:00

abstract：:Synthesis and antimicrobial activity of squalamine analogue 2 are reported. The synthesis of 2 was accomplished from bisnoralcohol 3. The spermidine moiety was introduced via reductive amination of an appropriately functionalized 3beta-aminosterol with spermidinyl aldehyde 17 utilizing sodium triacetoxyborohydride as ...

journal_title：Bioorganic & medicinal chemistry

authors： Kim HS,Choi BS,Kwon KC,Lee SO,Kwak HJ,Lee CH

更新日期：2000-08-01 00:00:00

abstract：:We herein report the anti-inflammatory activity of some newly synthesized heterocyclic pyridone and pyridine derivatives fused with steroidal structure. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). All compounds, except 3b, 22, and 23, were interestingly less toxic t...

journal_title：Bioorganic & medicinal chemistry

authors： Amr AG,Abdulla MM

更新日期：2006-07-01 00:00:00

abstract：:Two new bisalkaloids, dipiperamides D and E, were isolated as inhibitors of a drug metabolizing enzyme cytochrome P450 (CYP) 3A4 from the white pepper, Piper nigrum. Their structures were elucidated by spectroscopic methods. Dipiperamides D and E showed potent CYP3A4 inhibition with IC(50) values of 0.79 and 0.12 micr...

journal_title：Bioorganic & medicinal chemistry

authors： Tsukamoto S,Tomise K,Miyakawa K,Cha BC,Abe T,Hamada T,Hirota H,Ohta T

更新日期：2002-09-01 00:00:00

abstract：:The synthesis and antitumoral activity of ester and amide derivatives of 2-arylamino-6-trifluoromethyl-3-pyridinecarboxylic acids 8-58 is described. Trifluoromethylpyridine derivatives 8-58 were evaluated for their anticancer activity toward human tumoral cell lines by the National Cancer Institute (NCI). Most of them...

journal_title：Bioorganic & medicinal chemistry

authors： Onnis V,Cocco MT,Lilliu V,Congiu C

更新日期：2008-03-01 00:00:00

abstract：:Vinorine synthase (EC 2.3.1.160) catalyses the acetyl-CoA- or CoA-dependent reversible formation of the alkaloids vinorine (or 11-methoxy-vinorine) and 16-epi-vellosimine (or gardneral). The forward reaction leads to vinorine, which is a direct biosynthetic precursor along the complex pathway to the monoterpenoid indo...

journal_title：Bioorganic & medicinal chemistry

authors： Bayer A,Ma X,Stöckigt J

更新日期：2004-05-15 00:00:00

abstract：:Structural variations of the lead compound FAUC 88 led to dopaminergic enynes with an extended pi-system when Pd-catalyzed cross coupling reactions were employed for the key reaction steps. The dienyne 9b displayed substantial affinity for the dopamine receptor subtype D3 and remarkable selectivity over D4. Compared t...

journal_title：Bioorganic & medicinal chemistry

authors： Lenz C,Boeckler F,Hübner H,Gmeiner P

更新日期：2005-07-15 00:00:00

abstract：:Adenylyl cyclases (ACs) are promising pharmacological targets for treating heart failure, cancer, and psychosis. Ribose-substituted nucleotides have been reported as a potent family of AC inhibitors. In silico analysis of the docked conformers of such nucleotides in AC permits assembly of a consistent, intuitive QSAR ...

journal_title：Bioorganic & medicinal chemistry

authors： Wang JL,Guo JX,Zhang QY,Wu JJ,Seifert R,Lushington GH

更新日期：2007-04-15 00:00:00

abstract：:Fluorinated derivatives of 1,4-naphthoquinones are highly potent inhibitors of Cdc25A and Cdc25B phosphatases and growth of tumor cells. Eight new derivatives of polyfluoro-1,4-naphthoquinone were synthesized and their cytotoxicity in human myeloma, human mammary adenocarcinoma, mouse fibroblasts and primary mouse fib...

journal_title：Bioorganic & medicinal chemistry

authors： Zakharova OD,Ovchinnikova LP,Goryunov LI,Troshkova NM,Shteingarts VD,Nevinsky GA

更新日期：2011-01-01 00:00:00

abstract：:The synthesis of a neoglycopeptide building block is described. The key step is a cycloaddition where the chemistry is orthogonal to standard glycosyl transfer methodology. Also described is some exploratory chemistry of the building block. ...

journal_title：Bioorganic & medicinal chemistry

authors： Bartolozzi A,Li B,Franck RW

更新日期：2003-07-03 00:00:00

abstract：:A library of novel 2,5-disubtituted-1,3,4-oxadiazoles with benzimidazole backbone (3a-3r) was synthesized and evaluated for their potential as β-glucuronidase inhibitors. Several compounds such as 3a-3d, 3e-3j, 3l-3o, 3q and 3r showed excellent inhibitory potentials much better than the standard (IC50=48.4±1.25μM: d-s...

journal_title：Bioorganic & medicinal chemistry

authors： Zawawi NK,Taha M,Ahmat N,Wadood A,Ismail NH,Rahim F,Ali M,Abdullah N,Khan KM

更新日期：2015-07-01 00:00:00

abstract：:Synthesized series of cage dimeric 1,4-dihydropyridines have been systematically evaluated as MDR modulators in in vitro assays to investigate structure-dependent selectivity properties of inhibiting most cancer-relevant efflux pump proteins. Structure-activity relationships of each P-glycoprotein (P-gp) and multidrug...

journal_title：Bioorganic & medicinal chemistry

authors： Coburger C,Wollmann J,Krug M,Baumert C,Seifert M,Molnár J,Lage H,Hilgeroth A

更新日期：2010-07-15 00:00:00

abstract：:A number of 5-aminosubstituted 20(S)-camptothecin analogues were prepared via semi-synthesis starting from 20(S)-camptothecin and 9-methoxy 20(S)-camptothecin. In vitro anti-cancer activity of these analogues was determined using 60 human tumor cell line assay. Although water solubility of most of these compounds was ...

journal_title：Bioorganic & medicinal chemistry

authors： Subrahmanyam D,Sarma VM,Venkateswarlu A,Sastry TV,Kulakarni AP,Rao DS,Reddy KV

更新日期：1999-09-01 00:00:00

abstract：:Semipeptoids derived from the Ras farnesyl transferase inhibitor, CVFM, were synthesized by the Simultaneous Multiple Analogue Peptide Synthesis methodology. The semipeptoids were screened for their in vitro inhibition potency towards farnesyl transferase and geranylgeranyl transferase. Structure-activity relationship...

journal_title：Bioorganic & medicinal chemistry

authors： Reuveni H,Gitler A,Poradosu E,Gilon C,Levitzki A

更新日期：1997-01-01 00:00:00

abstract：:We investigated the carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activity of the clinically used antitumor agent bortezomib, a marketed proteasome inhibitor, against all the catalytically active mammalian isoforms CA I-VII, IX, XII-XV. Bortezomib effectively inhibited all these CAs in the micromolar range. hCA II, t...

journal_title：Bioorganic & medicinal chemistry

authors： Supuran CT

更新日期：2017-10-01 00:00:00

abstract：:Three new prenylflavonoids, namely corylifols A-C (1-3), together with 13 known ones, were isolated from the seeds of Psoralea corylifolia. Their structures were elucidated by spectral methods including 1D and 2D NMR techniques. All the isolates were tested on antibacterial assays, and nine of them showed significant ...

journal_title：Bioorganic & medicinal chemistry

authors： Yin S,Fan CQ,Wang Y,Dong L,Yue JM

更新日期：2004-08-15 00:00:00

abstract：:To clarify the structure-activity relationships of flavonoids for nitric oxide (NO) production inhibitory activity, we examined the inhibitory effects of 73 flavonoids on NO production in lipopolysaccharide-activated mouse peritoneal macrophages. Among those flavonoids, apigenin (IC(50)=7.7 microM), diosmetin (8.9 mic...

journal_title：Bioorganic & medicinal chemistry

authors： Matsuda H,Morikawa T,Ando S,Toguchida I,Yoshikawa M

更新日期：2003-05-01 00:00:00

abstract：:A series of structurally related citric acid-ciprofloxacin conjugates was synthesised to investigate the influence of the linker between citric acid and ciprofloxacin on antibacterial activities. Minimum inhibitory concentrations (MICs) were determined against a panel of reference strains and clinical isolates of bact...

journal_title：Bioorganic & medicinal chemistry

authors： Milner SJ,Snelling AM,Kerr KG,Abd-El-Aziz A,Thomas GH,Hubbard RE,Routledge A,Duhme-Klair AK

更新日期：2014-08-15 00:00:00

abstract：:Compounds that bind at the colchicine site of tubulin have drawn considerable attention with studies indicating that these agents suppress microtubule dynamics and inhibit tubulin polymerization. Data for 18 polysubstituted pyrrole compounds are reported, including antiproliferative activity against human MDA-MB-435 c...

journal_title：Bioorganic & medicinal chemistry

authors： Tripathi A,Fornabaio M,Kellogg GE,Gupton JT,Gewirtz DA,Yeudall WA,Vega NE,Mooberry SL

更新日期：2008-03-01 00:00:00

abstract：:In earlier investigations we have described the synthesis and biological evaluation of a panel of novel glycosylated heteroaromatics (1-12). It was found that these compounds can bind to DNA in vitro and are cytotoxic against several cancer cell lines at low micromolar concentration. We report here structure-activity ...

journal_title：Bioorganic & medicinal chemistry

authors： Shi W,Lowary TL

更新日期：2011-03-01 00:00:00

abstract：:Three carboranyltetraphenylporphyrins containing 40 or 80 boron atoms were synthesized and evaluated for their biodistribution and toxicity in EMT-6 tumor-bearing mice. Copper (II) meso-5,10,15,20-tetrakis[3-methoxy-4-(o-carboranylmethoxy)phenyl]porphyrin, 6, and copper (II) meso-5,10,15,20-tetrakis[3-hydroxy-4-(o-car...

journal_title：Bioorganic & medicinal chemistry

authors： Wu H,Micca PL,Makar MS,Miura M

更新日期：2006-08-01 00:00:00

abstract：:Two series of combretastatin A4 derivatives (acrylamide=carboxamide and carbamate) were synthesized in order to improve the water solubility and stabilize the cis-configuration of the double bond. Their cytotoxic effects were evaluated against MCF-7, KB-3-1 and IGROV human cancer cell lines, as well as their inhibitor...

journal_title：Bioorganic & medicinal chemistry

authors： Borrel C,Thoret S,Cachet X,Guénard D,Tillequin F,Koch M,Michel S

更新日期：2005-06-01 00:00:00

abstract：:Thionation of estrogen-like active cyclic peptides, segetalins A (1) and B (2), with Lawesson's reagent provided each two thiosegetalins; thiosegetalin A1 [Gly-1-psi(CS-NH)-Val-2; Trp-5-psi (CS-NH)-Ala-6]segetalin A, thiosegetalin A2 [Gly-1-psi(CS-NH)-Val-2; Ala-6-psi(CS-NH)-Gly-1]segetalin A, thiosegetalin B1 [Gly-1-...

journal_title：Bioorganic & medicinal chemistry

authors： Morita H,Yun YS,Takeya K,Itokawa H,Shirota O

更新日期：1997-03-01 00:00:00

abstract：:Described here are the syntheses and preliminary biological evaluations of the first two enzymatically activated prodrugs of docetaxel (Taxotere) reported to date. These prodrugs were designed as potential candidates for selective chemotherapy in ADEPT or PMT. They are constituted of a glucuronic acid moiety, a double...

journal_title：Bioorganic & medicinal chemistry

authors： Bouvier E,Thirot S,Schmidt F,Monneret C

更新日期：2004-03-01 00:00:00

abstract：:Antisense oligonucleotides (AS-ODNs) specifically hybridize with target mRNAs, resulting in interference with the splicing mechanism or the regulation of protein translation. In our previous reports, we demonstrated that β-glucan schizophyllan (SPG) can form a complex with AS-ODNs attached with oligo deoxyadenosine dA...

journal_title：Bioorganic & medicinal chemistry

authors： Sasaki S,Izumi H,Morimoto Y,Sakurai K,Mochizuki S

更新日期：2020-09-15 00:00:00

abstract：:Cytochrome P450 2C9 (2C9) is one of the three major drug metabolizing cytochrome P450 enzymes in human liver. Although the crystal structure of 2C9 has been solved, the important physicochemical properties of substrate-enzyme interactions remain difficult to be determined. This is due in part to the conformational fle...

journal_title：Bioorganic & medicinal chemistry

authors： Peng CC,Rushmore T,Crouch GJ,Jones JP

更新日期：2008-04-01 00:00:00

abstract：:We designed and synthesized new pyrazole thiourea chimeric derivatives and confirmed their structures by NMR and IR spectra. Apoptotic effects were studied in human cancer cells. The N-[(1-methyl-1H-pyrazol-4-yl)carbonyl]-N'-(3-bromophenyl)-thiourea compound (4b) exhibited the highest apoptosis-inducing effect. Compou...

journal_title：Bioorganic & medicinal chemistry

authors： Nitulescu GM,Draghici C,Olaru OT,Matei L,Ioana A,Dragu LD,Bleotu C

更新日期：2015-09-01 00:00:00

abstract：:Green photosynthetic bacteria have unique light-harvesting antenna systems called chlorosomes. Chlorobaculum tepidum, a model organism of the bacteria, biosynthesized monogalactosyl- and rhamnosylgalactosyldiacylglycerides possessing a methylene-bridged palmitoleyl group characterized by a cis-substituted cyclopropane...

journal_title：Bioorganic & medicinal chemistry

authors： Mizoguchi T,Tsukatani Y,Harada J,Takasaki S,Yoshitomi T,Tamiaki H

更新日期：2013-07-01 00:00:00

abstract：:A new series of 4-anilinoquinazolines with C-6 ureido and thioureido side chains and various substituents at the C-4 anilino moiety was designed, synthesized and evaluated as wild type (WT) and mutant EGFR inhibitors. Most of the compounds inhibited EGFR kinase wild type (EGFR WT) with IC50 values in the low nanomolar...

journal_title：Bioorganic & medicinal chemistry

authors： Mowafy S,Galanis A,Doctor ZM,Paranal RM,Lasheen DS,Farag NA,Jänne PA,Abouzid KA

更新日期：2016-08-15 00:00:00

abstract：:AIE molecule silole 1 could be used to detect G-quadruplex formation using an exonuclease I hydrolysis assay. This visual observation of G-quadruplexes has been successfully used in investigating multiple G-quadruplexes, including the one-stranded telomeric, c-myc, c-kit, VEGF G-quadruplexes, and a d(G(4)T(4)G(4)) int...

journal_title：Bioorganic & medicinal chemistry

authors： Huang J,Wang M,Zhou Y,Weng X,Shuai L,Zhou X,Zhang D

更新日期：2009-11-15 00:00:00