Synthesis and in vitro cytotoxicity of haloderivatives of noscapine.

abstract：:A series of 2-(3-aryl-2-propenoyl)-3-methylquinoxaline-1,4-dioxides 3a-l were prepared by condensation of various aryl aldehydes with 2-acetyl-3-methylquinoxaline-1,4-dioxide 2. These compounds inhibit the growth of human Molt 4/C8 and CEM T-lymphocytes and the IC(50) values are mainly in the 5-30 microM range. The qu...

journal_title：Bioorganic & medicinal chemistry

authors： Das U,Pati HN,Panda AK,De Clercq E,Balzarini J,Molnár J,Baráth Z,Ocsovszki I,Kawase M,Zhou L,Sakagami H,Dimmock JR

更新日期：2009-06-01 00:00:00

abstract：:In a course of our search for anticancer agent based on a novel anti-austerity strategy, we found that the CHCl3 extract of the roots of Securidaca longepedunculata (Polygalaceae), collected at Democratic Republic of Congo, killed PANC-1 human pancreatic cancer cells preferentially in nutrient-deprived medium (NDM). P...

journal_title：Bioorganic & medicinal chemistry

authors： Dibwe DF,Awale S,Kadota S,Morita H,Tezuka Y

更新日期：2013-12-15 00:00:00

abstract：:An efficient technique is presented which integrates cofactor dependent enzymic phosphorylation and dehydrogenation into a single, closed-loop system by employing phosphoenolpyruvate as the sacrificial reagent for sequential ATP and NAD+ recycling steps. Exemplary applications are developed for the synthesis of 6-phos...

journal_title：Bioorganic & medicinal chemistry

authors： Fessner WD,Sinerius G

更新日期：1994-07-01 00:00:00

abstract：:The purpose of this study is to probe the suitability of DFT based chemical reactivity parameter, electrophilicity index as a possible biological activity descriptor in the development of QSAR. Testosterone derivatives with activity described in terms of various biological activity parameters and the estrogen derivati...

journal_title：Bioorganic & medicinal chemistry

authors： Parthasarathi R,Subramanian V,Roy DR,Chattaraj PK

更新日期：2004-11-01 00:00:00

abstract：:A number of N-phenyl-N'-(2-chloroethyl)ureas (CEUs) have been shown to be potent antimitotics through their covalent binding to the colchicine-binding site on intracellular beta-tubulin. The present communication aimed to evaluate the role of the electrophilic 2-chloroethyl amino moiety of CEU on cell growth inhibitio...

journal_title：Bioorganic & medicinal chemistry

authors： Fortin JS,Lacroix J,Desjardins M,Patenaude A,Petitclerc E,C-Gaudreault R

更新日期：2007-07-01 00:00:00

abstract：:A group of regioisomeric (E)-1,3-diarylprop-2-en-1-one derivatives possessing a COX-2 SO2Me pharmacophore at the para position of the C-1 or C-3 phenyl ring, in conjunction with a C-3 or C-1 phenyl (4-H) or substituted-phenyl ring (4-F, 4-OMe and 4-Me), were designed for evaluation as selective cyclooxygenase-2 (COX-2...

journal_title：Bioorganic & medicinal chemistry

authors： Zarghi A,Arfaee S,Rao PN,Knaus EE

更新日期：2006-04-15 00:00:00

abstract：:KPU-105 (4), a potent anti-microtubule agent that contains a benzophenone was derived from the diketopiperazine-type vascular disrupting agent (VDA) plinabulin 3, which displays colchicine-like tubulin depolymerization activity. To develop derivatives with more potent anti-microtubule and cytotoxic activities, we furt...

journal_title：Bioorganic & medicinal chemistry

authors： Yamazaki Y,Sumikura M,Masuda Y,Hayashi Y,Yasui H,Kiso Y,Chinen T,Usui T,Yakushiji F,Potts B,Neuteboom S,Palladino M,Lloyd GK,Hayashi Y

更新日期：2012-07-15 00:00:00

abstract：:A series of benzyloxybenzaldehyde derivatives were prepared and tested against the HL-60 cell line for anticancer activity. Preliminary structure-activity relationships were established. It was discovered that 2-(benzyloxy)benzaldehyde (17), 2-(benzyloxy)-4-methoxybenzaldehyde (26), 2-(benzyloxy)-5-methoxybenzaldehyde...

journal_title：Bioorganic & medicinal chemistry

authors： Lin CF,Yang JS,Chang CY,Kuo SC,Lee MR,Huang LJ

更新日期：2005-03-01 00:00:00

abstract：:The discovery of 3-methoxy-9-(30,40,50-trimethoxyphenyl)-6,7-dihydro-5H-benzo[7]annulen-4-ol (a benzosuberene-based analogue referred to as KGP18) was originally inspired by the natural products colchicine and combretastatin A-4 (CA4). The relative structural simplicity and ease of synthesis of KGP18, coupled with its...

journal_title：Bioorganic & medicinal chemistry

authors： Herdman CA,Devkota L,Lin CM,Niu H,Strecker TE,Lopez R,Liu L,George CS,Tanpure RP,Hamel E,Chaplin DJ,Mason RP,Trawick ML,Pinney KG

更新日期：2015-12-15 00:00:00

abstract：:A series of trans-2-aryl-cyclopropylamine derived compounds were synthesized and evaluated their biological activities against DPP-IV. The structure-activity relationships (SAR) led to the discovery of novel series of DPP-IV inhibitors, having IC(50) values of <100 nM with excellent selectivity over the closely relate...

journal_title：Bioorganic & medicinal chemistry

authors： Tsai TY,Hsu T,Chen CT,Cheng JH,Yeh TK,Chen X,Huang CY,Chang CN,Yeh KC,Hsieh SH,Chien CH,Chang YW,Huang CH,Huang YW,Huang CL,Wu SH,Wang MH,Lu CT,Chao YS,Jiaang WT

更新日期：2009-03-15 00:00:00

abstract：:Bioactive compounds present in grapefruit juice are known to increase the bioavailability of certain medications by acting as potent CYP 3A4 inhibitors. An efficient technique has been developed for isolation and purification of three furocoumarins. The isolated compounds have been tested for the inhibition of human C...

journal_title：Bioorganic & medicinal chemistry

authors： Girennavar B,Poulose SM,Jayaprakasha GK,Bhat NG,Patil BS

更新日期：2006-04-15 00:00:00

abstract：:A group of (E)-3-(4-methanesulfonylphenyl)acrylic acids possessing a substituted-phenyl ring (4-H, 4-Br, 3-Br, 4-F, 4-OH, 4-OMe, 4-OAc, and 4-NHAc) attached to the acrylic acid C-2 position were prepared using a stereospecific Perkin condensation reaction. A related group of compounds having 4- and 3-(4-isopropyloxyph...

journal_title：Bioorganic & medicinal chemistry

authors： Moreau A,Chen QH,Praveen Rao PN,Knaus EE

更新日期：2006-12-01 00:00:00

abstract：:Indole beta-cyclodextrin (beta-1) was found to be able to prevent aggregation of citrate synthase (CS) on heating condition. As a result, beta-1 showed anti-CS aggregation in this system by regulating in early stage. The depression mechanism of beta-1 for aggregation of CS is as follows: the beta-1 formed a complex wi...

journal_title：Bioorganic & medicinal chemistry

authors： Toda M,Itoh H,Kondo Y,Hamada F

更新日期：2007-03-01 00:00:00

abstract：:Stereoselective reductive metabolism of various p-substituted acetophenone derivatives was studied using isolated rat liver 3alpha-hydroxysteroid dehydrogenase (3alpha-HSD). Kinetic experiments were performed and analyzed by measuring the products by HPLC using a chiral column. The results demonstrated that the presen...

journal_title：Bioorganic & medicinal chemistry

authors： Uwai K,Konno N,Yasuta Y,Takeshita M

更新日期：2008-02-01 00:00:00

abstract：:The benzamidine moiety, a well-known arginine mimetic, has been introduced in a variety of ligands, including peptidomimetic inhibitors of trypsin-like serine proteases. According to their primary substrate specificity, the benzamidine residue interacts with the negatively charged aspartate at the bottom of the S1 poc...

journal_title：Bioorganic & medicinal chemistry

authors： Dosa S,Stirnberg M,Lülsdorff V,Häußler D,Maurer E,Gütschow M

更新日期：2012-11-01 00:00:00

abstract：:New 7-aryl or 7-heteroarylamino-2,3-dimethylbenzo[b]thiophenes were prepared by palladium-catalyzed Buchwald-Hartwig cross-coupling of 7-bromo or 7-amino-2,3-dimethylbenzo[b]thiophenes, previously prepared by us, with substituted (4-methoxy or 3,4-dimethoxy) anilines and 3-aminopyridine or with substituted (3-methoxy ...

journal_title：Bioorganic & medicinal chemistry

authors： Queiroz MJ,Ferreira IC,Calhelha RC,Estevinho LM

更新日期：2007-02-15 00:00:00

abstract：:An unusual class of diterpenoid natural products, 'cycloterpenals' (with a central cyclohexadienal core), that arise in nature by condensation of retinoids and other isoprenes, have been isolated from a variety of organisms including marine sponges as well as from the human eye. A milk whey protein has also demonstrat...

journal_title：Bioorganic & medicinal chemistry

authors： Bench BJ,Tichy SE,Perez LM,Benson J,Watanabe CM

更新日期：2008-08-15 00:00:00

abstract：:Synthetic modification of cyclosporin A at P3-P4 positions led to the discovery of NIM258, a next generation cyclophilin inhibitor with excellent anti-hepatitis C virus potency, with decreased transporter inhibition, and pharmacokinetics suitable for coadministration with other drugs. Herein is disclosed the evolution...

journal_title：Bioorganic & medicinal chemistry

authors： Fu J,Becker C,Cao L,Capparelli M,Denay R,Fujimoto R,Gai Y,Gao Z,Guenat C,Karur S,Kim H,Li W,Li X,Li W,Lochmann T,Lu A,Lu P,Luneau A,Meier N,Mergo W,Ng S,Parker D,Peng Y,Riss B,Rivkin A,Roggo S,Schroede

更新日期：2018-02-15 00:00:00

abstract：:This article deals with the synthesis and the activities of some 1,5-dialkyl-3-arylureido-1,5-benzodiazepin-2,4-diones which were prepared as potential CCK2 antagonists, with the intention to find a possible follow up of our lead compound GV150013, showing an improved pharmacokinetic profile. The phenyl ring at N-5 wa...

journal_title：Bioorganic & medicinal chemistry

authors： Roberts K,Ursini A,Barnaby R,Cassarà PG,Corsi M,Curotto G,Donati D,Feriani A,Finizia G,Marchioro C,Niccolai D,Oliosi B,Polinelli S,Ratti E,Reggiani A,Tedesco G,Tranquillini ME,Trist DG,van Amsterdam FT

更新日期：2011-07-15 00:00:00

abstract：:NAD(P)H:quinone reductase 1 (QR1) belongs to a class of enzymes called cytoprotective enzymes. It exhibits its cancer protective activity mainly by inhibiting the formation of intracellular semiquinone radicals, and by generating α-tocopherolhydroquinone, which acts as a free radical scavenger. It is therefore believe...

journal_title：Bioorganic & medicinal chemistry

authors： Mayhoub AS,Marler L,Kondratyuk TP,Park EJ,Pezzuto JM,Cushman M

更新日期：2012-12-15 00:00:00

abstract：:BMS-986120 is a PAR4 antagonist that is being investigated as an antiplatelet agent in phase I clinical trial. An improved synthesis of BMS-986120 has been developed. Based on the novel synthetic approach to BMS-986120, a series of deuterated derivatives of BMS-986120 have been synthesized and biologically evaluated t...

journal_title：Bioorganic & medicinal chemistry

authors： Chen P,Ren S,Song H,Chen C,Chen F,Xu Q,Kong Y,Sun H

更新日期：2019-01-01 00:00:00

abstract：:The substitution of the sterically hindered carbon of the potent thyroid hormone agonist, GC-1, was effected by a reaction based on the solvolysis of the benzylic hydroxyl group. The reaction was found to proceed in high yield with a variety of nucleophiles including alcohols, thiols, allyl silanes and electron-rich a...

journal_title：Bioorganic & medicinal chemistry

authors： Yoshihara HA,Chiellini G,Mitchison TJ,Scanlan TS

更新日期：1998-08-01 00:00:00

abstract：:Thymidylate synthase (TS) (EC 2.1.1.45), an enzyme involved in the DNA synthesis of both prokaryotic and eukaryotic cells, is a potential target for the development of anticancer and antinfective agents. Recently, we described a series of phthalein and naphthalein derivatives as TS inhibitors. These compounds have str...

journal_title：Bioorganic & medicinal chemistry

authors： Ghelli S,Rinaldi M,Barlocco D,Gelain A,Pecorari P,Tondi D,Rastelli G,Costi MP

更新日期：2003-03-20 00:00:00

abstract：:Erypoegin K, an isoflavone isolated from the stem bark of Erythrina poeppigiana, has potent apoptosis-inducing effect on human leukemia HL-60 cells. Erypoegin K has a chiral carbon at the C-2'' position of its furan ring and naturally occurs as a racemic mixture of (S)- and (R)-isomers. In the present study, we semi-s...

journal_title：Bioorganic & medicinal chemistry

authors： Hikita K,Saigusa S,Takeuchi Y,Matsuyama H,Nagai R,Kato K,Murata T,Tanaka H,Wagh YS,Asao N,Kaneda N

更新日期：2020-06-01 00:00:00

abstract：:Aryl diketoacids (ADK) and their bioisosteres are among the most promising HIV-1 integrase (IN) inhibitors. Previously, we designed a series of ADK dimers as a new class of IN inhibitors that were hypothesized to target two divalent metal ions on the active site of IN. Herein we present a further structure-activity re...

journal_title：Bioorganic & medicinal chemistry

authors： Zeng LF,Jiang XH,Sanchez T,Zhang HS,Dayam R,Neamati N,Long YQ

更新日期：2008-08-15 00:00:00

abstract：:Semiempirical quantum mechanical and molecular mechanics calculations were carried out to identify and characterize the steric and electronic properties that modulate ligand recognition and activation of the cerebellar GABAA/benzodiazepine (BDZ) receptor. For this hypothesis development, thirteen compounds belonging t...

journal_title：Bioorganic & medicinal chemistry

authors： Schove LT,Perez JJ,Loew GH

更新日期：1994-10-01 00:00:00

abstract：:In order to improve the immunotherapeutical potential of H-Cys-Leu-Gly-Gly-Leu-Leu-Thr-Met-Val-OH (CLG) peptide, an Epstein-Barr virus (EBV) subdominant epitope derived from the membrane protein LMP2, we have synthesized and tested CLG analogues containing cis- and/or trans-4-aminocyclohexanecarboxylic acid (ACCA) rep...

journal_title：Bioorganic & medicinal chemistry

authors： Marastoni M,Bazzaro M,Micheletti F,Gavioli R,Tomatis R

更新日期：2002-09-01 00:00:00

abstract：:We have previously reported small-molecule inhibitors of Gli1-mediated transcription, an essential down-stream element of the Hh pathway. We created new derivatives of the previous compounds aiming to improve the druggable properties. The new compounds, amide conjugates of ketoprofen and indole, showed inhibitory acti...

journal_title：Bioorganic & medicinal chemistry

authors： Mahindroo N,Connelly MC,Punchihewa C,Yang L,Yan B,Fujii N

更新日期：2010-07-01 00:00:00

abstract：:We previously reported a series of 8-methyl-2-aryl-5-alkylaminoquinolines as a novel class of corticotropin-releasing factor-1 (CRF(1)) receptor antagonists. A critical issue encountered for this series of compounds was low aqueous solubility at physiological pH (pH 7.4). To address this issue, derivatization at key s...

journal_title：Bioorganic & medicinal chemistry

authors： Takeda K,Terauchi T,Hashizume M,Shikata K,Taguchi R,Murata-Tai K,Fujisawa M,Takahashi Y,Shin K,Ino M,Shibata H,Yonaga M

更新日期：2012-11-15 00:00:00

abstract：:The synthesis of novel melatonin analogues 3a and 4a-c designed as melatonin receptor ligands is described. Among the newly synthesized ligands, 2-((S)-2-hydroxymethylindolin-1-ylmethyl)-melatonin 4b displayed the highest affinity for MT(1) receptors (K(i)=9.8 nM) and for MT(2) subtype (K(i)=7.8 nM), whereas the rigid...

journal_title：Bioorganic & medicinal chemistry

authors： Attia MI,Witt-Enderby PA,Julius J

更新日期：2008-08-15 00:00:00