Semi-synthesis of C28-modified triterpene acid derivatives from maslinic acid or corosolic acid as potential α-glucosidase inhibitors.

abstract：:Eight new glycosides, morindaparvins P-W, were isolated from the butanol extract of the aerial parts of Morinda parvifolia. These new structures were elucidated by comprehensive spectroscopic analysis and by comparing the experimental and calculated electronic circular dichroism spectra. The butanol extract was observ...

journal_title：Bioorganic chemistry

authors： Su X,Li L,Sun H,Zhang F,Li C,Li F,Wang H,Li B,Chen R,Kang J

更新日期：2019-06-01 00:00:00

abstract：:Novel benzothiazole-based compounds were designed and synthesized as potential antimicrobial agents with dual DNA gyrase/topoisomerase IV inhibitory activity. The structures of the newly synthesized compounds were established on the basis of spectral (IR, NMR, MS) and elemental analyses. Most of the studied compounds ...

journal_title：Bioorganic chemistry

authors： Ismail MMF,Abdulwahab HG,Nossier ES,El Menofy NG,Abdelkhalek BA

更新日期：2020-01-01 00:00:00

abstract：:11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) is an enzyme that catalyzes the conversion of inactive cortisone into physiologically active cortisol. Inhibiting the activity of this enzyme plays a key role in the treatment of Cushing's syndrome, metabolic syndrome and type 2 diabetes. Therefore, new compounds that...

journal_title：Bioorganic chemistry

authors： Studzińska R,Kołodziejska R,Kupczyk D,Płaziński W,Kosmalski T

更新日期：2018-09-01 00:00:00

abstract：:The severe acute respiratory syndrome (SARS) virus depends on a chymotrypsin-like cysteine proteinase (3CL(pro)) to process the translated polyproteins to functional viral proteins. This enzyme is a target for the design of potential anti-SARS drugs. A series of ketones and corresponding mono- and di-fluoro ketones ha...

journal_title：Bioorganic chemistry

authors： Zhang J,Huitema C,Niu C,Yin J,James MN,Eltis LD,Vederas JC

更新日期：2008-10-01 00:00:00

abstract：:Two new series of ethyl benzoate bearing pyrrolizine and indolizine moieties 8-11 were synthesized and evaluated for their anti-inflammatory and anticancer activities. Among these derivatives, compounds 9a, 10b and 11b displayed in vivo anti-inflammatory and analgesic activity comparable to ibuprofen. The acute ulcero...

journal_title：Bioorganic chemistry

authors： Attalah KM,Abdalla AN,Aslam A,Ahmed M,Abourehab MAS,ElSawy NA,Gouda AM

更新日期：2020-01-01 00:00:00

abstract：:A novel series of resveratrol-cinnamoyl hybrids as tubulin polymerization inhibitors were designed and synthesized, and evaluated for their anti-proliferative activities against A549, MCF-7, HepG2, HeLa and MDA-MB-231 five cancer cell lines. Most designed compounds showed better anti-proliferative activities. Particul...

journal_title：Bioorganic chemistry

authors： Yin Y,Lian BP,Xia YZ,Shao YY,Kong LY

更新日期：2019-12-01 00:00:00

abstract：:This study deals with design and synthesis of novel benzofuran-pyrazole hybrids as anticancer agents. Eight compounds were chosen by National Cancer Institute (NCI), USA to evaluate their in vitro antiproliferative activity at 10(-5)M in full NCI 60 cell panel. The preliminary screening of the tested compounds showed ...

journal_title：Bioorganic chemistry

authors： Abd El-Karim SS,Anwar MM,Mohamed NA,Nasr T,Elseginy SA

更新日期：2015-12-01 00:00:00

abstract：:The galactofuranose moiety found in many surface constituents of microorganisms is derived from UDP-D-galactopyranose (UDP-Galp) via a unique ring contraction reaction catalyzed by a FAD-dependent UDP-Galp mutase. When the enzyme is reduced by sodium dithionite, its catalytic efficiency increases significantly. Since ...

journal_title：Bioorganic chemistry

authors： Huang Z,Zhang Q,Liu HW

更新日期：2003-12-01 00:00:00

abstract：:The stilbenoid resveratrol (1) was subjected to regioselective acetylation catalysed by Candida antarctica lipase (CAL) to obtain 4'-acetylresveratrol (2). CAL biocatalysed regioselective alcoholysis of 3,5,4'-triacetylresveratrol (3), 3,5,4'-tributanoylresveratrol (6), and 3, 4, 5'-trioctanoylresveratrol (9) afforded...

journal_title：Bioorganic chemistry

authors： Cardile V,Lombardo L,Spatafora C,Tringali C

更新日期：2005-02-01 00:00:00

abstract：:Porcelia macrocarpa (Warm.) R. E. Fries (Annonaceae) is an endemic plant in Brazil where its tasty pulp has been eaten fresh. The hexane extract from its flowers was subjected to chromatographic procedures to afford four acetylene derivatives identified as octadec-9-ynoic (stearolic acid - 1), (11E)-octadec-11-en-9-yn...

journal_title：Bioorganic chemistry

authors： Londero VS,da Costa-Silva TA,Gomes KS,Ferreira DD,Mesquita JT,Tempone AG,Young MCM,Jerz G,Lago JHG

更新日期：2018-08-01 00:00:00

abstract：:Succinimides are well recognized heterocyclic compounds in drug discovery which produce diverse therapeutically related applications in pharmacological practices. Researches in medicinal chemistry field have isolated and synthesized succinimide derivatives with multiple medicinal properties including anticonvulsant, a...

journal_title：Bioorganic chemistry

authors： Zhao Z,Yue J,Ji X,Nian M,Kang K,Qiao H,Zheng X

更新日期：2020-12-15 00:00:00

abstract：:Levels of cAMP that control critical platelet functions are regulated by cGMP-inhibited cAMP phosphodiesterase (PDE3A). We previously showed that millimolar concentrations of the hydrolyzable 8-[(4-bromo-2,3-dioxobutyl)thioadenosine 3',5'-cyclic monophosphate (8-BDB-TcAMP) inactivate PDE3A. We have now synthesized a n...

journal_title：Bioorganic chemistry

authors： Hung SH,Madhusoodanan KS,Beres JA,Boyd RL,Baldwin JL,Zhang W,Colman RW,Colman RF

更新日期：2002-02-01 00:00:00

abstract：:A phytochemical study to obtain new nitric oxide (NO) inhibitors resulted in the isolation of five new withanolides from the whole plants of Physalis peruviana. The structures were determined on the basis of extensive NMR spectroscopic data analysis as well as the time-dependent density functional theory (TDDFT) elect...

journal_title：Bioorganic chemistry

authors： Dong B,An L,Yang X,Zhang X,Zhang J,Tuerhong M,Jin DQ,Ohizumi Y,Lee D,Xu J,Guo Y

更新日期：2019-06-01 00:00:00

abstract：:Inhibition of carbonic anhydrases (CAs, EC 4.2.1.1) has clinical importance for the treatment of several diseases. They participate in crucial regulatory mechanisms for balancing intracellular and extracellular pH of the cells. Among CA isoforms, selective inhibition of hCA IX has been linked to decreasing of cell gro...

journal_title：Bioorganic chemistry

authors： Yamali C,Gul HI,Ece A,Bua S,Angeli A,Sakagami H,Sahin E,Supuran CT

更新日期：2019-11-01 00:00:00

abstract：:Tumor immunotherapy based on specific tumor antigen has become the focus for breast cancer, and research into cancer/testes antigens (CTA) is progressing. As an important member in the CTA, NY-ESO-1 plays a crucial role in the treatment and prognosis of breast cancer. In this study, we aimed to improve the binding abi...

journal_title：Bioorganic chemistry

authors： Shi W,Tong Z,Qiu Q,Yue N,Guo W,Zou F,Zhou D,Li J,Huang W,Qian H

更新日期：2020-10-01 00:00:00

abstract：:Diabetes mellitus is a chronic metabolic disorder which is rapidly spreading worldwide. It is characterized by persistent elevated blood glucose level above normal values (hyperglycemia) due to defect in either insulin secretion or in insulin action or both of them. Currently approved oral synthetic antidiabetic drugs...

journal_title：Bioorganic chemistry

authors： Abbas G,Al Harrasi A,Hussain H,Hamaed A,Supuran CT

更新日期：2019-05-01 00:00:00

abstract：:Optimization of IG-105 (1) on the carbazole ring provided five series of new carbazole sulfonamides derivatives, 7a-e, 8a-g, 9a-g, 10a-e, and 11a-g. All of the compounds were evaluated against HepG2, MCF-7, MIA PaCa-2, and Bel-7402 cells for antiproliferative activity. Each series of compounds was 2-5 times more activ...

journal_title：Bioorganic chemistry

authors： Sun L,Wang C,Hu X,Wu Y,Jiang Z,Li Z,Chen X,Hu L

更新日期：2020-06-01 00:00:00

abstract：:An E461G mutation of beta-galactosidase results in the disappearance of the high pL (L = H, D) downward break in the rate profiles for k(cat)/K(m) for wild-type enzyme-catalyzed hydrolysis of 4-nitrophenyl beta-D-galactopyranoside (Gal-OPNP) and a decrease from (k(cat))(HOH)/(k(cat))(DOD) = 1.7 to (k(cat))(HOH)/(k(cat...

journal_title：Bioorganic chemistry

authors： Richard JP,Huber RE,McCall DA

更新日期：2001-06-01 00:00:00

abstract：:In this study, we prepared a novel amino cellulose derivative (benzyl cellulose-g-poly [2-(N,N-Dimethylamino)ethyl methacrylate]) via a homogeneous ATRP method. The successful synthesis of the novel amino cellulose was confirmed by FT-IR and 1H NMR. This study addressed the different characteristics of the prepared po...

journal_title：Bioorganic chemistry

authors： Shokri M,Moradi S,Amini S,Shahlaei M,Seidi F,Saedi S

更新日期：2021-01-01 00:00:00

abstract：:The isomerization of l-amino acids in peptides and proteins into d-configuration under physiological conditions would affect the physiological dysfunction and caused protein conformational diseases. The presence of d-amino acids might change the higher-order structure of proteins and triggered abnormal aggregation. In...

journal_title：Bioorganic chemistry

authors： Yan L,Ke Y,Kan Y,Lin D,Yang J,He Y,Wu L

更新日期：2020-12-01 00:00:00

abstract：:We synthesized a new series of 2-[(3-(4-sulfamoylphenethyl)-4(3H)-quinazolinon-2-yl)thio]anilide derivatives (2-16) and evaluated their cytotoxic activity against breast adenocarcinoma (MCF-7), colorectal adenocarcinoma (HT-29), and acute myeloid leukemia (HL-60 and K562) cells. To reveal their selectivity toward canc...

journal_title：Bioorganic chemistry

authors： Alkahtani HM,Abdalla AN,Obaidullah AJ,Alanazi MM,Almehizia AA,Alanazi MG,Ahmed AY,Alwassil OI,Darwish HW,Abdel-Aziz AA,El-Azab AS

更新日期：2020-01-01 00:00:00

abstract：:Autophagy is an intracellular degradation/recycling pathway that provides nutrients and building blocks to cellular metabolism and keeps the cytoplasm clear of obsolete proteins and organelles. During recent years, dysregulated autophagy activity has been reported to be a characteristic of many different disease types...

journal_title：Bioorganic chemistry

authors： Tanc M,Cleenewerck M,Kurdi A,Roelandt R,Declercq W,De Meyer G,Augustyns K,Martinet W,Van der Veken P

更新日期：2019-06-01 00:00:00

abstract：:The dimeric Mycobacterium tuberculosis FabH (mtFabH) catalyses a Claisen-type condensation between an acyl-CoA and malonyl-acyl carrier protein (ACP) to initiate the Type II fatty acid synthase cycle. To analyze the initial covalent acylation of mtFabH with acyl-CoA, we challenged it with mixture of C6-C20 acyl-CoAs a...

journal_title：Bioorganic chemistry

authors： Sachdeva S,Musayev F,Alhamadsheh MM,Neel Scarsdale J,Tonie Wright H,Reynolds KA

更新日期：2008-04-01 00:00:00

abstract：:The coenzyme function of ubiquinone was subject of extensive studies in mitochondria since more than 40 years. The catalytic activity of ubiquinone (UQ) in electron transfer and proton translocation in cooperation with mitochondrial dehydrogenases and cytochromes contributes essentially to the bioenergetic activity of...

journal_title：Bioorganic chemistry

authors： Nohl H,Kozlov AV,Staniek K,Gille L

更新日期：2001-02-01 00:00:00

abstract：:In efforts to develop new antitubercular agents, we report here the synthesis of a series of novel pyrrole hydrazine derivatives. The molecules were evaluated against inhibitors of InhA, which is one of the key enzymes involved in type II fatty acid biosynthetic pathway of the mycobacterial cell wall as well as inhibi...

journal_title：Bioorganic chemistry

authors： Joshi SD,More UA,Dixit SR,Balmi SV,Kulkarni BG,Ullagaddi G,Lherbet C,Aminabhavi TM

更新日期：2017-12-01 00:00:00

abstract：:Oxaliplatin-based chemotherapy is the current standard of care in adjuvant therapy for advanced colorectal cancer (CRC). But acquired resistance to oxaliplatin eventually occurs and becoming a major cause of treatment failure. Thus, there is an unmet need for developing new chemical entities (NCE) as new therapeutic c...

journal_title：Bioorganic chemistry

authors： Li Y,Sun Z,Cui Y,Zhang H,Zhang S,Wang X,Liu S,Gao Q

更新日期：2021-01-08 00:00:00

abstract：:Aldose reductase (AR) catalyzes the NADPH-dependent reduction of glucose to sorbitol in the polyol pathway, which plays an important role in the development of diabetic complications including cataract, retinopathy, nephropathy, and neuropathy. AR has been considered as an important target to heal these long-term diab...

journal_title：Bioorganic chemistry

authors： Sever B,Altıntop MD,Demir Y,Akalın Çiftçi G,Beydemir Ş,Özdemir A

更新日期：2020-09-01 00:00:00

abstract：:Colchicine site antimitotic agents typically suffer from low aqueous solubilities and are formulated as phosphate prodrugs of phenolic groups. These hydroxyl groups are the aim of metabolic transformations leading to resistance. There is an urgent need for more intrinsically soluble analogues lacking these hydroxyl gr...

journal_title：Bioorganic chemistry

authors： Álvarez R,Aramburu L,Gajate C,Vicente-Blázquez A,Mollinedo F,Medarde M,Peláez R

更新日期：2020-05-01 00:00:00

abstract：:Xanthatin, a natural sesquiterpene lactone, occurs as one of the major constituents of Xanthium plants (Compositae) and exhibits many important biological properties. To discover natural products-based pesticides, forty-nine Michael-type thiol/amino adducts of xanthatin were synthesized and characterized, while their ...

journal_title：Bioorganic chemistry

authors： Zhi XY,Jiang LY,Li T,Song LL,Wu LJ,Cao H,Yang C

更新日期：2020-04-01 00:00:00

abstract：:A series of new 2,4,6-trisubstituted pyrimidines and their N-alkyl bromide derivatives were prepared based upon methoxy substituted azachalcones as the starting materials. All newly synthesized compounds were screened for their anti-proliferative, cytotoxic, antibacterial activities and DNA/protein binding affinity. I...

journal_title：Bioorganic chemistry

authors： Kahriman N,Serdaroğlu V,Peker K,Aydın A,Usta A,Fandaklı S,Yaylı N

更新日期：2019-03-01 00:00:00