Bioactive monoterpene indole alkaloids from Nauclea officinalis.

abstract：:Proton decoupled 31P and 13C solution NMR experiments were applied to mixtures of 3-deoxy-D-manno-2-octulosonate-8-phosphate (KDO8P) synthase, with each of its natural substrates, phosphoenolpyruvate and arabinose-5-phosphate (ASP), and product KDO8P to identify the formation of the enzyme-substrate and enzyme-product...

journal_title：Bioorganic chemistry

authors： Kaustov L,Baasov T,Schmidt A

更新日期：2003-08-01 00:00:00

abstract：:The ethanolic extract obtained from the stems of Glycosmis pentaphylla was found to suppress antigen-mediated degranulation of rat basophilic leukemia (RBL-2H3) cells. Four new geranylated 2-quinolone alkaloids, named glycopentanolones A-D (1-4), and 12 known metabolites (5-16) were isolated from the ethanolic extract...

journal_title：Bioorganic chemistry

authors： Choi YH,Seo C,Jeong W,Lee JE,Lee JY,Ahn EK,Kang JS,Lee JH,Choi CW,Oh JS,Lee D,Hong SS

更新日期：2019-06-01 00:00:00

abstract：:Monoamine oxidase inhibitors (MAOIs) are potential drug candidates for the treatment of various neurological disorders like Parkinson's disease, Alzheimer's disease and depression. In the present study, two series of 4-substituted phenylpiperazine and 1-benzhydrylpiperazine (1-21) derivatives were synthesized and scre...

journal_title：Bioorganic chemistry

authors： Kumar B,Sheetal,Mantha AK,Kumar V

更新日期：2018-04-01 00:00:00

abstract：:Hydrogen sulfide (H2S) is a biologically important gaseous molecule that exhibits promising protective effects against a variety of pathological processes. For example, it was recognized as a blood pressure lowering agent. Aligned with the need for easily modifiable platforms for the H2S supply, we report here the pre...

journal_title：Bioorganic chemistry

authors： Zaorska E,Hutsch T,Gawryś-Kopczyńska M,Ostaszewski R,Ufnal M,Koszelewski D

更新日期：2019-07-01 00:00:00

abstract：:To understand the effect of counter ions (Na+) on the secondary conformation and functionality of the lysozyme, we have studied the interaction of lysozyme with counterion associated iron oxide nanoparticles (IONPs). The investigation was carried out at pH 7.4 and 9.0, with three different types of NPs, namely, bare I...

journal_title：Bioorganic chemistry

authors： Dyawanapelly S,Mehrotra P,Ghosh G,Jagtap DD,Dandekar P,Jain R

更新日期：2019-02-01 00:00:00

abstract：:Three novel series of triazolophthalazine derivatives bearing hydrazone moiety were designed, synthesized, and evaluated for their anticancer activity against four human cancer cell lines by MTT assay. Six derivatives demonstrated comparable activity with Doxorubicin reference drug against the selected cancer cells. E...

journal_title：Bioorganic chemistry

authors： Abulkhair HS,Turky A,Ghiaty A,Ahmed HEA,Bayoumi AH

更新日期：2020-07-01 00:00:00

abstract：:Phosphonates-based agents are well-known bone-seeking radiopharmaceuticals with application in detection and therapy. With higher sensitivity and resolution offered by Positron Emission Tomography (PET), tracers based on this technique are gaining huge attention. 68Ga-based generator and radiotracers render independen...

journal_title：Bioorganic chemistry

authors： Chauhan K,Mann G,Jaswal AP,Ojha H,Mishra AK,Datta A

更新日期：2020-11-01 00:00:00

abstract：:Several new 5,6-dihydropyrimidine-2(1H)-thione derivatives have been prepared and investigated for their potencies for anticonvulsant activity against maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) test in mice. The acute neurotoxicity was measured by rotarod test. Compounds 3c and 3l were foun...

journal_title：Bioorganic chemistry

authors： Sahu M,Siddiqui N,Iqbal R,Sharma V,Wakode S

更新日期：2017-10-01 00:00:00

abstract：:Tuberculosis (TB) is the world's second commonest cause of death next to HIV/AIDS. The increasing emergence of multi drug resistance and the recalcitrant nature of persistent infections pose an additional challenge for the treatment of TB. Due to the development of resistance to conventional antibiotics there is a nee...

journal_title：Bioorganic chemistry

authors： Nilewar SS,Kathiravan MK

更新日期：2014-02-01 00:00:00

abstract：:Five new maleimide derivatives, (+)- and (-)- farinomalein F (1), (+)- and (-)- farinomalein G (2), farinomalein H (3) and one new linearly fused prenylated indole alkaloid phomoamide (8), along with five known compounds 4-7 and 9 were isolated from the mangrove endophytic fungus Phomopsis sp. SYSUQYP-23. Their struct...

journal_title：Bioorganic chemistry

authors： Chen Y,Zhang L,Zou G,Li C,Yang W,Liu H,She Z

更新日期：2020-04-01 00:00:00

abstract：:Euphoroids A-C (1-3), three new ent-abietane-type diterpenoids, together with ten known analogues (4-13) were obtained from the roots of Euphorbia ebracteolata. The structures of these compounds were determined by extensive spectroscopic data analysis, including UV, HRESIMS, 1D-, and 2D-NMR data. The inhibitory effect...

journal_title：Bioorganic chemistry

authors： Han C,Peng Y,Wang Y,Huo X,Zhang B,Li D,Leng A,Zhang H,Ma X,Wang C

更新日期：2018-12-01 00:00:00

abstract：:P-glycoprotein (P-gp) is one of the cell membrane pumps which mediate the efflux of molecules such as anticancer drugs to the extracellular matrix of tumor cells. P_gp is a member of the ATP-binding cassette (ABC) transporter family that is implicated in cancer multidrug resistance (MDR). Since MDR is a contributor to...

journal_title：Bioorganic chemistry

authors： Mollazadeh S,Sahebkar A,Kalalinia F,Behravan J,Hadizadeh F

更新日期：2019-10-01 00:00:00

abstract：:A new series of derivatives characterized by the presence of the 3,4,5-trimethoxylbenzamide substituted benzofurans were synthesized and evaluated for antiproliferative activity against four cancer cell lines and one normal human cell line. Among them, derivative 6g with greatest cytotoxicity significantly inhibited t...

journal_title：Bioorganic chemistry

authors： Li Q,Jian XE,Chen ZR,Chen L,Huo XS,Li ZH,You WW,Rao JJ,Zhao PL

更新日期：2020-09-01 00:00:00

abstract：:Hunting small molecules as anti-inflammatory agents/drugs is an expanding and successful approach to treat several inflammatory diseases such as cancer, asthma, arthritis, and psoriasis. Besides other methods, inflammatory diseases can be treated by lipoxygenase inhibitors, which have a profound influence on the devel...

journal_title：Bioorganic chemistry

authors： Muzaffar S,Shahid W,Riaz N,Saleem M,Ashraf M,Aziz-Ur-Rehman,Bashir B,Kaleem A,Al-Rashida M,Baral B,Bhattarai K,Gross H

更新日期：2020-12-03 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：:Staphylococcus aureus is the leading cause of bacteraemia and the dwindling supply of effective antibacterials has exacerbated the problem of managing infections caused by this bacterium. Isoliquiritigenin (ISL) is a plant flavonoid that displays therapeutic potential against S. aureus. The present study identified a ...

journal_title：Bioorganic chemistry

authors： Gupta VK,Gaur R,Sharma A,Akther J,Saini M,Bhakuni RS,Pathania R

更新日期：2019-03-01 00:00:00

abstract：:A series of new N-acyl 8,9-dihydro-4-methoxy-7H-2-benzo[de]quinolinalkanamines have been prepared and tested for their ability to activate pigment granule aggregation in Xenopus laevis melanophores and bind to the recombinant human MT(1) and MT(2) melatonin receptor subtypes expressed in NIH 3T3 cells. Compounds with ...

journal_title：Bioorganic chemistry

authors： Tsotinis A,Eleutheriades A,Hough KA,Davidson K,Sugden D

更新日期：2007-04-01 00:00:00

abstract：:A class of 3-substituted 1H-pyrrolo[2,3-b]pyridine derivatives were designed, synthesized and evaluated for their in vitro biological activities against maternal embryonic leucine zipper kinase (MELK). Among these derivatives, the optimized compound 16h exhibited potent enzyme inhibition (IC50 = 32 nM) and excellent a...

journal_title：Bioorganic chemistry

authors： Wang R,Chen Y,Yang B,Yu S,Zhao X,Zhang C,Hao C,Zhao D,Cheng M

更新日期：2020-01-01 00:00:00

abstract：:In the present work, a novel series of B-RAF kinase inhibitors having imidazo[2,1-b]oxazole scaffold was designed and synthesized based on the structures of the well-known B-RAF inhibitors. The twenty two final compounds were tested over A375 and SKMEL28 cell lines to determine the primary cytotoxic activity of these ...

journal_title：Bioorganic chemistry

authors： Abdel-Maksoud MS,Ammar UM,El-Gamal MI,Gamal El-Din MM,Mersal KI,Ali EMH,Yoo KH,Lee KT,Oh CH

更新日期：2019-12-01 00:00:00

abstract：:The structure-function relation of YR-10 (YGKPVAVPAR) was investigated by synthesizing four structural analogs of that including YHR-10 (YGKHVAVHAR), GA-8 (GKPVAVPA), GHA-8 (GKHVAVHA), and PAR-3 (PAR). GA-8 (GKPVAVPA) was synthesized on the basis of simulated enzymatic gastrointestinal digestion performed by bioinform...

journal_title：Bioorganic chemistry

authors： Mirzaei M,Mirdamadi S,Safavi M,Hadizadeh M

更新日期：2019-06-01 00:00:00

abstract：:A series of novel β-pinene-based thiazole derivatives were synthesized and characterized by HRMS, 1H NMR, and 13C NMR analyses as potential antineoplastic agents. Derivatives were evaluated for their anticancer activities in vitro, and the data manifested that most target compounds showed potent anti-proliferative act...

journal_title：Bioorganic chemistry

authors： Wang Y,Wu C,Zhang Q,Shan Y,Gu W,Wang S

更新日期：2019-03-01 00:00:00

abstract：:Starting from the compound (3,4-dimethoxyphenyl)(2-(3,4-dimethoxyphenyl)cyclopent-1-en-1-yl)methanone (4), two diols and three tetrol derivatives were synthesised. Morover, from the reactions of 1,3-dimethoxybenzene and 1,4-dimethoxybenzene with adipoyl chloride, fifteen new along with nine known compounds were obtain...

journal_title：Bioorganic chemistry

authors： Artunc T,Menzek A,Taslimi P,Gulcin I,Kazaz C,Sahin E

更新日期：2020-07-01 00:00:00

abstract：:Inflammation is a fundamental physiological process that is essential for survival of human being but at the same time is one of the major causes of human morbidity and mortality. In the past decade, numerous advances have taken place in the understanding and development of novel anti-inflammatory drugs. Therefore, in...

journal_title：Bioorganic chemistry

authors： El Sayed MT,El-Sharief MAMS,Zarie ES,Morsy NM,Elsheakh AR,Nayel M,Voronkov A,Berishvili V,Sabry NM,Hassan GS,Abdel-Aziz HA

更新日期：2018-02-01 00:00:00

abstract：:With the aim of finding new anti-inflammatory drugs, a series of new Glycyrrhetinic acid derivatives (1-34) have been designed and synthesized by structural modification, and their anti-inflammatory activities in vitro have been evaluated. The anti-inflammatory activities assay demonstrated that compound 5b suppressed...

journal_title：Bioorganic chemistry

authors： Bian M,Zhen D,Shen QK,Du HH,Ma QQ,Quan ZS

更新日期：2020-12-29 00:00:00

abstract：:A series of bis-indolone-N-oxides, 1a-f, was prepared from bis(ethynyl)benzenes and o-halonitroaryls and studied for their in vitro antiplasmodial activities against Plasmodium falciparum and representative strains of bacteria and candida as well as for their cytotoxicity against a human tumor cell line (MCF7). They d...

journal_title：Bioorganic chemistry

authors： Najahi E,Valentin A,Téné N,Treilhou M,Nepveu F

更新日期：2013-06-01 00:00:00

abstract：:A series of 4-imidazolylflavans having a variety of substituents on the 2-phenyl ring was synthesized and investigated for their inhibitory effect against aromatase. Structure-activity relationships of these compounds were determined. An additional chlorine atom or a cyano group at the 4' position did not enhance arom...

journal_title：Bioorganic chemistry

authors： Pouget C,Yahiaoui S,Fagnere C,Habrioux G,Chulia AJ

更新日期：2004-12-01 00:00:00

abstract：:In the present study, we have reported synthesis and biological evaluation of a series of fifteen 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole derivatives against both promastigotes and amastigotes of Leishmania parasites responsible for visceral (L. donovani) and cutaneous (L. amazonensis) leishmaniasis. Among these repo...

journal_title：Bioorganic chemistry

authors： Ashok P,Chander S,Chow LM,Wong IL,Singh RP,Jha PN,Sankaranarayanan M

更新日期：2017-02-01 00:00:00

abstract：:This study focused on synthesis various dimethyl N-benzyl-1H-1,2,3-triazole-4,5-dicarboxylate and (N-benzyl-1H-1,2,3-triazole-4,5-diyl)dimethanol derivatives under the conditions of green chemistry without the use of solvent and catalysts. Their inhibition properties were also investigated on xanthine oxidase (XO) act...

journal_title：Bioorganic chemistry

authors： Yagiz G,Noma SAA,Altundas A,Al-Khafaji K,Taskin-Tok T,Ates B

更新日期：2021-01-12 00:00:00

abstract：:Focal adhesion kinase (FAK) is an intracellular non-receptor tyrosine kinase responsible for development of various tumor types. Aiming to explore new potent inhibitors, two series of 2,4-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives were designed and synthesized on the base of structure-based design strategy....

journal_title：Bioorganic chemistry

authors： Wang R,Zhao X,Yu S,Chen Y,Cui H,Wu T,Hao C,Zhao D,Cheng M

更新日期：2020-09-01 00:00:00

abstract：:Eleven undescribed quinolone alkaloids, pesimquinolones I-S (1-4 and 6-12), as well as eleven known congeners (5 and 13-22), were isolated from the solid culture broth of the fungus Penicillium simplicissimum. Their chemical structures with absolute configurations were established by a combination of NMR spectroscopy,...

journal_title：Bioorganic chemistry

authors： Dai C,Li X,Zhang K,Li XN,Wang W,Zang Y,Chen X,Li Q,Wei M,Chen C,Zhu H,Zhang Y

更新日期：2021-01-08 00:00:00