Design, synthesis, biological evaluation and molecular docking studies of novel benzofuran-pyrazole derivatives as anticancer agents.

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：:Inhibition of soluble epoxide hydrolase (sEH) is considered as a promising target to reduce blood pressure, improve insulin sensitivity, and decrease inflammation. In this study, a series of some novel quinazoline-4(3H)-one derivatives (3a-t) with varying steric and electronic properties was designed, synthesized and ...

journal_title：Bioorganic chemistry

authors： Hejazi L,Rezaee E,Tabatabai SA

更新日期：2020-06-01 00:00:00

abstract：:Lysine specific demethylase 1 (LSD1) is a flavin-dependent amine oxidase that selectively removes one or two methyl groups from H3 at Lys4 and is recognized as a promising therapeutic target for cancer and other diseases. Here, a series of 3-oxoamino-benzenesulfonamides were synthesized and evaluated for their inhibit...

journal_title：Bioorganic chemistry

authors： Xi J,Xu S,Wu L,Ma T,Liu R,Liu YC,Deng D,Gu Y,Zhou J,Lan F,Zha X

更新日期：2017-06-01 00:00:00

abstract：:The first phytochemical investigation of the seeds of Euphorbia peplus led to the isolation and characterization of five new (1-5), named euphopepluanones A-E, and five known diterpenoids (6-10). Their structures were established by extensive spectroscopic analysis and X-ray crystallographic experiments. Euphopepluano...

journal_title：Bioorganic chemistry

authors： Chen YN,Ding X,Lu QY,Li DM,Li BT,Liu S,Yang L,Zhang Y,Di YT,Fang X,Hao XJ

更新日期：2020-12-01 00:00:00

abstract：:The complete assignment of the 1H and 13C NMR spectra of bendaline (BNDL) was performed by mono-dimensional and homo- and hetero-correlated two-dimensional NMR experiments. The interaction between bendaline and albumin was also studied by the analysis of the motional parameters spin-lattice relaxation times, allowing ...

journal_title：Bioorganic chemistry

authors： Delfini M,Bianchetti C,Di Cocco ME,Pescosolido N,Porcelli F,Rosa R,Rugo G

更新日期：2003-10-01 00:00:00

abstract：:Novel ammonium and betaine derivatives of p-tert-butylthiacalix[4]arene in cone and 1,3-alternate conformation were synthesized with high yields for the first time. The obtained compounds form in water spherical nanoparticles. It was shown by molecular docking calculations and in vitro experiments that amino and betai...

journal_title：Bioorganic chemistry

authors： Padnya PL,Bayarashov EE,Zueva IV,Lushchekina SV,Lenina OA,Evtugyn VG,Osin YN,Petrov KA,Stoikov II

更新日期：2020-01-01 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：:It is still challenging to determine the potential targets of natural products, which is essential for further drug research and development. Due to its novel mechanism of action of inducing autophagy effects in breast cancer cells, asperphenamate has received our considerable attention. However, its unknown target in...

journal_title：Bioorganic chemistry

authors： Yuan L,Sheng L,He W,Zou C,Hu B,Liu J,Ge W,Liu Y,Wang J,Ma E

更新日期：2018-12-01 00:00:00

abstract：:Several novel N-substituted N-nitrosohydroxylamines were synthesized. They all inhibited mushroom tyrosinase, but the type of inhibition was different depending on the substituent. Some N-(mono- or dihydroxybenzyl)-N-nitrosohydroxylamines exhibited uncompetitive inhibition with respect to L-dopa. Among them, compound ...

journal_title：Bioorganic chemistry

authors： Shiino M,Watanabe Y,Umezawa K

更新日期：2003-04-01 00:00:00

abstract：:5-Aryl-1H-tetrazoles (1-24) were synthesized and screened for their xanthine oxidase (XO) inhibitory activity using allopurinol as standard inhibitor (IC50 = 2.0 ± 0.01 µM). Six compounds 3, 4, 5, 9, 21, and 24 exhibited significant to weak activities with IC50 values in the range of 7.4-174.2 µM. Active compounds wer...

journal_title：Bioorganic chemistry

authors： Fatima I,Zafar H,Khan KM,Saad SM,Javaid S,Perveen S,Choudhary MI

更新日期：2018-09-01 00:00:00

abstract：:Lambertellin (1) and ergosta-5,7,22-trien-3-ol (2) were isolated from the solid rice fermentation of the plant pathogenic fungus Pycnoporus sanguineus MUCL 51321. Their structures were elucidated using comprehensive spectroscopic methods. The isolated compounds were tested on lipopolysaccharide (LPS)-stimulated RAW 26...

journal_title：Bioorganic chemistry

authors： Jouda JB,Mfotie Njoya E,Mbazoa CD,Zhou Z,Meli Lannang A,Wandji J,Shiono Y,Wang F

更新日期：2018-10-01 00:00:00

abstract：:In previous work, the target of asperphenamate as a natural product was successfully determined as cathepsin by the natural product consensus pharmacophore strategy. In order to develop accurate SAR (structure-activity relationship) of asperphenamate-type cathepsin inhibitor, we chose several novel analogs with hetero...

journal_title：Bioorganic chemistry

authors： Yuan L,Zou C,Ge W,Liu Y,Hu B,Wang J,Lin B,Li Y,Ma E

更新日期：2020-01-01 00:00:00

abstract：:In this work, three hydrosoluble azocalix[4]arene derivatives, 5-(o-methylphenylazo)-25,26,27-tris(carboxymethoxy)-28-hydroxycalix[4]arene (o-MAC-Calix), 5-(m-methylphenylazo)-25,26,27-tris(carboxymethoxy)-28-hydroxycalix[4]arene (m-MAC-Calix) and 5-(p-methylphenylazo)-25,26,27-tris(carboxymethoxy)-28-hydroxycalix[4]a...

journal_title：Bioorganic chemistry

authors： Fan P,Wan L,Shang Y,Wang J,Liu Y,Sun X,Chen C

更新日期：2015-02-01 00:00:00

abstract：:As an extension for our earlier effort in the field of discovery of anticancer agents acting on DNA and Topo II, eighteen quinoxaline derivatives were designed and synthesized. Such members were designed to possess the main essential pharmacophoric features of DNA intercalators. The cytotoxic potential of the synthesi...

journal_title：Bioorganic chemistry

authors： Abbass EM,Khalil AK,Mohamed MM,Eissa IH,El-Naggar AM

更新日期：2020-11-01 00:00:00

abstract：:Chalcones (1, 3-Diphenyl-2-propen-1-one) consist of a three carbon α, β-unsaturated carbonyl system and act as precursors for the biosynthesis of flavonoids in plants. However, laboratory synthesis of various chalcones has also been reported. Both natural and synthetic chalcones are known to exhibit a variety of pharm...

journal_title：Bioorganic chemistry

authors： Ur Rashid H,Xu Y,Ahmad N,Muhammad Y,Wang L

更新日期：2019-06-01 00:00:00

abstract：:A series of iminothiazolines (4a-j) featuring 2,4,5-trichlorophenyl moiety and aroyl/heteroaroyl substituents has been prepared from readily accessible thioureas. In-vitro screening against glucosidase enzymes showed highly specific inhibition of α-glucosidase with a marked dependence of the potency upon the nature of...

journal_title：Bioorganic chemistry

authors： Kazmi M,Zaib S,Amjad ST,Khan I,Ibrar A,Saeed A,Iqbal J

更新日期：2017-10-01 00:00:00

abstract：:A series of novel 2-substituted quinoline-4-carboxylic acids was synthesized by Doebner reaction starting from freely available protocatechuic aldehyde and vanillin precursors. Human dihydroorotate dehydrogenase (hDHODH) was recognised as a clear molecular target for these heterocycles. All compounds were also tested ...

journal_title：Bioorganic chemistry

authors： Petrović MM,Roschger C,Chaudary S,Zierer A,Mladenović M,Jakovljević K,Marković V,Botta B,Joksović MD

更新日期：2020-12-01 00:00:00

abstract：:A series of benzimidazole-oxindole conjugates were synthesized and evaluated for their cytotoxic activity. The cytotoxicity assay results suggest that conjugates 5c and 5p exhibit promising cytotoxicity against human breast cancer cell line (MCF-7). The Cell cycle analysis revealed that these conjugates induced cell c...

journal_title：Bioorganic chemistry

authors： Kamal A,Nagaseshadri B,Nayak VL,Srinivasulu V,Sathish M,Kapure JS,Suresh Reddy C

更新日期：2015-12-01 00:00:00

abstract：:Four cationic porphyrin-anthraquinone (Por-AQ) hybrids differing in lengths of flexible alkyl linkage, 5-[4-(1-N-anthraquinonon-yl)-L-oxophenyl]-10,15,20-tris(N-methylpyridinium-4-yl)porphyrin triiodide, (L = acetyl, pentanoyl, octanoyl, undecanoyl, designed as [AQATMPyP]I3, [AQPTMPyP]I3, [AQOTMPyP]I3 and [AQUTMPyP]I3...

journal_title：Bioorganic chemistry

authors： Zhao P,Xu LC,Huang JW,Fu B,Yu HC,Zhang WH,Chen J,Yao JH,Ji LN

更新日期：2008-12-01 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：:Three different modified phosphoramidite nucleoside building blocks equipped with additional protected imidazole, masked alcohol and masked carboxylate functionality are synthesized and incorporated into oligonucleotides. Based on the serine-protease active site model, doubly and triply modified duplexes are created a...

journal_title：Bioorganic chemistry

authors： Catry MA,Gheerardijn V,Madder A

更新日期：2010-06-01 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：:One of the many methods of treating cancer is to terminate the uncontrolled growth of cancer cells. So, aiming the apoptotic pathway is an exciting approach to finding new anticancer agents. A novel series of cyanopyridines was designed and synthesized for antiproliferative evaluation. 2-Amino-6-(4-(benzyloxy)phenyl)-...

journal_title：Bioorganic chemistry

authors： Ismail MMF,Farrag AM,Harras MF,Ibrahim MH,Mehany ABM

更新日期：2020-01-01 00:00:00

abstract：:YNT-185 is the first known small molecule acting as orexin 2 receptor (OX2R) agonist with implication to narcolepsy treatment, served as a template scaffold in generating a small set of seven compounds with predictive affinity to OX2R. The design of the new small molecules was driven mostly by improving physicochemica...

journal_title：Bioorganic chemistry

authors： Mezeiova E,Janockova J,Konecny J,Kobrlova T,Benkova M,Dolezal R,Prchal L,Karasova-Zdarova J,Soukup O,Korabecny J

更新日期：2020-10-01 00:00:00

abstract：:In trying to develop new anticancer agents, a series of 1H-pyrazolo[3,4-b]pyridine derivatives was designed and synthesized. Fifteen compounds were evaluated in vitro for their anti-proliferative activity against HePG-2, MCF-7, HCT-116, and PC-3 cell lines. Additionally, DNA binding affinity of the synthesized derivat...

journal_title：Bioorganic chemistry

authors： Eissa IH,El-Naggar AM,El-Hashash MA

更新日期：2016-08-01 00:00:00

abstract：:A series of six novel and six known thieno[2,3-d]pyrimidin-4-amines 2-13 were synthesized, and further were used as a starting material for preparation of a small series of eight novel thieno[2,3-d]pyrimidin-4-phthalimides 14-21. Eight compounds, five amine and three phthalimide derivatives, inhibited bovine pancreati...

journal_title：Bioorganic chemistry

authors： Ts Mavrova A,Dimov S,Yancheva D,Kolarević A,Ilić BS,Kocić G,Šmelcerović A

更新日期：2018-10-01 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：:In this work, an enlarged series of 1,2,4-triazolo[4,3-a]pyrazin-3-ones was designed to target the human (h) A2A adenosine receptor (AR) or both hA1 and hA2A ARs. The novel 8-amino-1,2,4-triazolopyrazin-3-one derivatives 1-25 featured a phenyl or a benzyl pendant at position 2 while different aryl/heteroaryl substitue...

journal_title：Bioorganic chemistry

authors： Falsini M,Catarzi D,Varano F,Dal Ben D,Marucci G,Buccioni M,Volpini R,Di Cesare Mannelli L,Ghelardini C,Colotta V

更新日期：2019-06-01 00:00:00

abstract：:Seven new diterpenoids (1-7), including five 7-membered ring vibsane-type diterpenoids, vibsanolide A-E (1-5) and a pair of epimers of 14,15,16,17-tetranorvibsane-type diterpenoids possessing bicyclo[4.2.1]nonane moiety, vibsanolide F-G (6-7), together with twelve known analogues (8-19) were isolated from the crude ex...

journal_title：Bioorganic chemistry

authors： Li SF,Yu XQ,Li YL,Bai M,Lin B,Yao GD,Song SJ

更新日期：2021-01-01 00:00:00

abstract：:We report design and synthesis of set of novel anticancer agents based on caffeine-hydrazones bearing 2-hydroxyaryl- or 2-N-heteroaryl moiety. Anticancer activity evaluation using seven cancer cell lines and two non-malignant cell lines demonstrated that several derivatives display significant anticancer activity and ...

journal_title：Bioorganic chemistry

authors： Kaplánek R,Jakubek M,Rak J,Kejík Z,Havlík M,Dolenský B,Frydrych I,Hajdúch M,Kolář M,Bogdanová K,Králová J,Džubák P,Král V

更新日期：2015-06-01 00:00:00