当前位置： SCI文献检索 > BIOORGANIC CHEMISTRY期刊下所有文献 > Discovery of novel quinazolines as potential anti-tubulin agents occupying three zones of colchicine domain.

Discovery of novel quinazolines as potential anti-tubulin agents occupying three zones of colchicine domain.

Abstract：

:A series of novel quinazolines as tubulin inhibitors occupying three zones of colchicine domain have been designed and synthesized inspired by the recently disclosed crystal structure of verubulin analogue 6 with tubulin. Among the newly synthesized compounds, 19c showed noteworthy potency against K562, HepG2, KB, HCT-8 and MDB-MB-231 cancer cells. In vitro microtubule polymerization assays identified 19c as a potent tubulin assembly inhibitor, the binding mode of which with tubulin was confirmed by molecular modeling studies to occupy three zones of tubulin domain. Furthermore, 19c disrupted the intracellular microtubule network, caused G2/M phase arrest, induced cell apoptosis and depolarized mitochondria of K562 cells. 19c also reduced the cell migration and disrupted the capillary-like tube formation of human umbilical vein endothelial cells (HUVECs). Importantly, 19c significantly and dose dependently inhibited tumor growth in H22 liver cancer xenograft mouse model. All these results suggested that 19c deserves further research as a novel and potential anti-tubulin agent for the treatment of cancers.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Li W,Yin Y,Shuai W,Xu F,Yao H,Liu J,Cheng K,Xu J,Zhu Z,Xu S

doi

10.1016/j.bioorg.2018.10.027

subject

Has Abstract

pub_date

2019-03-01 00:00:00

pages

380-390

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(18)30618-7

journal_volume

83

pub_type

杂志文章

相关文献

BIOORGANIC CHEMISTRY文献大全
  • Identification and evaluation of a napyradiomycin as a potent Nrf2 activator: Anti-oxidative and anti-inflammatory activities.

    abstract：:Natural products with antioxidant and anti-inflammatory properties are important sources of therapeutic agents. The nuclear factor E2-related factor 2 (Nrf2)/antioxidant response element (ARE) pathway is a well-known defense system against oxidative stress. In this study, a panel of extracts of plants, fungi, and bact...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104434

    authors： Choi JW,Kim GJ,Kim HJ,Nam JW,Kim J,Chin J,Park JH,Choi H,Park KD

    更新日期：2020-12-01 00:00:00

  • Structure-activity relationships and molecular docking of thirteen synthesized flavonoids as horseradish peroxidase inhibitors.

    abstract：:For the first time, the structure-activity relationships of thirteen synthesized flavonoids have been investigated by evaluating their ability to modulate horseradish peroxidase (HRP) catalytic activity. Indeed, a modified spectrophotometrically method was carried out and optimized using 4-methylcatechol (4-MC) as per...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2017.08.001

    authors： Mahfoudi R,Djeridane A,Benarous K,Gaydou EM,Yousfi M

    更新日期：2017-10-01 00:00:00

  • A comparison study on ribonuclease A modifications induced by substituted p-benzoquinones.

    abstract：:In this paper, we present our investigation on ribonuclease A (RNase) modifications induced by 1,4-benzoquinone (PBQ), 2-methyl-1,4-benzoquinone (MBQ), and 2-chloro-1,4-benzoquinone (CBQ). The goal of the study was to evaluate quinone-induced protein modifications as well as substituent effects, utilizing several tech...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2015.02.004

    authors： Kim J,Albu TV,Vaughn AR,Kang SM,Carver EA,Stickle DM

    更新日期：2015-04-01 00:00:00

  • Building fluorescent sensors for carbohydrates using template-directed polymerizations.

    abstract：:The ability to custom-make fluorescent sensors for different analytes could have a tremendous impact in a variety of areas. Template-directed polymerization or molecular imprinting seems to be a promising approach for the preparation of high-affinity and specific binding sites for different template molecules. However...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1006/bioo.2001.1219

    authors： Gao S,Wang W,Wang B

    更新日期：2001-10-01 00:00:00

  • Non-viral vectors for the mediation of RNAi.

    abstract：:Though the delivery of siRNA into cells, tissues or organs remains to be a big obstacle for its applications, recently siRNA therapeutics has developed rapidly and already there are clinical trials ongoing or planned. Some non-viral vectors have attracted much more attention and shown the great potential for combating...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.bioorg.2011.07.005

    authors： Zhang S,Zhao Y,Zhi D,Zhang S

    更新日期：2012-02-01 00:00:00

  • From orexin receptor agonist YNT-185 to novel antagonists with drug-like properties for the treatment of insomnia.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104179

    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

  • 2,4-Diketo esters: Crucial intermediates for drug discovery.

    abstract：:Convenient structures such as 2,4-diketo esters have been widely used as an effective pattern in medicinal chemistry and pharmacology for drug discovery. 2,4-Diketonate is a common scaffold that can be found in many biologically active and naturally occurring compounds. Also, many 2,4-diketo ester derivatives have bee...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.bioorg.2020.104343

    authors： Joksimović N,Janković N,Davidović G,Bugarčić Z

    更新日期：2020-12-01 00:00:00

  • Facile synthesis and antimicrobial activity of CdS-Ag2S nanocomposites.

    abstract：:In this study CdS-Ag2S nanocomposites for antibacterial activity were synthesized via facile co-precipitation method using PVP as capping agent. The prepared nanocomposites have particle sizes in the range of 50-100 nm (SEM) and PVP addition has good influence on the morphology of nanocomposites. The antimicrobial act...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103064

    authors： Iqbal T,Ali F,Khalid NR,Tahir MB,Ijaz M

    更新日期：2019-09-01 00:00:00

  • Synthesis of dual-action parthenolide prodrugs as potent anticancer agents.

    abstract：:Cancer stem cells are responsible for the failure of a large number of cancer treatments and the re-emergence of cancer in patients. Parthenolide is a potent anticancer sesquiterpene lactone that is also able to kill cancer stem cells. The main problem with this compound is its poor solubility in water. To solve this ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2017.01.020

    authors： Taleghani A,Nasseri MA,Iranshahi M

    更新日期：2017-04-01 00:00:00

  • Design, synthesis and molecular docking of pyrazolo [3,4d] thiazole hybrids as potential anti-HIV-1 NNRT inhibitors.

    abstract：:A series of pyrazolo[3.4,d]thiazole hybrids 6 were synthesized from 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5. The 5-arylidene-2-imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones 5 were synthesized from 2-amino-4-arylthiazoles 1 and 2-chloro-acetamido-4-arylthiazoles 2 via the formation of 2-imino-...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.02.006

    authors： Kasralikar HM,Jadhavar SC,Goswami SV,Kaminwar NS,Bhusare SR

    更新日期：2019-05-01 00:00:00

  • Design, synthesis, molecular modeling, in vivo studies and anticancer activity evaluation of new phthalazine derivatives as potential DNA intercalators and topoisomerase II inhibitors.

    abstract：:Herein we report the design and synthesis of a new series of phthalazine derivatives as Topo II inhibitors and DNA intercalators. The synthesized compounds were in vitro evaluated for their cytotoxic activities against HepG-2, MCF-7 and HCT-116 cell lines. Additionally, Topo II inhibitory activity and DNA intercalatin...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104233

    authors： El-Helby AA,Sakr H,Ayyad RR,Mahdy HA,Khalifa MM,Belal A,Rashed M,El-Sharkawy A,Metwaly AM,Elhendawy MA,Radwan MM,ElSohly MA,Eissa IH

    更新日期：2020-10-01 00:00:00

  • Water-soluble betaines and amines based on thiacalix[4]arene scaffold as new cholinesterase inhibitors.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103455

    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

  • Reconstitution of UDP-galactopyranose mutase with 1-deaza-FAD and 5-deaza-FAD: analysis and mechanistic implications.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2003.08.002

    authors： Huang Z,Zhang Q,Liu HW

    更新日期：2003-12-01 00:00:00

  • Recent advances in synthesis and medicinal chemistry of benzodiazepines.

    abstract：:Benzodiazepines (BZDs) represent a diverse class of bicyclic heterocyclic molecules. In the last few years, benzodiazepines have emerged as potential therapeutic agents. As a result, several mild, efficient and high yielding protocols have been developed that offer access to various functionalized benzodiazepines (BZD...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.bioorg.2020.103668

    authors： Arora N,Dhiman P,Kumar S,Singh G,Monga V

    更新日期：2020-04-01 00:00:00

  • Design, synthesis, and anticancer activity of imidazo[2,1-b]oxazole-based RAF kinase inhibitors.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103349

    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

  • Chemical characterization of cytotoxic indole acetic acid derivative from mulberry fruit (Morus alba L.) against human cervical cancer.

    abstract：:The fruit of the white mulberry tree (Morus alba L.) is a multiple fruit with a sweet flavor commonly consumed around the world. Chemical investigation of the fruits led to the isolation of two indole acetic acid derivatives (1 -2) including a new compound, which turned out to be an isolation artifact, 3S-(β-D-glucopy...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2017.10.015

    authors： Yu JS,Lee D,Lee SR,Lee JW,Choi CI,Jang TS,Kang KS,Kim KH

    更新日期：2018-02-01 00:00:00

  • Current development of 5-nitrofuran-2-yl derivatives as antitubercular agents.

    abstract：:Pulmonary tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis (MTB) and still remains one of the foremost fatal infectious diseases, infecting nearly a third of the worldwide population. The emergencies of multidrug-resistant and extensively drug-resistant tuberculosis (MDR and XDR-TB) prom...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.bioorg.2019.102969

    authors： Elsaman T,Mohamed MS,Mohamed MA

    更新日期：2019-07-01 00:00:00

  • Synthesis and in vitro antileishmanial activity of 5-substituted-2'-deoxyuridine derivatives.

    abstract：:We report herein the synthesis and the in vitro antileishmanial evaluation of 5-substituted-2'-deoxyuridine nucleosides. The most active compound against Leishmania donovani promastigotes was Thia-dU (3a) with an IC50 =3 microM. This compound exhibited the same activity as zidovudine (3'-azido-2'-deoxythymidine) used ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2005.07.001

    authors： Peyron C,Benhida R,Bories C,Loiseau PM

    更新日期：2005-12-01 00:00:00

  • A novel bi-functional chalcone inhibits multi-drug resistant Staphylococcus aureus and potentiates the activity of fluoroquinolones.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.10.024

    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

  • Natural product-based semisynthesis and biological evaluation of thiol/amino-Michael adducts of xanthatin derived from Xanthium strumarium as potential pesticidal agents.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.103696

    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

  • Chemo-enzymatic synthesis and cell-growth inhibition activity of resveratrol analogues.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2004.08.003

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

    更新日期：2005-02-01 00:00:00

  • Vibsane-type diterpenoids from Viburnum odoratissimum and their cytotoxic activities.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104498

    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

  • α-Tocopherol-ascorbic acid hybrid antioxidant based cationic amphiphile for gene delivery: Design, synthesis and transfection.

    abstract：:Natural antioxidants and vitamins have potential to protect biological systems from peroxidative damage induced by peroxyl radicals, α-tocopherol (Vitamin E, lipid soluble) and ascorbic acid (vitamin C, water soluble), well known natural antioxidant molecules. In the present study we described the synthesis and biolog...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2018.02.025

    authors： Muripiti V,Brijesh L,Rachamalla HK,Marepally SK,Banerjee R,Patri SV

    更新日期：2019-02-01 00:00:00

  • New bisphosphorothioates and bisphosphoroamidates: synthesis, molecular modeling and determination of insecticide and toxicological profile.

    abstract：:A series of new compounds, N,N'-bis(dialkylphosphoryl)diamines and S,S'-bis(dialkylphosphoryl)-1,3-propanedithiols were prepared by a Todd-Atherton like reaction of dialkylphosphites with symmetrical diamines and 1,3-propanedithiols in a biphasic system [F.R. Athertoon, H.T. Howard, A.R. Todd, J. Chem. Soc. (1948) 110...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2006.08.006

    authors： dos Santos VM,Sant'Anna CM,Moya Borja GE,Chaaban A,Côrtes WS,DaCosta JB

    更新日期：2007-02-01 00:00:00

  • 68Ga-Labeled bismacrocyclic methylene phosphonate as potential bone seeking PET radiopharmaceutical.

    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

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104185

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

    更新日期：2020-11-01 00:00:00

  • Functional studies of rat hydroxymethylbilane synthase.

    abstract：:The structurally related tetrapyrrolic pigments are a group of natural products that participate in many of the fundamental biosynthetic and catabolic processes of living organisms. Hydroxymethylbilane synthase catalyzes a rate-limiting step for the biosyntheses of tetrapyrrolic natural products. We carried out extens...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2008.07.001

    authors： Li N,Chu X,Wu L,Liu X,Li D

    更新日期：2008-10-01 00:00:00

  • Structure-activity relationship studies of prostate-specific membrane antigen (PSMA) inhibitors derived from α-amino acid with (S)- or (R)-configuration at P1' region.

    abstract：:Prostate-specific membrane antigen (PSMA), a type II membrane glycoprotein, is considered an excellent target for the diagnosis or treatment of prostate cancer. We previously investigated the effect of β- and γ-amino acids with (S)- or (R)-configuration in the S1 pocket on the binding affinity for PSMA. However, compr...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.104304

    authors： Kwon H,Lim H,Ha H,Choi D,Son SH,Nam H,Minn I,Byun Y

    更新日期：2020-11-01 00:00:00

  • Total synthesis and anti-inflammatory evaluation of violacin A and its analogues.

    abstract：:A concise total synthesis of an exceedingly potent anti-inflammatory agent violacin A as well as the preparation of thirty analogues of this lead from commercially available orcinol are described. Highlights of our synthetic efforts involve Friedel-Crafts acylation, the regioselective etherification and esterification...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103420

    authors： Liu Q,Mu Y,An Q,Xun J,Ma J,Wu W,Xu M,Xu J,Han L,Huang X

    更新日期：2020-01-01 00:00:00

  • Cytotoxicity of oleanolic and ursolic acid derivatives toward hepatocellular carcinoma and evaluation of NF-κB involvement.

    abstract：:Oleanolic and ursolic acids are two ubiquitous isomeric triterpene phytochemicals known for their anticancer activity. A set of derivatives of the two compounds with a modified oxidation state and lipophylicity at C-3 and C-28 positions, were prepared and tested as anticancer agents versus the lines HepG2, Hep3B and H...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2019.103054

    authors： Fontana G,Bruno M,Notarbartolo M,Labbozzetta M,Poma P,Spinella A,Rosselli S

    更新日期：2019-09-01 00:00:00

  • Structural elucidation and in vivo anti-arthritic activity of β-amyrin and polpunonic acid isolated from the root bark of Ziziphus abyssinica HochstEx. A Rich (Rhamnaceae).

    abstract：:Two natural products, compounds 1 and 2 were isolated from the root bark of Ziziphus abyssinica for the first time and were structurally elucidated as β-amyrin and polpunonic acid, respectively. Both compounds were further subjected to an in vivo study in rats to evaluate their anti-arthritic potency. Compared to the ...

    journal_title：Bioorganic chemistry

    pub_type： 杂志文章

    doi：10.1016/j.bioorg.2020.103744

    authors： Henneh IT,Huang B,Musayev FN,Hashimi RA,Safo MK,Armah FA,Ameyaw EO,Adokoh CK,Ekor M,Zhang Y

    更新日期：2020-05-01 00:00:00