当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Recent advances in the discovery of potent and selective HDAC6 inhibitors.

Recent advances in the discovery of potent and selective HDAC6 inhibitors.

Abstract：

:Histone deacetylase HDAC6, a member of the class IIb HDAC family, is unique among HDAC enzymes in having two active catalytic domains, and has unique physiological function. In addition to the modification of histone, HDAC6 targets specific substrates including α-tubulin and HSP90, and are involved in protein trafficking and degradation, cell shape and migration. Selective HDAC6 inhibitors are an emerging class of pharmaceuticals due to the involvement of HDAC6 in different pathways related to neurodegenerative diseases, cancer, and immunology. Therefore, extensive investigations have been made in the discovery of selective HDAC6 inhibitors. Based on their different zinc binding groups (ZBGs), in this review, HDAC6 inhibitors are grouped as hydroxamic acids, a sulfur containing ZBG based derivatives and other ZBG-derived compounds, and their enzymatic inhibitory activity, selectivity and other biological activities are introduced and summarized.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Wang XX,Wan RZ,Liu ZP

doi

10.1016/j.ejmech.2017.10.040

subject

Has Abstract

pub_date

2018-01-01 00:00:00

pages

1406-1418

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(17)30840-1

journal_volume

143

pub_type

杂志文章,评审

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • 5,10b-Ethanophenanthridine amaryllidaceae alkaloids inspire the discovery of novel bicyclic ring systems with activity against drug resistant cancer cells.

    abstract：:Plants of the Amaryllidaceae family produce a large variety of alkaloids and non-basic secondary metabolites, many of which are investigated for their promising anticancer activities. Of these, crinine-type alkaloids based on the 5,10b-ethanophenanthridine ring system were recently shown to be effective at inhibiting ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.05.004

    authors： Henry S,Kidner R,Reisenauer MR,Magedov IV,Kiss R,Mathieu V,Lefranc F,Dasari R,Evidente A,Yu X,Ma X,Pertsemlidis A,Cencic R,Pelletier J,Cavazos DA,Brenner AJ,Aksenov AV,Rogelj S,Kornienko A,Frolova LV

    更新日期：2016-09-14 00:00:00

  • Synthesis, biological evaluation and molecular docking studies of some pyrimidine derivatives.

    abstract：:Some novel pyrimidine-5-carbonitrile derivatives bearing various substituent have been synthesized. The structures of target compounds were confirmed by elemental analysis and spectral data. Some selected members of the newly synthesized compounds were investigated for their cytotoxic potency against certain human tum...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2013.05.028

    authors： Fargualy AM,Habib NS,Ismail KA,Hassan AM,Sarg MT

    更新日期：2013-08-01 00:00:00

  • Synthesis and structure-activity relationship of 3-O-acylated (-)-epigallocatechins as 5α-reductase inhibitors.

    abstract：:A series of 3-O-acylated (-)-epigallocatechins were synthesized and their inhibition of steroid 5α-reductase was studied. They were prepared from the reaction of EGCG with tert-butyldimethylsilyl chloride followed by reductive cleavage of the ester bond. The resultant (-)-epigallocatechins penta-O-tert-butyldimethylsi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.10.011

    authors： Lin SF,Lin YH,Lin M,Kao YF,Wang RW,Teng LW,Chuang SH,Chang JM,Yuan TT,Fu KC,Huang KP,Lee YS,Chiang CC,Yang SC,Lai CL,Liao CB,Chen P,Lin YS,Lai KT,Huang HJ,Yang JY,Liu CW,Wei WY,Chen CK,Hiipakka RA,Liao S

    更新日期：2010-12-01 00:00:00

  • TNF-α and IL-6 inhibitors: Conjugates of N-substituted indole and aminophenylmorpholin-3-one as anti-inflammatory agents.

    abstract：:The conjugates obtained by the combination of indole and aminophenyl morpholinone were screened for TNF-α and IL-6 inhibition in microglial cells. Compound 4 was found to be the most potent anti-inflammatory agent as it reduced LPS induced level of inflammatory cytokines TNF-α and IL-6 by 71% and 53%, respectively. A ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.09.003

    authors： Singh P,Kaur S,Sharma A,Kaur G,Bhatti R

    更新日期：2017-11-10 00:00:00

  • In vitro and in vivo anticancer activity of 2-deacetoxytaxinine J and synthesis of novel taxoids and their in vitro anticancer activity.

    abstract：:The taxane diterpneoid 2-deacetoxytaxinine J (2-DAT-J) 1 has been isolated from the bark of Himalayan yew, Taxus baccata L. spp. wallichiana in a reasonably good yield (0.1%) and its anticancer activity against breast cancer cell lines (MCF-7 and MDA-MB-231) and normal human kidney epithelial cell line (HEK-293) has b...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.04.022

    authors： Reddy KP,Bid HK,Nayak VL,Chaudhary P,Chaturvedi JP,Arya KR,Konwar R,Narender T

    更新日期：2009-10-01 00:00:00

  • Synthesis and in vitro cytotoxic activity of pyrrolo[2,3-e]indole derivatives and a dihydro benzoindole analogue.

    abstract：:The synthesis of pyrrolo[2,3-e]indole derivatives with the structural characteristics of DNA bis- and mono-intercalators are described. A dihydro benzoindol analogue was also synthesised to elucidate the major structural requirements for cytotoxic activity. A biological evaluation of the test compounds was carried out...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(01)01328-9

    authors： Chacón-García L,Martínez R

    更新日期：2002-03-01 00:00:00

  • Antitumor activity and carrier properties of novel hemocyanins coupled to a mimotope of GD2 ganglioside.

    abstract：:Conjugation to carrier proteins is a way to improve the immunogenicity of peptides. Such is the case for peptides mimicking carbohydrate tumor-associated antigens in cancer vaccine development. The most used protein for this purpose is the keyhole limpet hemocyanin (KLH) from Megathura crenulata. Its limited bioavaila...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.02.082

    authors： Palacios M,Tampe R,Del Campo M,Zhong TY,López MN,Salazar-Onfray F,Becker MI

    更新日期：2018-04-25 00:00:00

  • Conjugation of substituted ferrocenyl to thiadiazine as apoptosis-inducing agents targeting the Bax/Bcl-2 pathway.

    abstract：:Ferrocene compounds are a class of biologically active compounds that has antitumour and antifungal properties. This study investigated the induction of apoptosis in human fibrosarcoma cells (HT1080) after treatment with a series of 6-ferrocenyl-3-subsituted7H-1,2,4-triazolo[3,4-b]- 1,3,4-thiadiazine (FTFs). We found ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.08.007

    authors： Miao R,Wei J,Lv M,Cai Y,Du Y,Hui X,Wang Q

    更新日期：2011-10-01 00:00:00

  • Anthranilic acid based CCK1 receptor antagonists: preliminary investigation on their second "touch point".

    abstract：:In this phase of structure-affinity relationship study of VL-0395, a new anthranilic acid based CCK1 selective antagonist, we propose a series of unnatural aminoacidic derivatives. The result of this work is the identification of a new CCK ligand, which possesses an affinity (IC50 = 35 nm) one order of magnitude great...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2005.01.002

    authors： Varnavas A,Lassiani L,Valenta V,Mennuni L,Makovec F,Hadjipavlou-Litina D

    更新日期：2005-06-01 00:00:00

  • Discovery of hydrazone containing thiadiazoles as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors.

    abstract：:Tuberculosis, caused by Mycobacterium tuberculosis, is a serious infectious disease and remains a global health problem. There is an increasing need for the discovery of novel therapeutic agents for its treatment due to the emerging multi-drug resistance. Herein, we present the rational design and the synthesis of eig...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112035

    authors： Doğan H,Doğan ŞD,Gündüz MG,Krishna VS,Lherbet C,Sriram D,Şahin O,Sarıpınar E

    更新日期：2020-02-15 00:00:00

  • Enaminonitrile in heterocyclic synthesis: synthesis and antimicrobial evaluation of some new pyrazole, isoxazole and pyrimidine derivatives incorporating a benzothiazole moiety.

    abstract：:Enaminonitrile 2 was used as key intermediate for the synthesis of polyfunctionally substituted heterocycles (e.g. pyrazoles, isoxazole, pyrimidines, thiazolo[3,2-a]pyrimidine, tetrazolo[1,5-a]pyrimidine, pyrido[1,2-a]pyrimidine, 1,5-benzodiazepine, and pyrazolo[1,5-a]pyrimidine) incorporating benzothiazole moiety via...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.07.024

    authors： Bondock S,Fadaly W,Metwally MA

    更新日期：2009-12-01 00:00:00

  • Rational approaches, design strategies, structure activity relationship and mechanistic insights for anticancer hybrids.

    abstract：:A Hybrid drug which comprises the incorporation of two drug pharmacophores in one single molecule are basically designed to interact with multiple targets or to amplify its effect through action on another bio target as one single molecule or to counterbalance the known side effects associated with the other hybrid pa...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2014.03.018

    authors： Nepali K,Sharma S,Sharma M,Bedi PM,Dhar KL

    更新日期：2014-04-22 00:00:00

  • InCl3 mediated heteroarylation of indoles and their derivatization via CH activation strategy: Discovery of 2-(1H-indol-3-yl)-quinoxaline derivatives as a new class of PDE4B selective inhibitors for arthritis and/or multiple sclerosis.

    abstract：:A new class of PDE4 inhibitors were designed and synthesized via the InCl3 mediated heteroarylation of indoles and their further derivatization through the Pd(II)-catalyzed CH activation strategy. This effort allowed us to discover a series of 2-(1H-indol-3-yl)-quinoxaline based inhibitors possessing PDE4B selectivity...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.04.020

    authors： Sunke R,Bankala R,Thirupataiah B,Ramarao EVVS,Kumar JS,Doss HM,Medishetti R,Kulkarni P,Kapavarapu RK,Rasool M,Mudgal J,Mathew JE,Shenoy GG,Parsa KVL,Pal M

    更新日期：2019-07-15 00:00:00

  • Synthesis and evaluation of novel chlorophyll a derivatives as potent photosensitizers for photodynamic therapy.

    abstract：:Chlorophyll a exhibits excellent photosensitive activity in photosynthesis. The unstability limited its application as photoensitizer drug in photodynamic therapy. Here a series of novel chlorophyll a degradation products pyropheophorbide-a derivatives were synthesized and evaluated for lung cancer in PDT. These compo...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.111959

    authors： Gao YH,Zhu XX,Zhu W,Wu D,Chen DY,Yan YJ,Wu XF,O'Shea DF,Chen ZL

    更新日期：2020-02-01 00:00:00

  • Synthesis and evaluation of novel rutaecarpine derivatives and related alkaloids derivatives as selective acetylcholinesterase inhibitors.

    abstract：:A series of novel rutaecarpine derivatives and related alkaloid derivatives 3-aminoalkanamido-substituted rutaecarpine 4a-f and 7,8-dehydrorutaecarpine 5a-c, and 6-aminoalkanamido-substituted 3-[2-(3-Indolyl)ethyl]-4(3a)-quinazolinones 8a-c, were synthesized and subjected to pharmacological evaluation as acetylcholine...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.12.044

    authors： Wang B,Mai YC,Li Y,Hou JQ,Huang SL,Ou TM,Tan JH,An LK,Li D,Gu LQ,Huang ZS

    更新日期：2010-04-01 00:00:00

  • Synthesis of tropolone derivatives and evaluation of their in vitro neuroprotective activity.

    abstract：:beta-Thujaplicin (hinokitiol or 2-hydroxy-4-isopropyl-2,4,6-cycloheptatrien-1-one), a natural tropolone, shows numerous activities while its synthetic analogues were found to exhibit anticancer and anti-ischemic activity. However, the ability of tropolone derivatives to protect neuronal cells from oxidative stress-ind...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.12.006

    authors： Koufaki M,Theodorou E,Alexi X,Nikoloudaki F,Alexis MN

    更新日期：2010-03-01 00:00:00

  • 2-Propargylamino-naphthoquinone derivatives as multipotent agents for the treatment of Alzheimer's disease.

    abstract：:Alzheimer's disease is a progressive brain disorder with characteristic symptoms and several pathological hallmarks. The concept of "one drug, one target" has not generated any new drugs since 2004. The new era of drug development in the field of AD builds upon rationally designed multi-target directed ligands that ca...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.113112

    authors： Mezeiova E,Janockova J,Andrys R,Soukup O,Kobrlova T,Muckova L,Pejchal J,Simunkova M,Handl J,Micankova P,Capek J,Rousar T,Hrabinova M,Nepovimova E,Marco-Contelles JL,Valko M,Korabecny J

    更新日期：2021-02-05 00:00:00

  • Synthesis and biological evaluation of 2,3-diarylimidazo[1,2-a]pyridines as antileishmanial agents.

    abstract：:A novel series of 2,3-diarylimidazo[1,2-a]pyridines was synthesized and evaluated for their antileishmanial activities. Four derivatives exhibited good activity against the promastigote and intracellular amastigote stages of Leishmania major, coupled with a low cytotoxicity against the HeLa human cell line. The impact...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2012.10.048

    authors： Marhadour S,Marchand P,Pagniez F,Bazin MA,Picot C,Lozach O,Ruchaud S,Antoine M,Meijer L,Rachidi N,Le Pape P

    更新日期：2012-12-01 00:00:00

  • Design, synthesis, biological evaluation, and modeling studies of novel conformationally-restricted analogues of sorafenib as selective kinase-inhibitory antiproliferative agents against hepatocellular carcinoma cells.

    abstract：:Sorafenib is one of the clinically used anticancer agents that inhibits several kinases. In this study, novel indole-based rigid analogues of sorafenib were designed and synthesized in order to enhance kinase selectivity and hence minimize the side effects associated with its use. The target compounds possess differen...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.113081

    authors： Sbenati RM,Zaraei SO,El-Gamal MI,Anbar HS,Tarazi H,Zoghbor MM,Mohamood NA,Khakpour MM,Zaher DM,Omar HA,Alach NN,Shehata MK,El-Gamal R

    更新日期：2021-01-15 00:00:00

  • Non-chelating p-phenylidene-linked bis-imidazoline analogs of known influenza virus endonuclease inhibitors: Synthesis and anti-influenza activity.

    abstract：:A novel chemotype topologically similar to known influenza virus PA endonuclease inhibitors has been designed. It was aimed to reproduce the extended topology of the known metal-chelating ligands with a p-phenylidene-linked bis-imidazoline scaffold. It was envisioned that aromatic groups introduced to this scaffolds v...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.10.063

    authors： Dar'in D,Zarubaev V,Galochkina A,Gureev M,Krasavin M

    更新日期：2019-01-01 00:00:00

  • Database mining applied to central nervous system (CNS) activity.

    abstract：:A data set of 389 compounds, active in the central nervous system (CNS) and divided into eight classes according to the receptor type, was extracted from the RBI database and analyzed by Self-Organizing Maps (SOM), also known as Kohonen Artificial Neural Networks. This method gives a 2D representation of the distribut...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(01)01233-8

    authors： Pintore M,Taboureau O,Ros F,Chrétien JR

    更新日期：2001-04-01 00:00:00

  • Design and one-pot synthesis of alpha-aminophosphonates and bis(alpha-aminophosphonates) by iron(III) chloride and cytotoxic activity.

    abstract：:In this study, we used a solution of FeCl(3) in THF to facilitate the Mannich-type reaction of aldehyde, amine and phosphite compounds to form corresponding alpha-aminophosphonates in a one-pot, three-component reaction. Selected alpha-aminophosphonates were entered into a biological assay test and were studied by doc...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.07.009

    authors： Rezaei Z,Firouzabadi H,Iranpoor N,Ghaderi A,Jafari MR,Jafari AA,Zare HR

    更新日期：2009-11-01 00:00:00

  • Discovery of a new selective inhibitor of A Disintegrin And Metalloprotease 10 (ADAM-10) able to reduce the shedding of NKG2D ligands in Hodgkin's lymphoma cell models.

    abstract：:Hodgkin's lymphoma (HL) is the most common malignant lymphoma in young adults in the western world. This disease is characterized by an overexpression of ADAM-10 with increased release of NKG2D ligands, involved in an impaired immune response against tumor cells. We designed and synthesized two new ADAM-10 selective i...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.01.053

    authors： Camodeca C,Nuti E,Tepshi L,Boero S,Tuccinardi T,Stura EA,Poggi A,Zocchi MR,Rossello A

    更新日期：2016-03-23 00:00:00

  • Substituted quinolinyl chalcones and quinolinyl pyrimidines as a new class of anti-infective agents.

    abstract：:Frequency of tuberculosis and malaria is progressively increasing worldwide. New emerging strain of bacterium and resistance to currently available drugs make this field more conscientious and alarming. In this connection a series of substituted quinolinyl chalcones and substituted quinolinyl pyrimidines were synthesi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.10.011

    authors： Sharma M,Chaturvedi V,Manju YK,Bhatnagar S,Srivastava K,Puri SK,Chauhan PM

    更新日期：2009-05-01 00:00:00

  • Preparation and antitubercular activities in vitro and in vivo of novel Schiff bases of isoniazid.

    abstract：:Structural modification of the frontline antitubercular isonicotinic acid hydrazide (INH) provides lipophilic adaptations (3-46) of the drug in which the hydrazine moiety of the parent compound has been chemically blocked from the deactivating process of N(2)-acetylation by N-arylaminoacetyl transferases. As a class, ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.05.009

    authors： Hearn MJ,Cynamon MH,Chen MF,Coppins R,Davis J,Joo-On Kang H,Noble A,Tu-Sekine B,Terrot MS,Trombino D,Thai M,Webster ER,Wilson R

    更新日期：2009-10-01 00:00:00

  • Synthesis, structure, toxicological and pharmacological investigations of 4-hydroxycoumarin derivatives.

    abstract：:Twenty 4-hydroxycoumarin derivatives were synthesized. Five of them are described for the first time. The X-ray crystal structure analysis of 3,3'-(2,3,4-trimethoxyphenylmethylene)bis-(4-hydroxy-2H-1-benzopyran-2-one) (7) and 3,3'-(3,5-dimethoxy-4-hydroxyphenylmethylene)bis-(4-hydroxy-2H-1-benzopyran-2-one) (9) confir...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2006.03.007

    authors： Manolov I,Maichle-Moessmer C,Danchev N

    更新日期：2006-07-01 00:00:00

  • Synthesis and in vitro antibacterial activity of new steroidal thiosemicarbazone derivatives.

    abstract：:We investigated the antibacterial activity of some new steroidal thiosemicarbazone derivatives, prepared from the reaction of cholest-5-en-7-one with thiosemicarbazides, in ethanol in the presence of a few drops of HCl at 80 degrees C in high yield. All the compounds have been characterized by means of elemental analy...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2007.12.004

    authors： Khan SA,Kumar P,Joshi R,Iqbal PF,Saleem K

    更新日期：2008-09-01 00:00:00

  • Design, synthesis and anthelmintic activity of 7-keto-sempervirol analogues.

    abstract：:The plant-derived, diterpenoid 7-keto-sempervirol was recently reported to display moderate activity against larval stages of Schistosoma mansoni (IC50 = 19.1 μM) and Fasciola hepatica (IC50 = 17.7 μM), two related parasitic blood and liver flukes responsible for the neglected tropical diseases schistosomiasis and fas...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.04.032

    authors： Crusco A,Bordoni C,Chakroborty A,Whatley KCL,Whiteland H,Westwell AD,Hoffmann KF

    更新日期：2018-05-25 00:00:00

  • Synthesis and DNA-binding studies of two ruthenium(II) complexes of an intercalating ligand.

    abstract：:Two new ruthenium(II) complexes [Ru(bpy)(2)(HBT)](2+) (1) and [Ru(phen)(2)(HBT)](2+) (2) (bpy=2,2'-bipyridine; phen=1,10-phenanthroline; HBT=11H, 13H-4, 5,9,10,12,14-hexaaza-benzo [b] triphenylene) have been synthesized and characterized by elemental analysis, mass spectra, (1)H NMR and cyclic voltammetry. The DNA bin...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.10.013

    authors： Lawrence Arockiasamy D,Radhika S,Parthasarathi R,Nair BU

    更新日期：2009-05-01 00:00:00

  • Quinolone antibiotic derivatives as new selective Axl kinase inhibitors.

    abstract：:Axl is a new promising molecular target for antineoplastic therapies. A series of quinolone antibiotic derivatives were designed and synthesized as new selective Axl inhibitors. One of the most promising compound 8i bound tightly to Axl with a Kd value of 1.1 nM, and inhibited its kinase activity with an IC50 value of...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.01.065

    authors： Tan L,Zhang Z,Gao D,Chan S,Luo J,Tu ZC,Zhang ZM,Ding K,Ren X,Lu X

    更新日期：2019-03-15 00:00:00