Discovery of 1,4-pentadien-3-one derivatives containing quinoxaline scaffolds as potential apoptosis inducers.

abstract：:Aim: Anticancer immunochemotherapy represents an attractive paradigm to improve therapeutic responses and reduce side effects. Results & methodology: Here, we show that a naturally occurring host defense peptide, HN-1 inhibited multiple malignant cells proliferation and tumor growth in a xenografted human breast tumor...

journal_title：Future medicinal chemistry

authors： Qiao X,Yang H,Gao J,Cai S,Shi N,Wang M,Wang Y,Yu H

更新日期：2019-10-01 00:00:00

abstract：:VEGF is an important signaling protein involved in both vasculogenesis and angiogenesis. As an essential receptor protein tyrosine kinase propagating cellular signal transduction processes, VEGFR-2 is a central target for drug discovery against tumor-associated angiogenesis. Since the autophosphorylation of VEGFR-2 re...

journal_title：Future medicinal chemistry

authors： Huang L,Huang Z,Bai Z,Xie R,Sun L,Lin K

更新日期：2012-09-01 00:00:00

abstract：:An α-carbonic anhydrases (CAs, EC 4.2.1.1) was recently discovered, cloned and characterized in the genome of the protozoan parasite Trypanosoma cruzi, the causative agent of Chagas disease, a neglected but widespread tropical disease. Inhibition of this α-CAs (TcCA) with anions, sulfonamides, sulfamates, thiols and h...

journal_title：Future medicinal chemistry

authors： Supuran CT

更新日期：2016-01-01 00:00:00

abstract：:It is increasingly clear that academic high-throughput screening (HTS) and virtual HTS triage suffers from a lack of scientists trained in the art and science of early drug discovery chemistry. Many recent publications report the discovery of compounds by screening that are most likely artifacts or promiscuous bioacti...

journal_title：Future medicinal chemistry

authors： Dahlin JL,Walters MA

更新日期：2014-07-01 00:00:00

abstract：:Class I PI3Ks are composed of four catalytic subunit variants (p110α, p110β, p110δ and p110γ). The PI3K pathway is among the most frequently activated pathways in many diseases, and has emerged as an attractive target for drug development, in particular for the treatment of many human cancers including breast, prostat...

journal_title：Future medicinal chemistry

authors： Jeong Y,Kwon D,Hong S

更新日期：2014-05-01 00:00:00

abstract：BACKGROUND:Cucurbit[n]urils (CB[n]; n = 5, 6, 7, 8 or 10) are a family of macrocycles made from the acid-catalyzed condensation of glycoluril and formaldehyde. RESULTS:The synthesis of CB[n] using microwave radiation has been examined and the effect of acid type, reaction time and temperature on the distribution of pr...

journal_title：Future medicinal chemistry

authors： Wheate NJ,Patel N,Sutcliffe OB

更新日期：2010-02-01 00:00:00

abstract：:Aim: To encapsulate amphotericin B (AmB) with reduced toxicity and comparable activity. Results & methodology: The α-linolenic acid (ALA)-modified monomethoxy polyethylene glycol-g-PEI-g-ALA conjugate was employed to prepare AmB-loaded micelles (AmB-M). In vitro activity and release behavior of AmB-M were investigated...

journal_title：Future medicinal chemistry

authors： Xu H,Teng F,Zhou F,Zhu L,Wen Y,Feng R,Song Z

更新日期：2019-10-01 00:00:00

abstract：:Clinical development in brain diseases has one of the lowest success rates in the pharmaceutical industry, and many promising rationally designed single-target R&D projects fail in expensive Phase III trials. By contrast, successful older CNS drugs do have a rich pharmacology. This article will provide arguments sugge...

journal_title：Future medicinal chemistry

authors： Geerts H,Kennis L

更新日期：2014-01-01 00:00:00

abstract：:Sialic acid is associated with glycoproteins and gangliosides of eukaryotic cells. It regulates various molecular interactions, being implicated in inflammation and cancer, where its expression is regulated by sialyltransferases and sialidases. Angiogenesis, the formation of new capillaries, takes place during inflamm...

journal_title：Future medicinal chemistry

authors： Chiodelli P,Urbinati C,Paiardi G,Monti E,Rusnati M

更新日期：2018-12-01 00:00:00

abstract：:This review provides an overview of chemokines and their receptors, with an emphasis on general features and nomenclature along with a short summary of their properties and functions. It is intended as an introduction to the subject and a reference point for those wishing to learn key facts about chemokines and their ...

journal_title：Future medicinal chemistry

authors： Vinader V,Afarinkia K

更新日期：2012-05-01 00:00:00

abstract：BACKGROUND:The pathogenicity of influenza A and B viruses depends on the function of influenza neuraminidase (NA). Emerging resistant influenza A viruses of subtype H1N1 increasingly challenge the effectiveness of established NA inhibitors. Recent computational studies have indicated several weak points of NA that can ...

journal_title：Future medicinal chemistry

authors： Kirchmair J,Rollinger JM,Liedl KR,Seidel N,Krumbholz A,Schmidtke M

更新日期：2011-03-01 00:00:00

abstract：:The bromodomain proteins, known as the key targets in epigenetics, are 'readers' of acetylated lysine of histones. As a member of bromodomain proteins, bromodomain-containing protein 9 (BRD9) is a subunit of mammalian SWI/SNF chromatin remodeling complexes. However, the biological functions and the potential applicati...

journal_title：Future medicinal chemistry

authors： Hui M,Jian Z,Peiyuan Z,Zhenwei W,Huibin Z

更新日期：2018-04-01 00:00:00

abstract：:Cancer is a major devastating disease, and is a leading cause of death worldwide. Despite the progress in cancer treatment, cancer mortality rate remains high. Therefore, the discovery and development of improved anticancer drugs to treat cancer are needed. 4H-chromenes have strong cytotoxicity against a panel of huma...

journal_title：Future medicinal chemistry

authors： Patil SA,Patil R,Pfeffer LM,Miller DD

更新日期：2013-09-01 00:00:00

abstract：:Solomon Nwaka was born in Nigeria and grew up seeing at first hand the impact of neglected diseases. His research efforts have taken him across the globe, in both the developed and developing world. Following posts in academia, industry and at the Medicines for Malaria Venture, he is now at the WHO where he is engaged...

journal_title：Future medicinal chemistry

authors： Nwaka S

更新日期：2011-09-01 00:00:00

abstract：:Alzheimer's disease (AD) is the most common cause of dementia with no cure at present. Cholesterol metabolism is closely associated with AD at several stages. ACAT1 converts free cholesterol to cholesteryl esters, and plays important roles in cellular cholesterol homeostasis. Recent studies show that in a mouse model,...

journal_title：Future medicinal chemistry

authors： Shibuya Y,Chang CC,Chang TY

更新日期：2015-01-01 00:00:00

abstract：:The compound class of 3-carboranyl thymidine analogues (3CTAs) are boron delivery agents for boron neutron capture therapy (BNCT), a binary treatment modality for cancer. Presumably, these compounds accumulate selectively in tumor cells via intracellular trapping, which is mediated by hTK1. Favorable in vivo biodistri...

journal_title：Future medicinal chemistry

authors： Khalil A,Ishita K,Ali T,Tjarks W

更新日期：2013-04-01 00:00:00

abstract：:The emergence of antimicrobial resistance has created a need for the development of novel antibacterial therapies to treat infection. Natural products that exhibit antibacterial activity offer validated starting points for library generation, and the authors report here that small molecule mimics of tetramate-containi...

journal_title：Future medicinal chemistry

authors： Jeong YC,Moloney MG

更新日期：2015-01-01 00:00:00

abstract：AIM:Management of Type 2 diabetes mellitus by diet is achievable at the early stage of the disease; patients usually underestimate this approach and an appropriate drug therapy is required. RESULTS:Starting from quercetin and oleic acid, that have effect on insulin secretion, a small set of hybrid molecules was synthe...

journal_title：Future medicinal chemistry

authors： Badolato M,Carullo G,Perri M,Cione E,Manetti F,Di Gioia ML,Brizzi A,Caroleo MC,Aiello F

更新日期：2017-10-01 00:00:00

abstract：AIM:Research of the antitumor properties of biscationic compounds has received significant attention over the last few years. RESULTS:A novel family of 1,1'-([2,2'-bipyridine]-5,5'-diylbis(methylene))bis-substituted bromide (9a-k), containing two nitrogen atoms in the linker, considered as hypothetical hydrogen bond a...

journal_title：Future medicinal chemistry

authors： Castro-Navas FF,Schiaffino-Ortega S,Carrasco-Jimenez MP,Ríos-Marco P,Marco C,Espinosa A,Gallo MA,Mariotto E,Basso G,Viola G,Entrena-Guadix A,López-Cara LC

更新日期：2015-01-01 00:00:00

abstract：BACKGROUND:Traditional and current opioid pharmacology is fundamentally based on interactions between opioid receptors and compounds isolated from natural sources. Adverse effects associated with opioids have led to the search for compounds with diminished side effects. DISCUSSION:Recent discoveries of non-nitrogenous...

journal_title：Future medicinal chemistry

authors： Lovell KM,Simpson DS,Cunningham CW,Prisinzano TE

更新日期：2009-05-01 00:00:00

abstract：AIM:Cancer is among the leading causes of death worldwide. Medical interest has focused on macrocyclic polyamines because of their properties as antitumor agents. Results/Methodology: We have designed and synthesized a series of 1,2-diaminocyclohexane derivatives with notable in vitro antiproliferative activities again...

journal_title：Future medicinal chemistry

authors： Morales F,Ramírez A,Morata-Tarifa C,Navarro SA,Marchal JA,Campos JM,Conejo-García A

更新日期：2017-03-01 00:00:00

abstract：:Retinal microvascular alterations have been observed during diabetic retinopathy (DR) due to the retinal susceptibility towards subtle pathological alterations. Therefore, retinal microvascular pathology is essential to understand the nature of retinal degenerations during DR. In this review, the role of retinal micro...

journal_title：Future medicinal chemistry

authors： Barot M,Gokulgandhi MR,Patel S,Mitra AK

更新日期：2013-03-01 00:00:00

abstract：:The cystic fibrosis transmembrane conductance regulator (CFTR) is a cAMP-regulated chloride channel localized primarily at the apical surfaces of epithelial cells lining airway, gut and exocrine glands, where it is responsible for transepithelial salt and water transport. Several human diseases are associated with an ...

journal_title：Future medicinal chemistry

authors： Zhang W,Fujii N,Naren AP

更新日期：2012-03-01 00:00:00

abstract：:The pharmacokinetic treatment strategy targets the drug molecule itself, aiming to reduce drug concentration at the site of action, thereby minimizing any pharmacodynamic effect. This approach might be useful in the treatment of acute drug toxicity/overdose and in the long-term treatment of addiction. Phase IIa contro...

journal_title：Future medicinal chemistry

authors： Gorelick DA

更新日期：2012-02-01 00:00:00

abstract：BACKGROUND:Benzimidazole derivatives are promising compounds for the treatment of parasitic infections. The structure-activity relationships of 91 benzimidazoles with activity against Trichomonas vaginalis and Giardia intestinalis were analyzed using a novel activity landscape modeling approach. RESULTS:We identified ...

journal_title：Future medicinal chemistry

authors： Aguayo-Ortiz R,Pérez-Villanueva J,Hernández-Campos A,Castillo R,Meurice N,Medina-Franco JL

更新日期：2014-03-01 00:00:00

abstract：:New Delhi Metallo β-lactamase-1 (NDM-1) is a member of the Metallo-β-lactamase family, capable of catalyzing the hydrolysis of all β-lactam antibiotics. The rapid dissemination of NDM producers, 'superbugs', has become a worldwide concern to health workers. Seventeen different variants of NDM have been reported so far...

journal_title：Future medicinal chemistry

authors： Khan S,Ali A,Khan AU

更新日期：2018-01-01 00:00:00

abstract：:An accelerated rate of natural-product discovery is critical for the future of ion channel pharmacology. For the full potential of natural products to be realized, an interdisciplinary initiative is required that combines chemical ecology and ion channel physiology. A prime source of future drug leads targeted to ion ...

journal_title：Future medicinal chemistry

authors： Teichert RW,Olivera BM

更新日期：2010-05-01 00:00:00

abstract：:Filamenting temperature-sensitive mutant Z (FtsZ), an essential cell division protein in bacteria, has recently emerged as an important and exploitable antibacterial target. Cytokinesis in bacteria is regulated by the assembly dynamics of this protein, which is ubiquitously present in eubacteria. The perturbation of F...

journal_title：Future medicinal chemistry

authors： Panda D,Bhattacharya D,Gao QH,Oza PM,Lin HY,Hawkins B,Hibbs DE,Groundwater PW

更新日期：2016-06-01 00:00:00

abstract：:With the goal of refining our discovery DMPK workflow, we conducted a retrospective analysis on internal Celgene compounds by calculating the physicochemical properties and gathering data from several assays including solubility, rat and human liver S9 stability, Caco-2 permeability, and rat intravenous (iv.) and oral...

journal_title：Future medicinal chemistry

authors： Kulkarni A,Riggs J,Phan C,Bai A,Calabrese A,Shi T,Moghaddam MF

更新日期：2014-02-01 00:00:00

abstract：:Spinal muscular atrophy (SMA) is an inherited neurodegenerative disease that results in progressive dysfunction of motor neurons of the anterior horn of the spinal cord. SMA is caused by the loss of full-length protein expression from the survival of motor neuron 1 (SMN1) gene. The disease has a unique genetic profile...

journal_title：Future medicinal chemistry

authors： Cherry JJ,Androphy EJ

更新日期：2012-09-01 00:00:00