Replacing sulfa drugs with novel DHPS inhibitors.

abstract：:Radiation-induced lung injury (RILI) is a common complication in cancer patients receiving local thoracic radiation and bone marrow transplantation conditioning. It is divided into early-stage radiation pneumonitis and advanced radiation fibrosis of the lung. This severely hampers the quality of life and survival of c...

journal_title：Future medicinal chemistry

authors： Xia C,Shi W,Zhang Y,Ding L,Gao L,Wang Q,Shao L,Dong L,Gao Y

更新日期：2020-12-01 00:00:00

abstract：:Nicotinic receptors are membrane proteins involved in several physiological processes. They are considered suitable drug targets for various CNS disorders or conditions, as shown by the large number of compounds which have entered clinical trials. In recent years, nonconventional agonists have been discovered: positiv...

journal_title：Future medicinal chemistry

authors： Manetti D,Bellucci C,Chiaramonte N,Dei S,Teodori E,Romanelli MN

更新日期：2018-02-01 00:00:00

abstract：AIM:Confirm the use of Plectanthus spp. plants in traditional medicine, particularly as anti-inflammatory and anti-infective agents. MATERIALS & METHODS:Compounds previously isolated from Plectranthus spp. were studied for their anti-inflammatory activity using the SNAP assay and RAW 264.7 cells, by the quantification...

journal_title：Future medicinal chemistry

authors： Andrade JM,Custódio L,Romagnoli A,Reis CP,Rodrigues MJ,Garcia C,Petruccioli E,Goletti D,Faustino C,Fimia GM,Rijo P

更新日期：2018-07-01 00:00:00

abstract：:Structure-based virtual screening makes explicit or implicit use of 3D target structure information to detect novel active compounds. Results of nearly 300 currently available original applications have been analyzed to characterize the state-of-the-art in this field. Compound selection from docking calculations is mu...

journal_title：Future medicinal chemistry

authors： Ripphausen P,Stumpfe D,Bajorath J

更新日期：2012-04-01 00:00:00

abstract：AIM:The design and synthesis of chromenopyrimidines as microtubule destabilizing agents. MATERIALS & METHODS:Novel chromenopyrimidines and chromenotriazolopyrimidines were prepared and evaluated for their cytotoxicity against MCF-7 cell line. The most potent compound was tested for its possible effect on tubulin inhib...

journal_title：Future medicinal chemistry

authors： El-Bakhshawangy NM,El-Nassan HB,Kassab AE,Taher AT

更新日期：2018-06-01 00:00:00

abstract：:The use of electron density-based molecular descriptors in drug research, particularly in quantitative structure--activity relationships/quantitative structure--property relationships studies, is reviewed. The exposition starts by a discussion of molecular similarity and transferability in terms of the underlying elec...

journal_title：Future medicinal chemistry

authors： Matta CF,Arabi AA

更新日期：2011-06-01 00:00:00

abstract：:Matrix metalloproteinases are zinc-dependent enzymes whose main function is to cleave the components of the extracellular matrix. Their overexpression is evident in all cancers but to date there is no satisfactory way to inhibit their actions. Here, we look at their types, their structures, their functions and the dev...

journal_title：Future medicinal chemistry

authors： King SE

更新日期：2016-01-01 00:00:00

abstract：:Diabetes mellitus is an increasing public health problem in the world. Type 2 diabetes is the most common type of diabetes whose complications contribute to its high death rate. It seriously impacts healthcare systems and patients' quality of life. Therefore, effective measures and new treatment strategies are needed ...

journal_title：Future medicinal chemistry

authors： Turdu G,Gao H,Jiang Y,Kabas M

更新日期：2018-05-01 00:00:00

abstract：AIM:Alzheimer's disease is a progressive and neurodegenerative disorder of the CNS, affecting elderly people. The current pharmacological approach is based on the improvement of cholinergic neurotransmission by inhibiting acetylcholinesterase (AChE) with AChE inhibitors. The disease is also characterized by the acceler...

journal_title：Future medicinal chemistry

authors： de Almeida JR,Figueiro M,Almeida WP,de Paula da Silva CHT

更新日期：2018-05-01 00:00:00

abstract：:Dextran has become a hot research topic in drug vehicle material because of its biodegradable, nonspecific cell adhesion, resistance to protein adsorption, low price and ease of structural modification. The fate and changes of dextran in vivo are not fully understood. It is helpful to guide the design and modification...

journal_title：Future medicinal chemistry

authors： Huang S,Huang G

更新日期：2019-07-01 00:00:00

abstract：BACKGROUND:The objective of this study was to develop and evaluate a more effective mucoadhesive thiomer for buccal drug-delivery systems. METHODS:2-iminothiolane was covalently attached to a chitosan backbone. A preactivation step followed, mediated by 6,6´dithionicotinamide, thiol groups were modified by disulfide b...

journal_title：Future medicinal chemistry

authors： Laffleur F,Shahnaz G,Islambulchilar Z,Bernkop-Schnürch A

更新日期：2013-04-01 00:00:00

abstract：AIM:The present study was carried out to assess a new series of triazoloquinazolines 1-40 for their antioxidant activities using 1,1-diphenyl-2-picryl hydrazyl radical scavenging, ferric reduction antioxidant power and reducing power capability assays. RESULTS:All triazoloquinazolines 1-40 exhibited antioxidant activi...

journal_title：Future medicinal chemistry

authors： Al-Salahi R,Anouar EH,Marzouk M,Taie HA,Abuelizz HA

更新日期：2018-02-01 00:00:00

abstract：:Since the Hedgehog signaling pathway has been associated with cancer, it has emerged as a therapeutic target for cancer therapy. The main target among the key Hedgehog proteins is the GPCR-like Smo receptor. Therefore, some Smo antagonists that have entered clinical trials, including the US FDA-approved drugs vismodeg...

journal_title：Future medicinal chemistry

authors： Espinosa-Bustos C,Mella J,Soto-Delgado J,Salas CO

更新日期：2019-03-01 00:00:00

abstract：AIM:Triterpenes are natural compounds, whose wide biological activity predestines them for application as promising new chemotherapeutics. In this paper, we report the results of our investigations into the substitution of oleanolic acid with aromatic and nitroaromatic moieties acting as bioreducing agents. RESULTS:Th...

journal_title：Future medicinal chemistry

authors： Bednarczyk-Cwynar B,Ruszkowski P,Jarosz T,Krukiewicz K

更新日期：2018-03-01 00:00:00

abstract：:Since their initial isolation from the marine alga Delisea pulchra, bromofuranones have been investigated as potential inhibitors of quorum sensing (QS) in various bacterial strains. QS is an important mechanism by which bacteria co-ordinate their molecular response to the environment. QS is intrinsically linked to ba...

journal_title：Future medicinal chemistry

authors： Lyons T,Gahan CG,O'Sullivan TP

更新日期：2020-11-01 00:00:00

abstract：:Epigallocatechin gallate (EGCG), one of polyphenols isolated from green tea, exhibits biology-benefiting effects with minimum severe adverse. EGCG is known to be a mitochondrion-targeting medicinal agent, regulating mitochondrial metabolism, including mitochondrial biogenesis, mitochondrial bioenergetics, and mitochon...

journal_title：Future medicinal chemistry

authors： Shi W,Li L,Ding Y,Yang K,Chen Z,Fan X,Jiang S,Guan Y,Liu Z,Xu D,Wu L

更新日期：2018-04-01 00:00:00

abstract：:Background: Angiotensin II receptor blockers were designed as therapeutic agents to block the binding site of the angiotensin II receptor type 1 (AT1R). Methodology: The structure of telmisartan was modified by coordination to the biometal Zn(II), resulting in the compound ZnTelm. Its antihypertensive activity and cel...

journal_title：Future medicinal chemistry

authors： Martínez VR,Aguirre MV,Todaro JS,Lima AM,Stergiopulos N,Ferrer EG,Williams PA

更新日期：2021-01-01 00:00:00

abstract：:At present, the polysaccharide antitumor research is focused on how to further improve the antitumor activity of polysaccharides. The structural modification of polysaccharides can enhance their antitumor activity to a certain extent. The antitumor mechanisms of polysaccharide derivatives mainly contain the inducing a...

journal_title：Future medicinal chemistry

authors： Huang G,Huang H

更新日期：2017-10-01 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：:In comparison with other virus infections, such as HIV, HBV, HCV, influenza and herpes virus, dengue virus infections have received relatively little attention from a (chemo)therapeutic viewpoint, despite their global incidence (2.5 billion people estimated to be at risk) and absence of an effective prophylactic measu...

journal_title：Future medicinal chemistry

authors： De Clercq E

更新日期：2010-04-01 00:00:00

abstract：:Kinetic and thermodynamic ligand-protein binding parameters are gaining growing importance as key information to consider in drug discovery. The determination of the molecular structures, using particularly x-ray and NMR techniques, is crucial for understanding how a ligand recognizes its target in the final binding c...

journal_title：Future medicinal chemistry

authors： Deganutti G,Moro S

更新日期：2017-04-01 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：:Chemokines and their receptors are integral components of the immune response, regulating lymphocyte development, homing and trafficking, and playing a key role in the pathophysiology of many diseases. Chemokine receptors have, therefore, become the target for both small-molecule, peptide and antibody therapeutics. Ch...

journal_title：Future medicinal chemistry

authors： Fricker SP,Metz M

更新日期：2014-01-01 00:00:00

abstract：:Aim: Eight coumarin derivatives (1a-h) obtained from natural (-)-mammea A/BB (1) and 13 synthetic coumarins (2-14) had their cytotoxicity and biological activity evaluated against Mycobacterium tuberculosis H37Rv reference strain and multidrug-resistant clinical isolates. Materials & methods: Anti-M. tuberculosis acti...

journal_title：Future medicinal chemistry

authors： Pires CT,Scodro RB,Cortez DA,Brenzan MA,Siqueira VL,Caleffi-Ferracioli KR,Vieira LC,Monteiro JL,Corrêa AG,Cardoso RF

更新日期：2020-09-01 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：:Aim: The explosion of data based technology has accelerated pattern mining. However, it is clear that quality and bias of data impacts all machine learning and modeling. Results & methodology: A technique is presented for using the distribution of first significant digits of medicinal chemistry features: logP, logS, a...

journal_title：Future medicinal chemistry

authors： García-Sosa AT

更新日期：2019-09-01 00:00:00

abstract：AIM:The undeniable indomethacin potency has always suffered serious obstacles such as gastric damage. Continuous attempts to develop potent yet safe indomethacin analogs have never ceased. RESULTS:Herein are new indole derivatives 4a-h and 5a-c, which were synthesized via Fisher indole reaction, evaluated for both the...

journal_title：Future medicinal chemistry

authors： Amin NH,El-Saadi MT,Hefny AA,Abdelazeem AH,Elshemy HA,Abdellatif KR

更新日期：2018-12-06 00:00:00

abstract：AIM:The assumption in scaffold hopping is that changing the scaffold does not change the binding mode and the same structure-activity relationships (SARs) are seen for substituents decorating each scaffold. Results/methodology: We present the use of matched series analysis, an extension of matched molecular pair analys...

journal_title：Future medicinal chemistry

authors： Hunt P,Segall M,O'Boyle N,Sayle R

更新日期：2017-01-01 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：:The pharmaceutical industry is facing numerous, well-documented challenges - from the effects of patent expirations to high attrition rates in the drug-development pipeline. Future Medicinal Chemistry has invited a group of leaders from academia and industry to express their views on where the industry is heading and ...

journal_title：Future medicinal chemistry

authors： Cottens S,Eaton M,Fuhr J,Geary S,Johnson DS,Li G,Raveglia L,Robertson GM,Westwell A

更新日期：2011-11-01 00:00:00