Recent progress for the synthesis of selected carbocyclic nucleosides.

abstract：:The EGFR is one of the most popular targets for anticancer therapies and many drugs, such as erlotinib and gefitinib, have got enormous success in clinical treatments of cancer in past decade. However, the efficacy of these agents is often limited because of the quick emergence of drug resistance. Fundamental structur...

journal_title：Future medicinal chemistry

authors： Guan H,Du Y,Ning Y,Cao X

更新日期：2017-05-01 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：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：BACKGROUND:Due to the complex nature of Alzheimer's disease, there is a renewed and growing search for multitarget drugs. RESULTS:Donepezil-ferulic acid hybrids (DFAHs) were prepared by the one-pot Ugi-4CR in low-to-moderate yields. DFAHs are potent antioxidant agents, showing oxygen radical absorbance capacity values...

journal_title：Future medicinal chemistry

authors： Benchekroun M,Ismaili L,Pudlo M,Luzet V,Gharbi T,Refouvelet B,Marco-Contelles J

更新日期：2015-01-01 00:00:00

abstract：:Camellia oleifera Abel is a member of Camellia, and its seeds are used to extract Camellia oil, which is generally used as cooking oil in the south of China. Camellia oil consists of unsaturated fatty acids, tea polyphenol, squalene, saponin, carrot element and vitamins, etc. The seed remains after oil extraction of C...

journal_title：Future medicinal chemistry

authors： Xiao X,He L,Chen Y,Wu L,Wang L,Liu Z

更新日期：2017-11-01 00:00:00

abstract：:This review aims to bring the reader up to date with the more recent ruthenium compounds that have been synthesized and tested for their cytotoxicity. The chemistry of these transition metal complexes will be introduced and the basic principles that govern their common behavior outlined. The recent history of establis...

journal_title：Future medicinal chemistry

authors： Page SM,Boss SR,Barker PD

更新日期：2009-06-01 00:00:00

abstract：AIM:There is little information available on the monoamine oxidase isoform selectivity of N-alkyl harmine analogs, which exhibit a myriad of activities including MAO-A, DYRK1A and cytotoxicity to several select cancer cell lines. RESULTS:Compounds 3e and 4c exhibited an IC50 of 0.83 ± 0.03 and 0.43 ± 0.002 μM against ...

journal_title：Future medicinal chemistry

authors： Haider S,Alhusban M,Chaurasiya ND,Tekwani BL,Chittiboyina AG,Khan IA

更新日期：2018-06-01 00:00:00

abstract：:More research effort needs to be invested in antimicrobial drug development to address the increasing threat of multidrug-resistant organisms. The enzyme DHPS has been a validated drug target for over 70 years as the target for the highly successful sulfa drugs. The use of sulfa drugs has been compromised by the wides...

journal_title：Future medicinal chemistry

authors： Hammoudeh DI,Zhao Y,White SW,Lee RE

更新日期：2013-07-01 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：:Bromodomain and extra-terminal domain (BET) protein family plays an important role in regulating gene transcription preferentially at super-enhancer regions and has been involved with several types of cancers as a candidate. Up to now, there are 16 pan-BET inhibitors in clinical trials, however, most of them have unde...

journal_title：Future medicinal chemistry

authors： Yang Y,Wu Z,Chen P,Zheng P,Zhang H,Zhou J

更新日期：2020-09-01 00:00:00

abstract：:The emergence of multidrug-resistant Mycobacterium tuberculosis strains has made many of the currently available anti-tuberculosis (TB) drugs ineffective. Accordingly, there is a pressing need to identify new drug targets. Filamentous temperature-sensitive protein Z (FtsZ), a bacterial tubulin homologue, is an essenti...

journal_title：Future medicinal chemistry

authors： Kumar K,Awasthi D,Berger WT,Tonge PJ,Slayden RA,Ojima I

更新日期：2010-08-01 00:00:00

abstract：:Cyclin-dependent kinase 7 (CDK7) plays crucial roles in the regulation of cell cycle and transcription that are tightly associated with cancer development and metastasis. The recent identification of the first covalent inhibitor which possesses high specificity against CDK7 prompts intense studies on designing highly ...

journal_title：Future medicinal chemistry

authors： Wang M,Wang T,Zhang X,Wu X,Jiang S

更新日期：2020-05-01 00:00:00

abstract：AIM:To synthesize the new bioactive metabolites of mosapride (R)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]-propyl-5-chlorine-4-amino-2-ethoxyben-zamide (R-isomer) and (S)-N-[2-hydroxy-3-(4-fluorobenzyl)amino]-propyl-5-chlorine-4-amino-2-ethoxybenzamide (S-isomer) and evaluate their in vitro and in vivo pharmacological and ...

journal_title：Future medicinal chemistry

authors： Yao J,Li K,Song Y,He Z,Liu Z,Zhao L,Wang S

更新日期：2019-01-01 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：:Computer-aided drug design (CADD) methodologies have made great advances and contributed significantly to the discovery and/or optimization of many clinically used drugs in recent years. CADD tools have likewise been applied to the discovery of inhibitors of HIV-1 integrase, a difficult and worthwhile target for the d...

journal_title：Future medicinal chemistry

authors： Liao C,Nicklaus MC

更新日期：2010-07-01 00:00:00

abstract：:Prodrug entrapment into nanocarriers for tumor delivery is a strategy to achieve a valid therapy with high efficiency. The prodrug contains anticancer agents conjugating with functional moieties or ligands so that the active component is released after metabolism in the body or tumor. The advantages of nanosystems for...

journal_title：Future medicinal chemistry

authors： Lin MH,Hung CF,Hsu CY,Lin ZC,Fang JY

更新日期：2019-08-01 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：BACKGROUND:GABA derivatives are important for the development of drugs for disorders of the CNS and PNS. RESULTS:We describe a simple synthesis of N-benzyl γ-phenyl-γ-aminobutyric acids, via the reductive amination of the corresponding γ-keto acids with benzylamines using ammonia borane. CONCLUSION:This procedure pro...

journal_title：Future medicinal chemistry

authors： Ramachandran PV,Sakavuyi K,Mistry H

更新日期：2011-02-01 00:00:00

abstract：AIM:The pharmacotherapy of inflammatory bowel disease is difficult and currently available treatments bring mostly poor and unsatisfactory results. RESULTS:The purpose of this work was the synthesis of opiorphin, sialorphin, spinorphin and a series of their analogs and the in vitro characterization of their effect on ...

journal_title：Future medicinal chemistry

authors： Kamysz E,Sałaga M,Sobocińska M,Giełdoń A,Fichna J

更新日期：2016-12-01 00:00:00

abstract：:Carbonic anhydrases (CAs; EC 4.2.1.1) are well known zinc metalloproteins involved in the catalysis of a very simple but essential physiological reaction: carbon dioxide hydration to bicarbonate and proton. These enzymes are of clinical relevance in cancer therapy as among the 15 isoforms known in humans, two cell sur...

journal_title：Future medicinal chemistry

authors： Supuran CT,Winum JY

更新日期：2015-01-01 00:00:00

abstract：:The last 10 years have seen advances in automation and high-throughput biochemistry in the drug-discovery arena. However, these advances have not led to improvements in drug-discovery success. Drug programs must find new ways to identify superior compounds. Advances in label-free assay technologies may provide advanta...

journal_title：Future medicinal chemistry

authors： Lunn CA

更新日期：2010-11-01 00:00:00

abstract：:Several hundred genes associated or linked to obesity have been described in the scientific literature. Whereas many of these genes are potential targets for the treatment of obesity and associated conditions, none of them have permitted the developement of an efficient drug therapy. As proposed by the 'thrifty genoty...

journal_title：Future medicinal chemistry

authors： Braud S,Ciufolini M,Harosh I

更新日期：2010-12-01 00:00:00

abstract：AIM:Antibiotic resistance has become a major health problem. The σ(70):core interface of bacterial RNA polymerase is a promising drug target. Recently, the coiled-coil and lid-rudder-system of the β' subunit has been identified as an inhibition hot spot. Materials & methods & Results: By using surface plasmon resonance...

journal_title：Future medicinal chemistry

authors： Hüsecken K,Hinsberger S,Elgaher WA,Haupenthal J,Hartmann RW

更新日期：2014-09-01 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：AIM:Currently, dozens of BRAF inhibitors and MEK inhibitors targeting RAF-MEK-ERK pathway have been introduced into clinical trials for cancer therapy. However, after 6-8 months of initial response, acquired drug resistance among the majority of those treated patients sharply diminished their clinical efficacy. DISCUS...

journal_title：Future medicinal chemistry

authors： Yu Z,Ye S,Hu G,Lv M,Tu Z,Zhou K,Li Q

更新日期：2015-01-01 00:00:00

abstract：:Many natural products that consist of quinoline core are found to be bioactive and the versatility of quinoline and its derivatives have attracted great attention in the field of drug development. As a result, in recent years, many green and sustainable synthetic approaches for the synthesis of structurally diverse qu...

journal_title：Future medicinal chemistry

authors： Chung PY,Bian ZX,Pun HY,Chan D,Chan AS,Chui CH,Tang JC,Lam KH

更新日期：2015-01-01 00:00:00

abstract：:Graphical abstract [Formula: see text]. ...

journal_title：Future medicinal chemistry

authors： Choudhary S,Silakari O

更新日期：2020-02-01 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：:Chronic pain is one of the most ubiquitous diseases in the world, but treatment is difficult with conventional methods, due to undesirable side effects of treatments and unknown mechanisms of pathological pain states. The endogenous peptide, dynorphin A has long been established as a target for the treatment of pain. ...

journal_title：Future medicinal chemistry

authors： Hall SM,Lee YS,Hruby VJ

更新日期：2016-01-01 00:00:00

abstract：:Platinum-based anticancer agents have been widely used in the clinic to successfully treat many different types of cancer. However, the therapeutic efficacy of platinum drugs is limited by serious side effects and the occurrence of inherent or acquired resistance of tumor cells. Nanoparticulate drug-delivery systems h...

journal_title：Future medicinal chemistry

authors： Bryde S,de Kroon AI

更新日期：2009-11-01 00:00:00