Indole molecules as inhibitors of tubulin polymerization: potential new anticancer agents.

abstract：:Mitochondria play a key role in ATP generation, redox homeostasis and regulation of apoptosis. Due to the essential role of mitochondria in metabolism and cell survival, targeting mitochondria in cancer cells is considered as an attractive therapeutic strategy. However, metabolic flexibility in cancer cells may enable...

journal_title：Future medicinal chemistry

authors： Cui Q,Wen S,Huang P

更新日期：2017-06-01 00:00:00

abstract：:Immunoadjuvant Quillaja spp. tree saponins stimulate both cellular and humoral responses, significantly widening vaccine target pathogen spectra. Host toxicity of specific saponins, fractions and extracts may be rather low and further reduced using lipid-based delivery systems. Saponins contain a hydrophobic central a...

journal_title：Future medicinal chemistry

authors： Magedans YV,Yendo AC,Costa F,Gosmann G,Fett-Neto AG

更新日期：2019-06-01 00:00:00

abstract：:Chronic obstructive pulmonary disease (COPD) is one of the leading causes of death in the world today. Bronchodilators, particularly muscarinic antagonists and β(2) agonists, are recommended for patients with moderate to severe COPD. Dual-pharmacology muscarinic antagonist- β(2) agonist (MABA) molecules present an exc...

journal_title：Future medicinal chemistry

authors： Hughes AD,Jones LH

更新日期：2011-10-01 00:00:00

abstract：:Epothilone is a newly developed antitumor drug; its antitumor principle is to stop the cell cycle by binding to tubulin in tumor cells, promoting tubulin polymerization, inhibiting depolymerization of microtubules, and ultimately inducing apoptosis. There are many analogs of epothilone, such as epothilone B, epothilon...

journal_title：Future medicinal chemistry

authors： Cheng H,Huang G

更新日期：2018-06-01 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：:Due to the impermeable structure and barrier function of the blood-brain barrier (BBB), the delivery of therapeutic molecules into the CNS is extremely limited. Nanodelivery systems are regarded as the most effective and versatile carriers for the CNS, as they can transport cargo molecules across the BBB via various m...

journal_title：Future medicinal chemistry

authors： Kim KT,Lee HS,Lee JJ,Park EK,Lee BS,Lee JY,Bae JS

更新日期：2018-11-01 00:00:00

abstract：:Micro-organisms express a wide range of transmembrane pumps known as multidrug efflux pumps that improve the micro-organism's ability to survive in severe environments and contribute to resistance against antibiotic and antimicrobial agents. There is significant interest in developing efflux inhibitors as an adjunct t...

journal_title：Future medicinal chemistry

authors： Jamshidi S,Sutton JM,Rahman KM

更新日期：2016-01-01 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 synthesize novel antiproliferative agents. Results & methodology: A variety of 1,4-pentadien-3-one derivatives bearing quinoxaline scaffolds was designed and synthesized and their antiproliferative activities were evaluated. Notably, compounds N3 and N4 exhibited markedly greater antiproliferative activities a...

journal_title：Future medicinal chemistry

authors： Tang X,He J,Li Q,Tang X,Chen M,Hao G,Huai Z,Huang Y,Xue W

更新日期：2020-08-01 00:00:00

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：: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：: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：:This review summarizes the basic milestones of the research of 5-azacytosine nucleosides chronologically from their discovery and anticancer activity identification, through to subsequent unveiling of their mechanism of action based on DNA hypomethylation and tumor-suppressor gene reactivation, to the final US FDA app...

journal_title：Future medicinal chemistry

authors： Krečmerová M,Otmar M

更新日期：2012-05-01 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：:The design of a high-quality screening collection is of utmost importance for the early drug-discovery process and provides, in combination with high-quality assay systems, the foundation of future discoveries. Herein, we review recent trends and observations to successfully expand the access to bioactive chemical spa...

journal_title：Future medicinal chemistry

authors： Renner S,Popov M,Schuffenhauer A,Roth HJ,Breitenstein W,Marzinzik A,Lewis I,Krastel P,Nigsch F,Jenkins J,Jacoby E

更新日期：2011-04-01 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：: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：: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：: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：:Mammalian target of rapamycin (mTOR) belongs to the atypical kinase family of phosphatidylinositol-3-kinase-related kinase and function as a master regulators of the switch between catabolic and anabolic metabolism. In the last decade mTOR has emerged as a therapeutic target for various diseases such as cancer, inflam...

journal_title：Future medicinal chemistry

authors： Roychowdhury A,Sharma R,Kumar S

更新日期：2010-10-01 00:00:00

abstract：:Background: Andrographolide and its benzylidene derivatives, SRJ09 and SRJ23, potentially bind oncogenic K-Ras to exert anticancer activity. Their molecular interactions with K-Ras oncoproteins that lead to effective biological activity are of major interest. Methods & results:In silico docking and molecular dynamics ...

journal_title：Future medicinal chemistry

authors： Quah SY,Tan MS,Ho KL,Manan NA,Gorfe AA,Deb PK,Sagineedu SR,Stanslas J

更新日期：2020-09-01 00:00:00

abstract：AIM:Tuberculosis is responsible for 9.6 million infections and 1.5 million deaths in 2015. The development of multidrug-resistant and extensively drug-resistant strains has impeded the development of effective antitubercular therapy. Results/methodology: The present manuscript describes the synthesis of a series of 4-a...

journal_title：Future medicinal chemistry

authors： Singh A,Viljoen A,Kremer L,Kumar V

更新日期：2017-10-01 00:00:00

abstract：:Mammalian carbonic anhydrases (CAs; EC 4.2.1.1) of which 16 isoforms are known, are involved in important physiological functions. Their inhibition is exploited pharmacologically for the treatment of many diseases (glaucoma, edema, epilepsy, obesity, hypoxic tumors, neuropathic pain, etc.) but the activators were less...

journal_title：Future medicinal chemistry

authors： Supuran CT

更新日期：2018-03-01 00:00:00

abstract：BACKGROUND:Due to the complex etiology of neurodegenerative diseases, there is growing interest in multitarget drugs. In this study we synthesized and evaluated a new series of compounds, with benzo[f]coumarin structure, as potential inhibitors of MAO-A, MAO-B, AChE and BuChE. RESULTS:In vitro studies show that most o...

journal_title：Future medicinal chemistry

authors： Matos MJ,Janeiro P,González Franco RM,Vilar S,Tatonetti NP,Santana L,Uriarte E,Borges F,Fontenla JA,Viña D

更新日期：2014-03-01 00:00:00

abstract：:Responsive optical probes play a vital role in following and understanding biological events. In this review, we focus on the use of lanthanide complexes as molecular probes, as they offer many advantages in imaging and assays, particularly when used in time-gated protocols. We describe systems that illustrate the key...

journal_title：Future medicinal chemistry

authors： Allain C,Faulkner S

更新日期：2010-03-01 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：: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：: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

abstract：:As has been widely reviewed elsewhere, the pharmaceutical industry is experiencing an 'innovation deficit' as evidenced by the decline in new chemical entity output. This decline, compounded by increased costs and regulatory requirements highlights the need to significantly revise strategic options across the drug-dis...

journal_title：Future medicinal chemistry

authors： Robertson GM,Mayr LM

更新日期：2011-12-01 00:00:00

abstract：:The DNA repair protein, O6-methylguanine DNA methyltransferase (MGMT), can confer resistance to guanine O6-alkylating agents. Therefore, inhibition of resistant MGMT protein is a practical approach to increase the anticancer effects of such alkylating agents. Numerous small molecule inhibitors were synthesized and exh...

journal_title：Future medicinal chemistry

authors： Sun G,Zhao L,Zhong R,Peng Y

更新日期：2018-08-01 00:00:00