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 human cancer cell lines involving pathways that include microtubule depolarization and tumor vasculature disruption. A chromene analog, Crolibulin™ (EPC2407) is currently in Phase I/II clinical trials for the treatment of advanced solid tumors. This article reviews the general synthesis, biological activities and structure-activity relatinships of different classes of chromenes.
journal_name
Future Med Chemjournal_title
Future medicinal chemistryauthors
Patil SA,Patil R,Pfeffer LM,Miller DDdoi
10.4155/fmc.13.126subject
Has Abstractpub_date
2013-09-01 00:00:00pages
1647-60issue
14eissn
1756-8919issn
1756-8927journal_volume
5pub_type
杂志文章,评审abstract:AIM:The similarity in the biological function of the bioisosteric pair, carboxyl and sulfonamide functional groups, is studied using the quantitative tool, average electron density of the bioisosteric moiety in drug molecules and the qualitative tool, electrostatic potential. Results/methodology: Five different capping...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2017-0136
更新日期:2017-12-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc.13.97
更新日期:2013-07-01 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
pub_type: 杂志文章
doi:10.4155/fmc.10.263
更新日期:2010-12-01 00:00:00
abstract:BACKGROUND:Histone lysine demethylases (KDMs) are well-recognized targets in oncology drug discovery. They function at the post-translation level controlling chromatin conformation and gene transcription. KDM1A is a flavin adenine dinucleotide-dependent amine oxidase, overexpressed in several tumor types, including acu...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2017-0003
更新日期:2017-07-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc.09.112
更新日期:2009-11-01 00:00:00
abstract:BACKGROUND:The understanding of biomolecular interactions ultimately depends on knowledge about the structural and dynamic details of the interacting system. Rational structure-based drug design implements computational methodology in this rationale. DISCUSSION:Together with increasing throughput of structural biology...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.09.7
更新日期:2009-04-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc.11.160
更新日期:2011-12-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc-2018-0586
更新日期:2019-07-01 00:00:00
abstract::Cap analogs are chemically modified derivatives of the unique cap structure present at the 5´ end of all eukaryotic mRNAs and several non-coding RNAs. Until recently, cap analogs have served primarily as tools in the study of RNA metabolism. Continuing advances in our understanding of cap biological functions (includi...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.13.96
更新日期:2013-06-01 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
pub_type: 杂志文章
doi:10.4155/fmc.13.33
更新日期:2013-04-01 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
pub_type: 杂志文章
doi:10.4155/fmc.13.190
更新日期:2014-02-01 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
pub_type: 杂志文章
doi:10.4155/fmc-2017-0098
更新日期:2017-10-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc.09.25
更新日期:2009-06-01 00:00:00
abstract::This perspective explores the origins of both fluorine and medicinal chemistry a century ago and traces the early history of the intersection of these areas and the subsequent roles that fluorine has played in advancing medicinal innovations and diagnoses during the past 60 years. The overview highlights remarkable br...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.09.65
更新日期:2009-08-01 00:00:00
abstract::Despite the wealth of information available for the reverse transcriptase (RT)-associated ribonuclease H (RNaseH) domain of lentiviruses, gammaretroviruses and long terminal repeat containing retrotransposons, exploiting this information in the form of an RNaseH inhibitor with high specificity and low cellular toxicit...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.13.178
更新日期:2013-12-01 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
pub_type: 杂志文章
doi:10.4155/fmc-2017-0154
更新日期:2018-03-01 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
pub_type: 杂志文章
doi:10.4155/fmc-2020-0093
更新日期:2021-01-01 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
pub_type: 杂志文章
doi:10.4155/fmc.10.15
更新日期:2010-04-01 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
pub_type: 杂志文章
doi:10.4155/fmc-2020-0244
更新日期:2020-11-01 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
pub_type: 杂志文章
doi:10.4155/fmc-2016-0156
更新日期:2016-12-01 00:00:00
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journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2018-0438
更新日期:2019-06-01 00:00:00
abstract::Richard H Ebright talks to Rachel Coleby, Commissioning Editor: Ebright is at Rutgers University (New Brunswick, NJ, USA), where he performs research on the structure, mechanism, and regulation of bacterial transcription and on antibacterial drug discovery targeting bacterial transcription. He has received research aw...
journal_title:Future medicinal chemistry
pub_type: 面试
doi:10.4155/fmc-2017-0188
更新日期:2017-10-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc.10.220
更新日期:2010-08-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc-2017-0243
更新日期:2018-04-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc.10.233
更新日期:2010-10-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc.14.28
更新日期:2014-05-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc.12.1
更新日期:2012-03-01 00:00:00
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
pub_type: 杂志文章,评审
doi:10.4155/fmc-2017-0011
更新日期:2017-06-01 00:00:00
abstract::Graphical abstract [Formula: see text]. ...
journal_title:Future medicinal chemistry
pub_type: 社论
doi:10.4155/fmc-2019-0313
更新日期:2020-02-01 00:00:00
abstract::During the current decade, data on the post-translational hydroxylation of specific amino acid residues of some ribosomal proteins and translation factors in both eukaryotes and eubacteria have accumulated. The reaction is catalyzed by dedicated oxygenases (so-called ribosomal oxygenases), whose action is impaired und...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2018-0317
更新日期:2019-02-25 00:00:00