Abstract:
:This review presents the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment in Cancer facts and figures 2017 American Chemical Society has shown progressive development in fighting cancer. Researchers all over the world in both developed and developing countries are in a continuous effort to tackle this serious concern. Benzimidazole and its derivatives showed a broad range of biological activities due to their resemblance with naturally occurring nitrogenous base i.e. purine. The review discussed benzimidazole derivatives showing anticancer properties through a different mechanism viz. intercalation, alkylating agents, topoisomerases, DHFR enzymes, and tubulin inhibitors. Benzimidazole derivatives act through a different mechanism and the substituents reported from the earlier and recent research articles are prerequisites for the synthesis of targeted based benzimidazole derivatives as anticancer agents. The review focuses on an easy comparison of the substituent essential for potency and selectivity through SAR presented in figures. This will further provide a better outlook or fulfills the challenges faced in the development of novel benzimidazole derivatives as anticancer.
journal_name
Curr Med Chemjournal_title
Current medicinal chemistryauthors
Akhtar MJ,Yar MS,Sharma VK,Khan AA,Ali Z,Haider MDR,Pathak Adoi
10.2174/0929867326666190808122929subject
Has Abstractpub_date
2020-01-01 00:00:00pages
5970-6014issue
35eissn
0929-8673issn
1875-533Xpii
CMC-EPUB-100218journal_volume
27pub_type
杂志文章,评审abstract::Since its discovery in 1995 adiponectin has garnered considerable interest from the academic, clinical and biotech communities due to its proposed salutary anti-inflammatory, anti-diabetic, anti-atherogenic and cardioprotective properties. As a result our appreciation of adiponectin's structure and the importance of p...
journal_title:Current medicinal chemistry
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doi:10.2174/092986712803833155
更新日期:2012-01-01 00:00:00
abstract::Endothelium plays an essential role in human homeostasis by regulating arterial blood pressure, distributing nutrients and hormones as well as providing a smooth surface that modulates coagulation, fibrinolysis and inflammation. Endothelial dysfunction is present in Diabetes Mellitus (DM) and contributes to the develo...
journal_title:Current medicinal chemistry
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abstract::Dimerization and oligomerization of G protein-coupled receptors (GPCRs), proposed almost 30 years ago, have crucial relevance for drug design. Indeed, formation of GPCR oligomers may affect the diversity and performance by which extracellular signals are transferred to G proteins in the process of receptor transductio...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986711797379285
更新日期:2011-01-01 00:00:00
abstract::The hyaluronidases (HAases) are a group of less extensively studied glycosidases distributed throughout the animal kingdom and are popularly known as 'spreading factors'. In recent years, HAases received much attention due to their ability to abruptly alter the hyaluronic acid (HA) homeostasis. HAases preferentially d...
journal_title:Current medicinal chemistry
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abstract::APN is an important zinc dependent metallo-exopeptidase; it has been considered as a suitable target for anti-cancer drug design. In this review we focus on the most effective and the most promising inhibitors of aminopeptidase N. Their binding modes to the enzyme, the attempt to explain the origin of the inhibitory a...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986708786242840
更新日期:2008-01-01 00:00:00
abstract:BACKGROUND:Serotonin reuptake inhibitors (SRIs) and cognitive-behavioral psychotherapy (CBT) are first-line treatments for obsessive-compulsive disorder (OCD). Since response is often inadequate, in recent years researchers investigated whether combining CBT and SRIs, either ab initio or sequentially, results in a grea...
journal_title:Current medicinal chemistry
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abstract::Small conductance Ca(2+)-activated K(+) (SK(Ca)) channels comprise an important subclass of K(+) channels. Selective blockade of SK(Ca) channels may find application in the therapy of myotonic muscular dystrophy, gastrointestinal dysmotilities, memory disorders, narcolepsy, and alcohol abuse. In the cyclophanes descri...
journal_title:Current medicinal chemistry
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abstract:BACKGROUND:During lead identification and optimization, the advancement criteria may be driven based on scientific principles, prior experiences, and/or by examining the path paved by approved drugs. However, accessing the discovery data on physicochemical and ADME properties of the approved kinase inhibitors is a monu...
journal_title:Current medicinal chemistry
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doi:10.2174/0929867324666170523124441
更新日期:2017-01-01 00:00:00
abstract::Non-small cell lung cancer (NSCLC) remains a fatal disease: the majority of patients are diagnosed as having metastases or advanced inoperable tumors. The activity of chemotherapy in NSCLC patients is low with objective response rarely complete and sustained. Cisplatin-based combinations are considered as the standard...
journal_title:Current medicinal chemistry
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更新日期:2002-04-01 00:00:00
abstract::Evidence indicates that nerve gas toxins operate in ways in addition to inhibition of acetylcholine esterase. Alternative bioactivities are discussed with focus on electron transfer. The main class, including pralidoxime (2-PAM), incorporates conjugated iminium and oxime moieties that are electron affinic. Various phy...
journal_title:Current medicinal chemistry
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更新日期:2003-12-01 00:00:00
abstract::In the last decade much attention has been paid to the development of metabolically non-reversible dimeric or hybrid compounds, which combine two structural units of one or two lead compounds of interest for the treatment of Alzheimer's disease. As a consequence of their capability to simultaneously interact with two ...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986706775527974
更新日期:2006-01-01 00:00:00
abstract::Cocaine is one of the most used psychomotor stimulants all over the world. On this basis, the interest for the pharmacological activity and the pharmacodynamic and pharmacokinetic aspects of this drug is very prominent in both clinical and forensic toxicological environments. The review presents and discusses 65 scien...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986712803988794
更新日期:2012-01-01 00:00:00
abstract::Paclitaxel has been proven to be effective against different types of cancer. A delivery system loaded with paclitaxel at tumor site should provide a high local concentration of the drug detrimental to malignant cells, which prevents the re-growth and metastasis of tumor. In this review, paclitaxel formulations for sy...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867043455981
更新日期:2004-02-01 00:00:00
abstract::Similarly to a series of chronic diseases, essential arterial hypertension (HTN) may be manifested during childhood as a blood pressure (BP) reading which repeatedly rises above the 95(th) percentile of population-specific standards. Since BP tends to track along the same percentiles throughout life, children with hig...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867321666140304093848
更新日期:2014-01-01 00:00:00
abstract::The polystyrene-based 2-chlorotrityl resin was originally used in the synthesis of peptides using an Fmoc-amino acid/carboxyl-linked protocol. While traditionally employed to prepare a number of biologically active peptides, the resin has received increasing attention as a support for the synthesis of pseudopeptide an...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/0929867013373192
更新日期:2001-05-01 00:00:00
abstract::More than five decades since the Discovery of Penicillin, the chemistry and biological activity of b-lactams continue to attract the wide spread attention of research workers. Owing to high efficacy and extremely safe toxicological profile, they are agents of choice in the current therapeutic index for the bacterial i...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:
更新日期:1999-03-01 00:00:00
abstract::The therapeutical use of drugs involves the application of dosage forms, serving as carrier systems together with several excipients to deliver the active ingredient to the site of action. Drug delivery technology combines an understanding of medicinal chemistry and pharmacology with the skill of formulation, aiming t...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
doi:10.2174/092986706778201648
更新日期:2006-01-01 00:00:00
abstract::Artificial intelligence methods, in particular, machine learning, has been playing a pivotal role in drug development, from structural design to clinical trial. This approach is harnessing the impact of computer-aided drug discovery thanks to large available data sets for drug candidates and its new and complex manner...
journal_title:Current medicinal chemistry
pub_type: 杂志文章
doi:10.2174/0929867327666201111144048
更新日期:2020-11-11 00:00:00
abstract:OBJECTIVE:We found a novel marine drug, SZ-685C, that was isolated from the secondary metabolites of a mangrove endophytic fungus (No. 1403) collected from the South China Sea, which has been reported to inhibit the proliferation of certain tumor cells. However, its anticancer mechanism remains unknown. The aims of thi...
journal_title:Current medicinal chemistry
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doi:10.2174/0929867311320160007
更新日期:2013-01-01 00:00:00
abstract::Advances in combinatorial chemistry, high-throughput screening, and molecular modeling have revolutionized the process of drug discovery in the pharmaceutical industry. Drug discovery efforts for the primary protozoal parasitic diseases of the developing world, malaria, leishmaniasis, and trypanosomiasis, have also be...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2000-08-01 00:00:00
abstract::In the last decade, drug resistant invasive mycoses have become significantly more common and new antifungal drugs and ways to specifically deliver them to the fungal cell are being looked for. One of the biggest obstacles in finding such comes from the fact that fungi share essential metabolic pathways with humans. O...
journal_title:Current medicinal chemistry
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更新日期:2016-01-01 00:00:00
abstract::Heparanase is an endo-beta-D-glucuronidase that degrades heparan sulfate glycosaminoglycan side chains of the proteoglycans in extracellular matrix and basement membrane. Heparanase enzymatic activity is important in the promotion of tumor angiogenesis, primary tumor growth, invasion, and metastasis. Expression of hep...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2006-01-01 00:00:00
abstract::Nature continues to be the main source of inspiration for synthetic chemists in their quest to make novel conjugates, which can have different physical, biological and medicinal properties. Nature makes these conjugates from mixed biosynthesis and some of these chimeras are found to exhibit unusual biological properti...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:2006-01-01 00:00:00
abstract::Correct QSAR analysis requires reliable measured or calculated logP values, being logP the most frequently utilized and most important physico-chemical parameter in such studies. Since the publication of theoretical fundamentals of logP prediction, many commercial software solutions are available. These programs are a...
journal_title:Current medicinal chemistry
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更新日期:2002-10-01 00:00:00
abstract::Inosine monophosphate dehydrogenase (IMPDH) catalyzes the conversion of IMP to XMP with the concomitant reduction of NAD to NADH. This reaction is the rate-limiting step in guanine nucleotide biosynthesis. IMPDH is a proven target for immunosuppressive, anticancer and antiviral chemotherapy, and may also be a target f...
journal_title:Current medicinal chemistry
pub_type: 杂志文章,评审
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更新日期:1999-07-01 00:00:00
abstract::Some DNA or RNA sequences rich in guanine (G) nucleotides can adopt noncanonical conformations known as G-quadruplexes (G4). In the nuclear genome, G4 motifs have been associated with genome instability and gene expression defects, but they are increasingly recognized to be regulatory structures. Recent studies have r...
journal_title:Current medicinal chemistry
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更新日期:2019-01-01 00:00:00
abstract::The concept of click chemistry represented by the formation of the 1,2,3-triazole core has found wide application in drug discovery, particularly in the early discovery phases and the lead optimization process. 1,2,3-Triazoles ha ve attracted considerable attention in recent years because of their wide range of biolog...
journal_title:Current medicinal chemistry
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更新日期:2015-01-01 00:00:00
abstract::Snakes are fascinating creatures and have been residents of this planet well before ancient humans dwelled the earth. Venomous snakes have been a figure of fear, and cause notable mortality throughout the world. The venom constitutes families of proteins and peptides with various isoforms that make it a cocktail of di...
journal_title:Current medicinal chemistry
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更新日期:2017-01-01 00:00:00
abstract::Recent advances have identified the podocyte as a key target in glomerular injury. The podocyte is a highly specialized cell which is responsible for the glomerular permselectivity for proteins in the kidney. Podocyte injury or loss leads to proteinuria. Apoptosis has been shown to contribute to renal cell loss, inclu...
journal_title:Current medicinal chemistry
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更新日期:2008-01-01 00:00:00
abstract::Atrial fibrillation (AF) and chronic kidney disease (CKD) are disorders with increasing prevalence. The presence of CKD increases the risk of incident AF and vice versa, and the presence of AF may accelerate CKD progression. Nearly a third of patients with established CKD also have AF, whilst half of AF patients may h...
journal_title:Current medicinal chemistry
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更新日期:2016-01-01 00:00:00