The majority of heterocycle compounds and typically common heterocycle fragments present in most pharmaceuticals currently marketed, alongside with their intrinsic versatility and unique physicochemical properties, have poised them as true cornerstones of medicinal chemistry. Apart from the already marketed drugs, there are many other being investigated for their promising activity against several malignancies. In particular, anticancer research has been capitalizing on the intrinsic versatility and dynamic core scaffold of these compounds. Nevertheless, as for any other promising anticancer drugs, heterocyclic compounds do not come without shortcomings. In this review, we provide for a concise overview of heterocyclic active compounds and families and their main applications in medicine. We shall focus on those suitable for cancer therapy while simultaneously addressing main biochemical modes of action, biological targets, structure-activity relationships as well as intrinsic limitation issues in the use of these compounds. Finally, considering the advent of nanotechnology for effective selective targeting of drugs, we shall discuss fundamental aspects and considerations on nanovectorization of such compounds that may improve pharmacokinetic/pharmacodynamic properties of heterocycles.

/pdf/heterocyclic-anticancer-compounds-recent-advances-and-the-4fi53ej151.pdf

Heterocyclic Anticancer Compounds: Recent Advances and the Paradigm Shift towards the Use of Nanomedicine's Tool Box.

Indole: A privileged scaffold for the design of anti-cancer agents.

proceedings, in not being up-to-date. There are almost no references to papers later than 1990, except for some self-citations which extend to 1991. In addition to well known major contributors to the field of metastasis, research participants were also drawn from laboratories in Continental Europe, which are not frequently represented at Symposia of this type. Some of the papers are general overviews, while others report the Authors own studies in detail. On the whole the various contributions are rather disparate, but occasionally authors compare and contrast a related phenomenon. An example is the role of the CD-44, a transmembrane protein involved in lymphocyte transport, for which the group of Herrlich (Karlsruhe, Germany) have obtained convincing evidence of a role in metastasis. On the other hand, I.R. Hart (London, UK) described studies involving a panel of melanoma cells in which no evidence for a direct involvement of CD-44 in metastasis was found. The subject matter is divided into the following sections: The first section has papers dealing with the role of ras oncogenes and bladder carcinoma and the initial steps in cancer dissemination of rat bladder carcinoma. These raise questions without providing any answers. The second section is concerned principally with cell adhesion and highlights complexity and conflicting results. In the third section the discussion of angiogenesis is disappointing and work is reported from investigators who are not prominent in the area. There is, however, a very valuable chapter from L. Weiss (Buffalo, New York). He analyses, in detail, a mechanism for the destruction of cancer cells in the microvasculature based on deformation. Weiss' data for the destruction of cancer cells when trapped in capillaries has long been a key observation in the field of blood-borne metastatic spread. It leads to the concept of metastatic inefficiency which is so evident when the relative infrequency of metastasis is compared with the number of cancer cells shed into the circulation. Weiss' suggestion as to how this destruction occurs is compelling and he provides most interesting new data which indicates that treatment of cells with doxorubicin increases biomechanical destruction. In the section on melanoma there are two rather unconvincing contributions on metastasis-associated surface molecules, in addition to the critical analysis of the role of CD-44 to which reference has already been made. The last two sections contain a mixture of topics and on the whole are of little interest. Immunotherapy with autologous tumour 'vaccines' …

Protein Kinase C

Indole in the target-based design of anticancer agents: A versatile scaffold with diverse mechanisms.

Background Cancer is spreading all over the world, and it is becoming the leading cause of major deaths. Today's most difficult task for every researcher is to invent a new drug that can treat cancer with minimal side effects. Many factors, including pollution, modern lifestyle and food habits, exposure to oncogenic agents or radiations, enhanced industrialization, etc. can cause cancer. Treatment of cancer is done by various methods that include chemotherapy, radiotherapy, surgery and immunotherapy in combination or singly along with kinase inhibitors. Most of the anti-cancer drugs use the concept of kinase inhibition. Objective The number of drugs being used in chemotherapy has heterocycles as their basic structure in spite of various side effects. Medicinal chemists are focusing on nitrogen-containing heterocyclic compounds like pyrrole, pyrrolidine, pyridine, imidazole, pyrimidines, pyrazole, indole, quinoline, oxadiazole, azole, benzimidazole, etc. as the key building blocks to develop active biological compounds. The aim of this study is to attempt to compile a dataset of nitrogen-containing heterocyclic anti-cancer drugs. Methods We adopted a structural search on notorious journal publication websites and electronic databases such as Bentham Science, Science Direct, PubMed, Scopus, USFDA, etc. for the collection of peer-reviewed research and review articles for the present review. The quality papers were retrieved, studied, categorized into different sections, analyzed and used for article writing. Conclusion As per FDA databases, nitrogen-based heterocycles in the drug design are almost 60% of unique small-molecule drugs. Some of the nitrogen-containing heterocyclic anti-cancer drugs are Axitinib, Bosutinib, Cediranib, Dasatanib (Sprycel®), Erlotinib (Tarceva®), Gefitinib (Iressa®), Imatinib (Gleevec®), Lapatinib (Tykerb ®), Linifanib, Sorafenib (Nexavar®), Sunitinib (Sutent®), Tivozanib, etc. In the present review, we shall focus on the overview of nitrogen-containing heterocyclic active compounds as anti-cancer agents.

Nitrogen-Containing Heterocycles as Anticancer Agents: An Overview.

http://clok.uclan.ac.uk/12392/1/__lha-014_pers-J_00051247_My%20Documents_Publications_2014_Chris%20Sherer%20review_To%20Send_Response%20to%20referees_Sherer_Snape%20MS_Amended_ii.pdf

Heterocyclic scaffolds as promising anticancer agents against tumours of the central nervous system: Exploring the scope of indole and carbazole derivatives.

Heterocyclic Scaffolds as Promising Anticancer Agents Against Tumors of the Central Nervous System: Exploring the Scope of Indole and Carbazole Derivatives

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Heterocyclic scaffolds as promising anticancer agents against tumours of the central nervous system: Exploring the scope of indole and carbazole derivatives.

Heterocyclic Scaffolds as Promising Anticancer Agents Against Tumors of the Central Nervous System: Exploring the Scope of Indole and Carbazole Derivatives