Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

A comprehensive review on the biological interest of quinoline and its derivatives.

Benzofuran compounds are a class of compounds that are ubiquitous in nature. Numerous studies have shown that most benzofuran compounds have strong biological activities such as anti-tumor, antibacterial, anti-oxidative, and anti-viral activities. Owing to these biological activities and potential applications in many aspects, benzofuran compounds have attracted more and more attention of chemical and pharmaceutical researchers worldwide, making these substances potential natural drug lead compounds. For example, the recently discovered novel macrocyclic benzofuran compound has anti-hepatitis C virus activity and is expected to be an effective therapeutic drug for hepatitis C disease; novel scaffold compounds of benzothiophene and benzofuran have been developed and utilized as anticancer agents. Novel methods for constructing benzofuran rings have been discovered in recent years. A complex benzofuran derivative is constructed by a unique free radical cyclization cascade, which is an excellent method for the synthesis of a series of difficult-to-prepare polycyclic benzofuran compounds. Another benzofuran ring constructed by proton quantum tunneling has not only fewer side reactions, but also high yield, which is conducive to the construction of complex benzofuran ring systems. This review summarizes the recent studies on the various aspects of benzofuran derivatives including their important natural product sources, biological activities and drug prospects, and chemical synthesis, as well as the relationship between the bioactivities and structures.

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Natural source, bioactivity and synthesis of benzofuran derivatives

Recently, quinoline has become an essential heterocyclic compound due to its versatile applications in the fields of industrial and synthetic organic chemistry. It is a vital scaffold for leads in drug discovery and plays a major role in the field of medicinal chemistry. Nowadays there are plenty of articles reporting syntheses of the main scaffold and its functionalization for biological and pharmaceutical activities. So far, a wide range of synthesis protocols have been reported in the literature for the construction of this scaffold. For example, Gould–Jacob, Friedlander, Pfitzinger, Skraup, Doebner–von Miller and Conrad–Limpach are well-known classical synthesis protocols used up to now for the construction of the principal quinoline scaffold. Transition metal catalysed reactions, metal-free ionic liquid mediated reactions, ultrasound irradiation reactions and green reaction protocols are also useful for the construction and functionalization of this compound. The main part of this review focuses on and highlights the above-mentioned synthesis procedures and findings to tackle the drawbacks of the syntheses and side effects on the environment. Furthermore, various selected quinolines and derivatives with potential biological and pharmaceutical activities will be presented.

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Recent advances in the synthesis of biologically and pharmaceutically active quinoline and its analogues: a review

Design, synthesis, molecular docking and biological activity evaluation of some novel indole derivatives as potent anticancer active agents and apoptosis inducers.

Novel series of heterocycliccompounds pairing hybrids pyrazole, naphthalene and pyrazoline/thiazoldinemoieties were synthesized. The starting compounds pyrazolyl hydrazinecarbothioamidewere synthesized by the reaction of the 4-formyl pyrazole derivatives with thiosemicarbazide to afford the substituted carbothioamide in good yields. The carbothioamideswere used as starting materials for synthesis of a variety of pyrazolylhydrazinylthiazole derivativesandpyrazolylhydrazonothiazolidin derivatives. The structures of the newly synthesized compounds were deduced depending on their spectrum data and elemental analysis. The cytotoxicity of the selected compounds was screened in vitro against three human breast cancer cell lines. The four compounds showed a gradual decrease in cell viability and theonly compound thiazolidin-4-one10b showed IC5010.16, 8.25 and 4.88 μM against the above cell lines, respectively. Thus, it was selected for further in vitro biological investigations. The Structure-activity relationship for these compounds was interpreted in terms of molecular docking. 

Mohamed F. El Shehry

Papers

Design, Synthesis, Cytotoxic Activity and Molecular Docking Studies of Naphthyl Pyrazolyl Thiazole Derivatives as Anticancer Agents