Review on Isatin- A Remarkable Scaffold for Designing Potential Therapeutic Complexes and Its Macrocyclic Complexes with Transition Metals.

Role of synthetic coordination chemistry in pharmaceutical science is expeditiously increased due to its sundry relevances in this field. The present review endows the synthesized macrocyclic complexes of transition metal ions containing isatin and its derivatives as ligand precursors, their characterization and their copious pharmaceutical applications. Isatin (1H-Indole-2,3-dione) is a protean compound (presence of lactam and keto moiety permits to change its molecular framework) that can be obtained from marine animals, plants, and is also found in mammalian tissues and in human fluids as a metabolite of amino acids. It can be used for the synthesis of miscellaneous organic and inorganic complexes and for designing of drugs since it has remarkable utility in pharmaceutical industry due to its wide range of biological and pharmacological activities, for instance anti-microbial, anti-HIV, anti-tubercular, anti-cancer, anti-viral, anti-oxidant, anti-inflammatory, anti-angiogenic, analgesic activity, anti-Parkinson's disease, anti-convulsant etc. This review provides extensive information about the latest methods for the synthesis of isatin or its substituted derivatives based macrocyclic complexes of transition metals and their plentiful applications in medicinal chemistry.

Oxygen- and Sulphur-Containing Heterocyclic Compounds as Potential Anticancer Agents.

Oxygen- and sulphur-based heterocycles form the core structure of many biologically active molecules as well as U.S. FDA-approved drugs. Moreover, they possess broad range of biological activities, viz. anticancer, antiinflammatory, antioxidant, antitumour, antibacterial, antiviral, antidiabetic, anticonvulsant, anti-tubercular, analgesic, anti-leishmanial, antimalarial, antifungal, and anti-histaminic, Hence, O- and S-based heterocycles are gaining more attention in recent years on the road to the discovery of innovative anticancer drugs after the extensive investigation of nitrogen-based heterocycles as anticancer agents. Several attempts have been made to synthesize fused oxygen- and sulphur-based heterocyclic derivatives as joining one heterocyclic moiety with another may lead to improvement in the biological profile of a molecule. Humans have been cursed with cancer since long time. Despite the development of several heterocyclic anticancer medications such as 5-fluorouracil, doxorubicin, methotrexate, and daunorubicin, cure of cancer is difficult. Hence, researchers are trying to synthesize new fused/spiro heterocyclic molecules to discover novel anticancer drugs which may show promising anticancer effects with fewer side effects. Furthermore, fused heterocycles behave as DNA intercalating agents which have the ability to interact with DNA, leading to cell death thereby exerting anticancer effect. This review article highlights the synthesis and anticancer potentiality of oxygen- and sulphur-containing heterocyclic compounds covering the period from 2011 to 2021.

Design and Development of Triazole Derivatives as Prospective Anticancer Agents: A Review.

BACKGROUND: In recent years, there has been a crucial need for the design and development of novel anticancer drugs that can lessen the serious health problems and unwanted side effects associated with currently used anticancer drugs. The triazole nucleus is well-recognized to possess numerous pharmacological activities, including anticancer, as revealed by various investigations on anticancer drugs and the latest research findings. OBJECTIVE: The aim of this review article is to summarise the anticancer potential of 1, 2, 3-triazole, 1, 2, 4-triazole and heterocycle-fused triazole derivatives against several human cancer cell lines, compiling research articles published between 2010 and 2021. METHODS: Data were collected from PubMed, Google scholar and Research Gate using keywords "anticancer activity of 1, 2, 3-triazole derivatives", "anticancer activity of 1, 2, 4-triazole derivatives" and "anticancer activity of heterocycle- fused triazole derivatives" and reviewed comprehensively. RESULTS: This review examines the anticancer potential of 1,2,3-triazole coupledoleanolic acid/dithiocarbamate/ pyrido[ 2,3-d] pyrimidine derivatives, 1,2,3-triazole linked pyrimidine/1,4-naphthoquinone hybrids, and 1,2,4-triazole substituted methanone derivatives, acridine-based 1,2,4-triazole derivatives, 1,2,4-thiadiazol coupled with 1,2,4- triazole and 5-ene-thiazolo[3,2-b][1,2,4]triazole-6(5H)-one derivatives against several human cancer cell lines. CONCLUSION: This review highlights the key findings in the area of cancer therapy. Triazole derivatives possess anticancer activity against various human cancer cell lines, and hence the triazole core may act as a lead molecule for the synthesis of novel anticancer drugs.

Lithium-acetate-mediated Biginelli one-pot multicomponent synthesis under solvent-free conditions and cytotoxic activity against the human lung cancer cell line A549 and breast cancer cell line MCF7.

Various Biginelli compounds (dihydropyrimidinones) have been synthesized efficiently and in high yields under mild, solvent-free, and eco-friendly conditions in a one-pot reaction of 1,3-dicarbonyl compounds, aldehydes, and urea/thiourea/acetyl thiourea using lithium-acetate as a novel catalyst without the addition of any proton source. Comparative catalytic efficiency of lithium-acetate and polyphosphoric acid to catalyze Biginelli condensation is also studied under neat conditions. The reaction is carried out in the absence of any solvent and represents an improvement of the classical Biginelli protocol and an advantage in comparison with FeCl(3)·6H(2)O, NiCl(2)·6H(2)O and CoCl(2)·6H(2)O that were used with HCl as a cocatalyst. Compared to classical Biginelli reaction conditions, the present method has advantages of good yields, short reaction times, and experimental simplicity. The obtained products have been identified by spectral ((1)H NMR and IR) data and their melting points. The prepared compounds are evaluated for anticancer activity against two human cancer cell lines (lung cancer cell line A549 and breast cancer cell line MCF7).