The versatile multicomponent Mannich reaction occupies a salient position in organic chemistry and drug design. Sound knowledge of its scope and variations and of the biological activities of Mannich bases is crucial for the development and improvement of drugs for various diseases. Areas covered: The following article provides an overview of the latest developments in the field of drugs based on the Mannich reaction. Web-based literature searching tools such as PubMed and SciFinder were applied to obtain useful articles. In addition, pertinent literature that was recently published by the authors is discussed in this manuscript. The chemical structures of bioactive Mannich bases are also given. Expert opinion: The Mannich reaction represents a feasible and cost-effective procedure with great potential for drug development. Several newly discovered Mannich bases exhibit sound activities against various human diseases as well as favorable pharmacokinetics. Thus, scientific research about Mannich bases is prospering and appears very attractive both for chemists and for clinicians.
Curcumin, a polyphenol, has a wide range of biological properties such as anticancer, antibacterial, antitubercular, cardioprotective and neuroprotective. Moreover, the anti-proliferative activities of Curcumin have been widely studied against several types of cancers due to its ability to target multiple pathways in cancer. Although Curcumin exhibited potent anticancer activity, its clinical use is limited due to its poor water solubility and faster metabolism. Hence, there is an immense interest among researchers to develop potent, water-soluble, and metabolically stable Curcumin analogs for cancer treatment. While drug resistance remains a major problem in cancer therapy that renders current chemotherapy ineffective, curcumin has shown promise to overcome the resistance and resensitize cancer to chemotherapeutic drugs in many studies. In the present review, we are summarizing the role of curcumin in controlling the proliferation of drug-resistant cancers and development of curcumin-based therapeutic applications from cell culture studies up to clinical trials.
Background: Chalcones are structurally simple compounds that are easily accessible by synthetic methods.
Heterocyclic chalcones have gained the interest among scientists due to their diverse biological activities. The anti-tumor
activities of heterocyclic chalcones are especially remarkable and the growing number of publications dealing with this
topic warrants an up-to-date compilation.Methods: Search for antitumor active heterocyclic chalcones was carried out using Pubmed and Scifinder as common
web-based literature searching tools. Pertinent and current literature is covered from 2015/2016 to 2019. Chemical
structures, biological activities and modes of action of anti-tumor active heterocyclic chalcones are summarized.Results:Simply prepared chalcones have emerged over the last years with promising antitumor activities. Among them is
a considerable number of tubulin polymerization inhibitors. But there are also new chalcones targeting special enzymes
such as histone deacetylases or with DNA-binding properties.Conclusion:This review provides a summary of recent heterocyclic chalcone derivatives with distinct anti-tumor
activities.
As there is no specified drug available to fight COVID-19, it is essential to have a different strategy to fight this virus. In the present study, using molecular docking, we have identified possible protease inhibitors of COVID-19 by the molecules present in Nigella sativa L. (black cumin), which is a reputed healing herb extensively used for processing Ayurvedic and Unani remedies. Herein, we perform molecular docking and study of various physical properties/descriptors of four derivatives of thymoquinone found in the essential oil of the said seeds and they are compared with the docking results of chloroquine to determine its potential against COVID-19 infection.
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