Indole based prostate cancer agents

Cancer weakens the immune system which fails to fight against the rapidly growing cells. Among the various types of cancers, prostate cancer (PCa) is causing greater number of deaths in men after lung cancer, demanding advancement to prevent, detect and treat PCa. Several small molecule heterocycles and few peptides are being used as oncological drugs targeting PCa. Heterocycles are playing crucial role in the development of novel cancer chemotherapeutics as well as immunotherapeutics. Indole skeleton, being a privileged structure has been extensively used for the discovery of novel anticancer agents and the application of indole derivatives against breast cancer is well documented. The present article highlights the usefulness of indole linked heterocyclic compounds as well as the fused indole derivatives against prostate cancer.

Current developments in the Pyran-Based Analogues as Anticancer Agents

: Heterocyclic compounds offer an enormous area for new lead molecules for drug discovery. Till today, efforts are being continuously made to find appropriate treatment for the management of the deadly disease of cancer. Amongst the large number of heterocycles that are found in nature, heterocycles having oxygen obtained noteworthy attention due to their distinctive and pharmacological activities.‘Pyran’ is one of the most significant non-aromatic, six-membered ring composed of one oxygen atom and five carbon atoms. It is considered a privileged structure since pyran and its related derivatives exhibit a wide spectrum of biological activities. Pyran derivatives are found to have excellent anti-cancer properties against various types of cancer. The present review focussed on the current advances in different types of pyran-based derivatives as anti-cancer agents. Various in-vitro (cell based testing), in-vivo (animal based testing) models as well as molecular docking along with results are also covered. A subsection describing briefly natural pyran containing anticancer compounds is also incorporated in the review.

The Fellowship of Privileged Scaffolds—One Structure to Inhibit Them All

Over the past few years, the application of privileged structure has emerged as a powerful approach to the discovery of new biologically active molecules. Privileged structures are molecular scaffolds with binding properties to the range of different biological targets. Moreover, privileged structures typically exhibit good drug-like properties, thus assuring more drug-like properties of modified compound. Our main objective is to discuss the privileged structures used for the development of antiviral agents.

Advances in the application of 1,2,4-triazole-containing hybrids as anti-tuberculosis agents

Tuberculosis is a deadly communicable disease caused by the bacillus Mycobacterium tuberculosis (MTB), and pulmonary tuberculosis accounts for over 80% of the total cases. The 1,2,4-triazole is a privileged structure in the discovery of new drugs, and its derivatives act on various targets in MTB. In particular, 1,2,4-triazole hybrids can not only exert dual or multiple antitubercular mechanisms of action but also have the potential to enhance efficacy and reduce side effects. The present work aims to summarize the current status of 1,2,4-triazole hybrids as potential antitubercular agents, covering articles published between 2010 and 2020, to aid the further rational design of novel potential drug candidates endowed with higher efficacy, better compliance and fewer side effects.

A Meticulous Review on Coumarin Derivatives as a Marvel Medication for Thousands of Ailments

Coumarin derivatives have progressively enticed medicinal chemists because of their potential role in preventing and treating ailments. They epitomize a key motif nucleus in heterocyclic chemistry and a privileged structure in medicinal chemistry because of its extensive-range pharmacological activity. Regardless of the advancement in medicine over the past century, cancer is still remain the prominent source of death in the world and it makes indispensible needs to synthesize the compounds with coumarin as the core nucleus. Synthesis of various coumarin derivatives and evaluation of their pharmacological effects can perceive a solution to certain enigmatic demands in health sector. This review article is fixated on different synthetic routes of coumarin nucleus containing compounds. The review article also highlights different biological activities such as anticancer, antibacterial, anti- inflammatory, antihyperlipidemic and enzyme inhibition activities.

Synthetic Approach to Potential Anticancer Benzimidazole Derivatives- A Review

: Cancer is one of the deadliest diseases in many developed and developing countries. Continuous efforts are required for designing better therapeutic agents for the treatment of cancer with more efficacy, selectivity, and less toxicity. The fused heterocyclic ring system has been identified by several researchers as a privileged structure that can be used as a basis for drug discovery in medicinal chemistry. The hetero-aromatic bicyclic ring system acts as a pharmacophore in a wide range of drugs with therapeutic potential. According to studies in the literature, variously substituted benzimidazoles have distinct pharmacological profiles with multi-targeting ability, making them an important anchor for the production of novel therapeutic agents against complex cancers including breast cancer, skin cancer, and blood cancer. In this presented article we are discussed various synthetic methods for the synthesis of anticancer benzimidazoles and their derivatives in different solvent conditions, substrates, and various catalysts mainly those which are eco-friendly, and economical, which shows the anticancer activity. We also focused on various derivatives are under clinical trials containing Benzimidazole moiety.

Juglone: a versatile natural platform for obtaining new bioactive compounds

: Juglone is a metabolite produced by several species of plants, in particular Juglans nigra. Additionally, juglone is a 1,4-naphthoquinone that has several biological actions. Antimicrobial, antifungal, sedative, oxidizing, antihypertensive, and especially anti-proliferative actions have been described for juglone. This justifies that 1,4-naphthoquinone is a privileged structure for Medicinal Chemistry, and it is useful for the development of new prototypes with varied actions. In this work, we make a profound review of juglone synthesis methodology, the biological actions of juglone, and mainly the synthesis and pharmacological actions of juglone derivatives. We hope that the potent biological actions described for these derivatives in this review will stimulate the continuous design, synthesis, and pharmacological evaluation of new juglone derivatives.

Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.