Heterocyclic compounds are well known for their different biological activity. The heterocyclic analogs are the building blocks for synthesis of the pharmaceutical active compounds in the organic chemistry. These derivatives show various type of biological activity like anticancer, antiinflammatory, anti-microbial, anti-convulsant, anti-malarial, anti-hypertensive, etc. From the last decade research showed that the quinoline analogs plays a vital role in the development of newer medicinal active compounds for treating various type of disease. Quinoline reported for their antiviral, anticancer, anti-microbial and anti-inflammatory activity. This review will summarize the various synthetic approaches for synthesis of quinoline derivatives and to check their biological activity. Derivatives of quinoline moiety plays very important role in the development of various types of newer drugs and it can be used as lead compounds for future investigation in the field of drug discovery process.

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It has been established on the basis of reported research that benzimidazoles and their analogs are active scaffolds. Benzimidazole is a benzofused imidazole compound that is present in several marketed molecules with a wide range of uses that established its importance in pharmaceutical sectors and industry. Drugs with a benzimidazole nucleus have unique structural characteristics and an electron-rich environment that allows them to attach to a variety of physiologically significant sites and produce a variety of actions. The development of benzimidazole heterocyclic molecules as antihistaminic (H1-receptor antagonist, for example, bilastine; 5-HT3 antagonist, for example, leri-setron); antimicrobial (antibiotic, for example, ridinilazole); antiulcer (proton pump inhibitor (PPI), for example, ilaprazole); antihypertensive (calcium channel blocker, for example, mibefradil); and drugs used to treat cancer include those that are antiparasitic (specifically anthelmintic, such as fubendazole), antipsychotic (D2 receptor antagonist, such as clopimozide), analgesic (opioid analgesic, such as clonitazene), and phosphodiesterase inhibitor (PDE3 inhibitor, such as adibendan). Due to its broad applications, scientists are continuously enthralled by benzimidazoles and their derivatives to study their chemistry. Several synthesis strategies can prepare benzimidazole or its derivatives and the focus will always be on new, greener, and more economical ways for its synthesis. Among all methods, catalytic cyclization, catalytic coupling, and catalytic reactions are the most used approaches for the synthesis of benzimidazoles and their analogs. The present review entitled various synthetic approaches for synthesizing benzimidazole from 2009 to 2021 and its derivatives, which will be very useful to researchers for developing benzimidazole moieties.

: 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.