Coumarins as anticancer agents: A review on synthetic strategies, mechanism of action and SAR studies

Coumarin heterocyclic derivatives: chemical synthesis and biological activity

Coumarin hybrids as novel therapeutic agents.

We present herein the first visible-light-driven hydrocarboxylation as well as carbocarboxylation of alkynes using CO2 via an iridium/cobalt dual catalysis. Such transformations provide access to various pharmaceutically important heterocycles in a one-pot procedure from readily available alkynes. Coumarins, 2-quinolones, and 2-benzoxepinones were directly accessed through a one-pot alkyne hydrocarboxylation/alkene isomerization/cyclization sequence in which the Ir photocatalyst serves a dual role to promote single-electron transfer in alkyne hydrocarboxylation and energy transfer in the subsequent alkene isomerization. Moreover, an unprecedented cobalt carboxylation/acyl migration cascade enables alkyne difunctionalization to introduce γ-hydroxybutenolides with high efficiency. We expect that this cascade strategy will inspire new perspectives for alkyne and alkene difunctionalization.

Visible-Light-Driven Alkyne Hydro-/Carbocarboxylation Using CO2 via Iridium/Cobalt Dual Catalysis for Divergent Heterocycle Synthesis

Phytochemicals are chemical compounds that occur naturally in the plant kingdom. Some are responsible for the organoleptic properties of the natural sources in which they are present. The term is generally used to refer to those chemicals that may have biological significance, for example carotenoids, flavonoids, coumarins, or chromones, but not all are established as essential nutrients. There may be as many as 4,000 different phytochemicals having potential activity against several diseases such as cancer and metabolic or degenerative diseases.

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Coumarins — An Important Class of Phytochemicals

Numerous research reports have indicated the coumarin nucleus as a potential candidate for development of anti-inflammatory drugs. Various phytoconstituents such as umbelliferone, scopoletin, columbiatnetin, visniadin, marmin, and many more derived from coumarin nucleus are found to have potent anti-inflammatory as well as antioxidant activities. A large number of coumarin derivatives have also been designed, synthesized, and evaluated to have mild-to-very potent anti-inflammatory activity through different mechanisms. However, despite the continuing efforts in search of these drugs, no major breakthrough has been achieved so far. In the present review, a critical analysis of various reports on naturally as well as the synthetically derived coumarin derivatives having anti-inflammatory activity has been carried out and a structural–activity relationship around the coumarin nucleus has been proposed to assist the medicinal chemists in rationally designing the anti-inflammatory drugs.

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Coumarin: a potential nucleus for anti-inflammatory molecules

Two series of novel derivatives have been designed by coupling medicinally important coumarin and benzimidazole nuclei through different linkers. These compounds have been predicted to be potent anti-inflammatory and anthelmintic by in silico studies using PASS (prediction of activity spectra for substances) software. The compounds are synthesized and evaluated for the predicted activities as well as for their in vitro antioxidant potential. Compounds of first series (4a–4f) are found good to moderate anti-inflammatory agents. Among these, compounds 4b and 4f exhibited maximum anti-inflammatory activity (45% inhibition), which is equivalent to the activity of indomethacin (48% inhibition) after 3 h (peak inflammatory response time). Compounds of second series (5a–5f) exhibit anthelmintic activity. Amongst these, compound 5f has mortality activity marginally higher than albendazole (10–11 s). Compound 5e is found to be the most potent antioxidant with remarkable EC50 value (0.08 µM/mL), which is though a little less than that of ascorbic acid (0.03 µM/mL). In addition, a comparative analysis of calculated Lipinski’s parameters reveals that all test compounds have the propensity to be orally bioavailable. Based on these findings, compounds 4b, 4f, 5e, and 5f are identified as new leads to develop potent anti-inflammatory, anthelmintic, and antioxidant compounds.

Synthesis and PASS-assisted evaluation of coumarin–benzimidazole derivatives as potential anti-inflammatory and anthelmintic agents

Lung adenocarcinoma or non-small cell lung cancer (NSCLC) represents one of the most diagnosed cancers worldwide. Anaplastic lymphoma kinase (ALK) mutation, a tyrosine kinase and ALK fusion or rearrangement oncogene, has been found rarely in patients with NSCLC. Newer treatment modalities with different ALK inhibitors in targetable specific ALK mutations have recently made great strides in the management of NSCLC patients. We present a case of NSCLC harboring ALK mutation with primary cutaneous marginal zone B-cell lymphoma (PCMZL) treated with adjuvant chemotherapy with pemetrexed and cisplatin, and ALK-echinoderm microtubule-associated protein-like 4 (EML4)-targeting treatment alectinib.

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Anaplastic Lymphoma Kinase (ALK) Mutation-Targeting Treatment With Alectinib in Lung Adenocarcinoma and Primary Cutaneous Marginal Zone B-Cell Lymphoma

Purva Sethi

Papers

Coumarin: a potential nucleus for anti-inflammatory molecules

Synthesis and PASS-assisted evaluation of coumarin–benzimidazole derivatives as potential anti-inflammatory and anthelmintic agents

Anaplastic Lymphoma Kinase (ALK) Mutation-Targeting Treatment With Alectinib in Lung Adenocarcinoma and Primary Cutaneous Marginal Zone B-Cell Lymphoma