Design, synthesis and computational studies of new azaheterocyclic coumarin derivatives as anti- agents targeting enoyl acyl carrier protein reductase (InhA).

In this study, we designed and synthesized a series of coumarin derivatives as antitubercular agents targeting the enoyl acyl carrier protein reductase (InhA) enzyme. Among the synthesized compounds, the tetrazole derivative 4c showed the most potent antitubercular effect with a minimum inhibitory concentration value (MIC) of 15 μg mL against H37Rv and could also inhibit the growth of the mutant strain (Δ). Compound 4c was able to penetrate -infected human macrophages and suppress the intracellular growth of tubercle bacilli.

New pyrazolylindolin-2-one based coumarin derivatives as anti-melanoma agents: design, synthesis, dual BRAF/VEGFR-2 inhibition, and computational studies.

Malignant melanoma is the most invasive skin cancer with the highest risk of death. The inhibition of BRAF appears relevant for overcoming secondary resistance developed during melanoma treatment. BRAF triggers angiogenesis modification of the expression of angiogenic inducers, which play a crucial role in the metastasis of melanoma.