ABSTRACT
The increased expression of VEGFR-2 in a variety of cancer cells promotes a cascade of cellular responses that improve cell survival, growth, and proliferation. Heterocycles are common structural elements in medicinal chemistry and commercially available medications that target several biological pathways and induce cell death in cancer cells. Herein, the evaluation of indazolyl-acyl hydrazones as antioxidant and anticancer agents is reported. Compounds 4e and 4j showed inhibitory activity in free radical scavenging assays (DPPH and FRPA). The titled compounds were employed in cell viability studies using MCF-7 cells, and it was observed that compounds 4f and 4j exhibited IC50 values 15.83 µM and 5.72 µM, respectively. In silico docking revealed the favorable binding energies of -7.30 kcal/mol and -8.04 kcal/mol for these compounds towards Vascular Endothelial Growth Factor Receptor-2 (VEGFR-2), respectively. In conclusion, compounds with antioxidant activity and that target VEGFR-2 in breast cancer cells are reported.
Subject(s)
Antineoplastic Agents , Breast Neoplasms , Humans , Female , Molecular Structure , Structure-Activity Relationship , Antioxidants/pharmacology , Vascular Endothelial Growth Factor Receptor-2 , Breast Neoplasms/drug therapy , Hydrazones/pharmacology , Vascular Endothelial Growth Factor A/pharmacology , Cell Proliferation , Drug Design , Molecular Docking Simulation , Antineoplastic Agents/chemistry , Drug Screening Assays, AntitumorABSTRACT
The recognition and sensing of various analytes in aqueous and biological systems by using fluorometric or colorimetric chemosensors possessing high selectivity and sensitivity, low cost has gained enormous attention. Furthermore, thiophene derivatives possess exceptional photophysical properties compared to other heterocycles, and therefore they can be employed in chemosensors for analyte detection. In this review, we have tried to explore the design and detection mechanism of various thiophene-based probes, practical applicability, and their advanced models (design guides), which could be thoughtful for the synthesis of new thiophene-based probes. This review provides an insight into the reported chemosensors (2008-2020) for thiophene scaffold as effective emission and absorption-based chemosensors.
Subject(s)
Metals/analysis , Thiophenes , Colorimetry , Energy Transfer , Fluorescence , Fluorometry , Ions , Metals/chemistry , Molecular Structure , Photochemical Processes , Thiophenes/chemistryABSTRACT
Thiazole is the most common heterocyclic compound in heterocyclic chemistry and in drug design. Presence of several reaction sites in the thiazole moiety extends their range of applications and leads to new solutions for challenges in synthetic and medicinal chemistry. Thiazole derivatives are widely used as bioactive agents, liquid crystals, sensors, catalysts, etc. The motivating molecular architecture of 1,3-thiazoles makes them suitable moieties for drug development. In this review, our aim is to corroborate the recent data available on various synthetic strategies and biological properties of 1,3- thiazole derivatives.
