Synthesis, molecular docking, antibacterial, antioxidant, and cytotoxicity activities of novel pyrido-cyclopenta[b]indole analogs
| Autor: | A. Amuthavalli, Gunasekaran Bhuvaneswari, Madhusudhanan Gogulramnath, R. Velmurugan, Ramaraj Thirugnanasampandan, B. Prakash |
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| Rok vydání: | 2020 |
| Předmět: |
Indole test
Antioxidant 010405 organic chemistry medicine.medical_treatment Organic Chemistry 010402 general chemistry 01 natural sciences Combinatorial chemistry 0104 chemical sciences Dimethyl acetal chemistry.chemical_compound chemistry medicine Dimethylformamide Knoevenagel condensation Cytotoxicity |
| DOI: | 10.6084/m9.figshare.11955693.v1 |
| Popis: | A series of new pyrido-cyclopenta[1,2-b]indole derivatives were synthesized via Knoevenagel reaction and followed by reflux with dimethylformamide dimethyl acetal. Their structures were investigated by spectral techniques and elemental analysis. In vitro antibacterial assessment against seven selected microorganisms evidenced that the compounds with halogen substituent have strong inhibitory action than that of the reference drugs. The antioxidant results were apparent that the compounds 5b, 5c, and 6c manifested explicit activity when compared with Butylhydroxyanisole and Vitamin-C. Cytotoxic activity analysis toward HeLa and MCF-7 cell lines was also assessed. Analogs 6c (IC50 values 15.1 μM and 18.6 μM) and 6d (IC50 values 17.4 μM and 20.7 μM) illustrated the interesting cytotoxicity activity. Molecular docking studies against p38 MAP kinase displayed a potential binding affinity with the receptor. Furthermore, in silico pharmacokinetic studies articulated the drug-likeness nature of the target compounds. |
| Databáze: | OpenAIRE |
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