Synthesis, in vitro and in silico anti-proliferative activity of 4-aryl-4 H-chromene derivatives.

Autor: Parthiban, A., Kumaravel, M., Muthukumaran, J., Rukkumani, R., Krishna, R., Rao, H.
Zdroj: Medicinal Chemistry Research; Jul2016, Vol. 25 Issue 7, p1308-1315, 8p
Abstrakt: A new series of C4- N, N-dialkylaniline-substituted 4-aryl-4 H-chromenes were synthesized, and their anti-proliferative properties were evaluated against human cancer cell lines, namely, laryngeal carcinoma (Hep2), lung adenocarcinoma (A549), and cervical cancer (HeLa). The best among them, the 4-aryl-4 H-chromene with C4-1-phenylpiperidine substitution was selected for further structure activity relationship (SAR) studies. Among the derivatives, N,6-dimethyl-3-nitro-4-(4-(piperidine-1-yl)phenyl)-4 H-chromene-2-amine 3k showed most potent cytotoxic activity against all three cancer cell lines. Toxicity studies revealed that the 4-aryl-4 H-chromenes specifically target the cancer cell lines. Molecular docking studies of this compound revealed its efficient interaction with the active site of αβ-tubulin protein. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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