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New 3‐Substituted‐2‐(4‐hydroxyanilino)pyridine Derivatives: Synthesis, Antitumor Activity, and Tubulin Polymerization Inhibition
Author(s) -
Elmeligie Salwa,
Khalil Nadia A.,
Ahmed Eman M.,
Emam Soha H.
Publication year - 2017
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201600256
Subject(s) - chemistry , pyridine , colchicine , in vitro , tubulin , mtt assay , stereochemistry , cytotoxic t cell , cell culture , cytotoxicity , biological activity , antimitotic agent , microtubule polymerization , cell growth , microtubule , biochemistry , medicinal chemistry , biology , genetics , microbiology and biotechnology
A series of new pyridine derivatives 4a–c , 5a–d , 6a–d , 7a–f , and 8a–f structurally related to ABT‐751 were synthesized and characterized by spectroscopic means and elemental analysis. All the synthesized compounds were tested for their cytotoxic activity in vitro against the HCT‐116 and HepG‐2 cancer cell lines using the MTT assay. The results showed that compound 8d has higher cytotoxic activity than the reference antimitotic agent colchicine, against both tested cell lines, with IC 50 = 0.52 and 1.40 μM, respectively. The three most active compounds, 5d , 8b , and 8d , were further screened in vitro for inhibition of tubulin and showed remarkable results in comparison to colchicine.