New 3-Substituted-2-(4-hydroxyanilino)pyridine Derivatives: Synthesis, Antitumor Activity, and Tubulin Polymerization Inhibition.
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 IC50= 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.
Faculty of Pharmacy, Department of Pharmaceutical Organic Chemistry, Cairo University, Cairo, Egypt.
Salwa
S
Elmeligie
Faculty of Pharmacy, Department of Pharmaceutical Organic Chemistry, Cairo University, Cairo, Egypt.
Nadia A
NA
Khalil
Faculty of Pharmacy, Department of Pharmaceutical Organic Chemistry, Cairo University, Cairo, Egypt.
Eman M
EM
Ahmed
Faculty of Pharmacy, Department of Pharmaceutical Organic Chemistry, Cairo University, Cairo, Egypt.
Soha H
SH
Emam
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D016923:Cell Death / Q000187:drug effects; D002460:Cell Line; D045744:Cell Line, Tumor; D003078:Colchicine / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D058105:Polymerization / Q000187:drug effects*; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D050257:Tubulin Modulators / Q000138:chemical synthesis* / Q000494:pharmacology*
D000970:Antineoplastic Agents; D011725:Pyridines; D050257:Tubulin Modulators; D003078:Colchicine
Cytotoxic activity; Inhibitors; Synthesis