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Novel indole hydrazide derivatives: Synthesis and their antiproliferative activities through inducing apoptosis and DNA damage
Author(s) -
KilicKurt Zühal,
Acar Cemre,
Ergul Mustafa,
BakarAtes Filiz,
Altuntas Tunca G.
Publication year - 2020
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.202000059
Subject(s) - apoptosis , annexin , cell cycle checkpoint , chemistry , hydrazide , cell cycle , western blot , cell culture , microbiology and biotechnology , programmed cell death , dna damage , cell growth , indole test , phosphorylation , dna , mcf 7 , biochemistry , biology , cancer cell , gene , cancer , genetics , human breast , organic chemistry
A series of novel indole hydrazide derivatives was synthesized and evaluated for their anticancer activities. Compound 12 exhibited the highest antiproliferative activity against the MCF‐7 cell line, with an IC 50 value of 3.01 µM. Treatment of MCF‐7 cells with compound 12 led to cell cycle arrest at the G0/G1 phase and also displayed a significant annexin V binding pattern, indicating that compound 12 is effective in apoptotic cell death. The Western blot analysis showed that compound 12 increased the expression of proapoptotic Bax and decreased the levels of the antiapoptotic Bcl‐2 protein. It was also observed that MCF‐7 cells treated with compound 12 showed reduced levels of procaspase‐3 and ‐9 proteins. Moreover, compound 12 treatment induced a significant DNA damage in MCF‐7 cells by increasing H2AX and ATM phosphorylation.