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Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Screening Novel SAHA Derivatives as Anti-lung Carcinoma Agents: Synthesis, Biological Evaluation, Docking Studies and Further Mechanism Research between Apoptosis and Autophagyetween Apoptosis and Autophagy

Author(s): Weibin Huang, Song Zhang, Zhicheng Yang and Binghong Feng

Volume 15 , Issue 10 , 2015

Page: [1277 - 1284] Pages: 8

DOI: 10.2174/1871520615666150629101107

Price: $65


Four suberoylanilide hydroxamic acid (SAHA) derivatives (N34, N4I, N4B, N24) were designed and synthesized on the basis of our previous studies on N25. Assays for anti-proliferative activity and histone deacetylase (HDAC) activity were performed against human lung cancer (SPC-A-1, LTEP-a-2, NCI-H1650) and normal lung cells (MRC-5), which were compared with those of SAHA. Molecular docking was used to theoretically confirm the receptor-binding ability of N34. Ultimately, N34 was validated as the best HDAC inhibitor candidate. Furthermore, the effects of N34 on the levels of apoptosis- and autophagy-associated proteins caspase-3, caspase-9, Bcl-2 and Beclin-1 in SPC-A-1 cells were evaluated. N34 exerted more evident effects on human lung cancer than the other three SAHA derivatives did.

Keywords: Anti-proliferative activity, apoptosis- and autophagy-associated protein, HDAC activity assay, suberoylanilide hydroxamic acid (SAHA) derivaties, synthesis.

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