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

Title: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

Volume: 15 Issue: 10

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Huang Weibin, Zhang Song, Yang Zhicheng and Feng Binghong, 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, Anti-Cancer Agents in Medicinal Chemistry 2015; 15 (10) . https://dx.doi.org/10.2174/1871520615666150629101107