Design, Synthesis and Bioevaluation of Novel N‐Substituted‐3,5‐Bis(Arylidene)‐4‐piperidone Derivatives as Cytotoxic and Antitumor Agents with Fluorescent Properties

• DOI: 10.1111/cbdd.12254
• Publication Date: 2013-10-22T19:08:39Z
• Authors: Jufeng Sun; Shuping Zhang; Chen Yu; Guige Hou; Xiaofan Zhang; Keke Li; Feng Zhao
• Keywords: 0301 basic medicine; Dose-Response Relationship, Drug; Molecular Structure; Antineoplastic Agents; 01 natural sciences; 0104 chemical sciences; 3. Good health; 03 medical and health sciences; Cell Line, Tumor; Drug Design; Humans; Drug Screening Assays, Antitumor; Piperidones; Fluorescent Dyes

Ten new N ‐substituted‐3,5‐bis(arylidene)‐4‐piperidone derivatives (series 1 and 2 ) were synthesized subsequently evaluated against human carcinoma cell lines SW 1990, MIA PaCa‐2, PG ‐ BE 1, NCI ‐H460, SK BR ‐3 for cytotoxic activity by the CCK ‐8 method, their fluorescent properties investigated as well. The compounds confirmed to display greater neoplastic cells, approximately 50% of IC 50 values lower than 5 μ m . In particular, 1a , 1c 1d, 1e bearing 3‐bromophenyl groups revealed most active antitumor drug candidates had average 1.94, 1.11, 1.16, 0.817 respectively. Furthermore, interesting might contribute visualization distribution in tumor cells. Some possible reasons disparity between two series explored. This study high potential these molecules further development agents.