title: Discovery of hybrid dual N-acylhydrazone and diaryl urea derivatives as potent antitumor agents: design, synthesis and cytotoxicity evaluation.
abstract: Based on the hybrid pharmacophore design concept, a novel series of dual diaryl urea and N-acylhydrazone derivatives were synthesized and evaluated for their in vitro cytotoxicity by the standard MTT assay. The pharmacological results indicated that most compounds exhibited moderate to excellent activity. Moreover, compound 2g showed the most potent cytotoxicity against HL-60, A549 and MDA-MB-231 cell lines, with IC50 values of 0.22, 0.34 and 0.41 μM, respectively, which was 3.8 to 22.5 times more active than the reference compounds sorafenib and PAC-1. The promising compound 2g thus emerges as a lead for further structural modifications.
authors: Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, Liaoning, China.
authors: Xin
authors: X
authors: Zhai
authors: Qiang
authors: Q
authors: Huang
authors: Nan
authors: N
authors: Jiang
authors: Di
authors: D
authors: Wu
authors: Hongyu
authors: H
authors: Zhou
authors: Ping
authors: P
authors: Gong
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000633:toxicity*; D045744:Cell Line, Tumor; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans; D006835:Hydrazones / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D014508:Urea / Q000031:analogs & derivatives / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D006835:Hydrazones; D014508:Urea