210358-58-0Relevant academic research and scientific papers
Study of arginine mimetic benzamidine urea derivatives as PAD4 inhibitors
Kurdekar, Vadiraj,Dighe, Satish N.,Jadhav, Hemant R.
, p. 1273 - 1278 (2020/12/04)
Rheumatoid Arthritis (RA) is an autoimmune inflammatory disease, where antibodies are generated against citrullinated proteins. Citrullinated proteins are catalytic products of the Peptidyl Arginine Deiminase 4 (PAD4) enzyme. Since PAD4 acts on peptidyl a
Discovery of hybrid dual N-acylhydrazone and diaryl urea derivatives as potent antitumor agents: Design, synthesis and cytotoxicity evaluation
Zhai, Xin,Huang, Qiang,Jiang, Nan,Wu, Di,Zhou, Hongyu,Gong, Ping
, p. 2904 - 2923 (2013/05/09)
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.
Design, synthesis and antiproliferative activities of diaryl urea derivatives bearing N-acylhydrazone moiety
Zhang, Bei,Zhao, Yan Fang,Zhai, Xin,Fan, Wei Jie,Ren, Jun Ling,Wu, Chun Fu,Gong, Ping
, p. 915 - 918 (2012/08/28)
A new series of diaryl urea derivatives bearing N-acylhydrazone moiety were designed and synthesized. All the target compounds were evaluated for their antiproliferative activities against human leukemia cell line (HL-60), human lung adenocarcinoma epithelial cell line (A549) and human breast cancer cell line (MDA-MB-231) in vitro by standard MTT assay. The pharmacological results indicated that some compounds exhibited promising antitumor activities. Compound 1j showed the most potent antiproliferative activity against the tested three cell lines with IC50 values of 0.13 μmol/L, 0.7 μmol/L and 0.5 μmol/L, respectively.
