Literature DB >> 22460030

New diarylureas and diarylamides possessing acet(benz)amidophenyl scaffold: design, synthesis, and antiproliferative activity against melanoma cell line.

Hee Jin Kim1, Hye Jung Cho, Hwan Kim, Mohammed I El-Gamal, Chang-Hyun Oh, So Ha Lee, Taebo Sim, Jung-Mi Hah, Kyung Ho Yoo.   

Abstract

A series of new diarylurea and diarylamide derivatives possessing acet(benz)amidophenyl scaffold was synthesized. Their in vitro antiproliferative activity was tested against A375P human melanoma cell line. Compounds 1c,d and 2c,d showed the highest potencies with IC(50) values in sub-micromolar scale. In addition, compounds 1b,e,l and 2e,l were more potent than Sorafenib but with IC(50) values in micromolar range. Moreover, compound 2c was equipotent to Vemurafenib, and 2d showed higher potency than Vemurafenib against A375P. Molar refractometry calculation and ADME profiling of the highest potent four derivatives 1c,d and 2c,d are also reported.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22460030     DOI: 10.1016/j.bmcl.2012.03.020

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Biological evaluation, docking and molecular dynamic simulation of some novel diaryl urea derivatives bearing quinoxalindione moiety.

Authors:  Sedighe Sadeghian-Rizi; Ghadamali Ali Khodarahmi; Amirhossein Sakhteman; Ali Jahanian-Najafabadi; Mahboubeh Rostami; Mahmoud Mirzaei; Farshid Hassanzadeh
Journal:  Res Pharm Sci       Date:  2017-12

2.  Synthesis and biological evaluation of a new series of 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as new anticancer agents.

Authors:  Jian Feng; Tai Li; Shishao Liang; Chuanming Zhang; Xiaoyu Tan; Ning Ding; Xin Wang; Xiaoping Liu; Chun Hu
Journal:  Med Chem Res       Date:  2020-05-18       Impact factor: 1.965

3.  Synthesis and characterization of some novel diaryl urea derivatives bearing quinoxalindione moiety.

Authors:  Sedighe Sadeghian-Rizi; Ghadamali Khodarahmi; Amirhossein Sakhteman; Ali Jahanian-Najafabadi; Mahboubeh Rostami; Mahmoud Mirzaei; Farshid Hassanzadeh
Journal:  Res Pharm Sci       Date:  2018-02
  3 in total

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