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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kim HJ,Cho HJ,Kim H,El-Gamal MI,Oh CH,Lee SH,Sim T,Hah JM,Yoo KH

doi

10.1016/j.bmcl.2012.03.020

subject

Has Abstract

pub_date

2012-05-01 00:00:00

pages

3269-73

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00327-7

journal_volume

22

pub_type

杂志文章

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