Literature DB >> 26724730

Design and synthesis of new imidazo[1,2-a]pyridine and imidazo[1,2-a]pyrazine derivatives with antiproliferative activity against melanoma cells.

Rita Garamvölgyi1, Judit Dobos2, Anna Sipos2, Sándor Boros2, Eszter Illyés2, Ferenc Baska2, László Kékesi2, István Szabadkai2, Csaba Szántai-Kis2, György Kéri3, László Őrfi4.   

Abstract

Melanoma is an aggressive form of skin cancer and it is generally associated with poor prognosis in patients with late-stage disease. Due to the increasing occurrence of melanoma, there is a need for the development of novel therapies. A new series of diarylamide and diarylurea derivatives containing imidazo[1,2-a]pyridine or imidazo[1,2-a]pyrazine scaffold was designed and synthesized to investigate their in vitro efficacy against the A375P human melanoma cell line. We found several compounds expressing submicromolar IC50 values against the A375P cells, from which 15d, 17e, 18c, 18h, 18i demonstrated the highest potencies with IC50 below 0.06 μM.
Copyright © 2015 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  A375P; Antiproliferative activity; Diarylamide; Diarylurea; Imidazo[1,2-a]pyrazine; Imidazo[1,2-a]pyridine; Melanoma

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Substances:

Year:  2015        PMID: 26724730     DOI: 10.1016/j.ejmech.2015.12.001

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  3 in total

1.  Electro-organic synthesis of tetrahydroimidazo[1,2-a]pyridin-5(1H)-one via a multicomponent reaction.

Authors:  Mohammad Reza Asghariganjeh; Ali Asghar Mohammadi; Elham Tahanpesar; Ayeh Rayatzadeh; Somayeh Makarem
Journal:  Mol Divers       Date:  2020-01-09       Impact factor: 2.943

2.  [Design and synthesis of imidazo-fused heterocycles derivatives and their anti-tumor activity against breast cancer in mice].

Authors:  Jin Zhou; Bohong Liao; Yinggui Deng; Xiaowen Guo; Jialan Zhao; Jie Sun; Zhibo Zhu
Journal:  Nan Fang Yi Ke Da Xue Xue Bao       Date:  2018-08-30

3.  Synthesis of benzo[4,5]imidazo[1,2-a]pyrimidines and 2,3-dihydroquinazolin-4(1H)-ones under metal-free and solvent-free conditions for minimizing waste generation.

Authors:  Phuong Hoang Tran; Thanh-Phuong Thi Bui; Xuan-Quynh Bach Lam; Xuan-Trang Thi Nguyen
Journal:  RSC Adv       Date:  2018-10-26       Impact factor: 4.036

  3 in total

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