Literature DB >> 25455487

Serendipitous discovery of 2-((phenylsulfonyl)methyl)-thieno[3,2-d]pyrimidine derivatives as novel HIV-1 replication inhibitors.

Junwon Kim1, Jeongjin Kwon1, Doohyun Lee1, Suyeon Jo1, Dong-Sik Park1, Jihyun Choi1, Eunjung Park1, Jong Yeon Hwang1, Yoonae Ko1, Inhee Choi1, Moon Kyeong Ju1, JiYe Ahn1, Junghwan Kim1, Sung-Jun Han1, Tae-Hee Kim1, Jonathan Cechetto1, Jiyoun Nam1, Sujin Ahn1, Peter Sommer1, Michel Liuzzi1, Jinhwa Lee1.   

Abstract

We identified a novel class of 2-((phenylsulfonyl)methyl)-thieno[3,2-d]pyrimidine compounds as potent HIV-1 replication inhibitors serendipitously during the process of evaluation of triazolothienopyrimidine (TTPM) compounds. Herein, we report synthesis and biological evaluation of 2-((phenylsulfonyl)methyl)-thieno[3,2-d]pyrimidine compounds using a cell-based full replication assay to identify thienopyrimidines 6 and 30, which could be further utilized as viable lead compounds.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Cell-based assay; HIV-1; Inhibitor; Structure–activity relationship; Thienopyrimidine

Mesh:

Substances:

Year:  2014        PMID: 25455487     DOI: 10.1016/j.bmcl.2014.10.007

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


  2 in total

1.  Metal-free cascade synthesis of unsymmetrical 2-aminopyrimidines from imidazolate enaminones.

Authors:  Xue Cui; Jianting Ma; Tingting Zeng; Junyu Xu; Youbin Li; Xuesong Wang
Journal:  RSC Adv       Date:  2021-07-14       Impact factor: 4.036

Review 2.  Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents.

Authors:  Prisca Lagardère; Cyril Fersing; Nicolas Masurier; Vincent Lisowski
Journal:  Pharmaceuticals (Basel)       Date:  2021-12-27
  2 in total

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