Literature DB >> 16682186

Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621.

Shenlin Huang1, Peter J Connolly, Ronghui Lin, Stuart Emanuel, Steve A Middleton.   

Abstract

A novel prodrug strategy for cyclin-dependent kinase inhibitor JNJ-7706621 has been explored. Through N-acylation of a sulfonamide substituent, tails containing different solubilizing groups (amino, carboxyl, alkoxyl, and hydroxyl) were attached to JNJ-7706621. Most of the prodrugs exhibited good aqueous solubility and the N-acyl groups on the sulfonamide were metabolically cleaved to generate active drug in rat PK study.

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Year:  2006        PMID： 16682186     DOI： 10.1016/j.bmcl.2006.04.071

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


  7 in total

1.  The role of the acidity of N-heteroaryl sulfonamides as inhibitors of bcl-2 family protein-protein interactions.

Authors:  B Barry Touré; Karen Miller-Moslin; Naeem Yusuff; Lawrence Perez; Michael Doré; Carol Joud; Walter Michael; Lucian DiPietro; Simon van der Plas; Michael McEwan; Francois Lenoir; Madelene Hoe; Rajesh Karki; Clayton Springer; John Sullivan; Kymberly Levine; Catherine Fiorilla; Xiaoling Xie; Raviraj Kulathila; Kara Herlihy; Dale Porter; Michael Visser
Journal:  ACS Med Chem Lett       Date:  2013-01-04       Impact factor: 4.345

2.  Discovery of a first-in-class CDK2 selective degrader for AML differentiation therapy.

Authors:  Liguo Wang; Xuejing Shao; Tianbai Zhong; Yue Wu; Aixiao Xu; Xiuyun Sun; Hongying Gao; Yongbo Liu; Tianlong Lan; Yan Tong; Xue Tao; Wenxin Du; Wei Wang; Yingqian Chen; Ting Li; Xianbin Meng; Haiteng Deng; Bo Yang; Qiaojun He; Meidan Ying; Yu Rao
Journal:  Nat Chem Biol       Date:  2021-03-04       Impact factor: 15.040

Review 3.  Targeting cyclin-dependent kinases in human cancers: from small molecules to Peptide inhibitors.

Authors:  Marion Peyressatre; Camille Prével; Morgan Pellerano; May C Morris
Journal:  Cancers (Basel)       Date:  2015-01-23       Impact factor: 6.639

4.  Design, synthesis and anticancer activity of some novel thioureido-benzenesulfonamides incorporated biologically active moieties.

Authors:  Mostafa M Ghorab; Mansour S Alsaid; Mohamed S Al-Dosary; Yassin M Nissan; Sabry M Attia
Journal:  Chem Cent J       Date:  2016-04-07       Impact factor: 4.215

5.  Deregulations in the cyclin-dependent kinase-9-related pathway in cancer: implications for drug discovery and development.

Authors:  Gaetano Romano
Journal:  ISRN Oncol       Date:  2013-06-06

6.  Synthesis, Molecular Structure, Metabolic Stability and QSAR Studies of a Novel Series of Anticancer N-Acylbenzenesulfonamides.

Authors:  Beata Żołnowska; Jarosław Sławiński; Mariusz Belka; Tomasz Bączek; Anna Kawiak; Jarosław Chojnacki; Aneta Pogorzelska; Krzysztof Szafrański
Journal:  Molecules       Date:  2015-10-21       Impact factor: 4.411

7.  Design, synthesis, and biological evaluation of novel N 4 -substituted sulfonamides: acetamides derivatives as dihydrofolate reductase (DHFR) inhibitors.

Authors:  Essam M Hussein; Munirah M Al-Rooqi; Shimaa M Abd El-Galil; Saleh A Ahmed
Journal:  BMC Chem       Date:  2019-07-11
  7 in total

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