Literature DB >> 27305384

1,2-Benzisothiazole Derivatives Bearing 4-, 5-, or 6-Alkyl/arylcarboxamide Moieties Inhibit Carbonic Anhydrase Isoform IX (CAIX) and Cell Proliferation under Hypoxic Conditions.

Vito Coviello1, Beatrice Marchi1, Stefania Sartini1, Luca Quattrini1, Anna Maria Marini1, Francesca Simorini1, Sabrina Taliani1, Silvia Salerno1, Paola Orlandi2, Anna Fioravanti2, Teresa Di Desidero2, Daniela Vullo3, Federico Da Settimo1, Claudiu T Supuran4, Guido Bocci2, Concettina La Motta1.   

Abstract

Three novel series of 1,2-benzisothiazole derivatives have been developed as inhibitors of carbonic anhydrase isoform IX. Compounds 5c and 5j, tested in vitro on the human colon cell line HT-29, blocked the growth of cells cultured under chemically induced hypoxic conditions, displaying a specific activity against cancer cells characterized by CAIX up-regulation. Moreover, a synergistic activity of 5c with SN-38 (the active metabolite of irinotecan) and 5-fluorouracil on cell proliferation under hypoxic conditions was demonstrated.

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Year:  2016        PMID： 27305384     DOI： 10.1021/acs.jmedchem.6b00616

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  6 in total

1.  Isolation and Expression Analysis of Three Types of α-Carbonic Anhydrases from the Antarctic Alga Chlamydomonas sp. ICE-L under Different Light Stress Treatments.

Authors:  Chongli Shi; Meiling An; Jinlai Miao; Yingying He; Zhou Zheng; Changfeng Qu; Xixi Wang; Huan Lin; Junhong Liu
Journal:  Mol Biotechnol       Date:  2019-03       Impact factor: 2.695

2.  Inhibitory activity against carbonic anhydrase IX and XII as a candidate selection criterion in the development of new anticancer agents.

Authors:  Mikhail Krasavin; Stanislav Kalinin; Tatiana Sharonova; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051

3.  Design, Synthesis, Molecular Docking Analysis, and Carbonic Anhydrase IX Inhibitory Evaluations of Novel N-Substituted-β-d-Glucosamine Derivatives that Incorporate Benzenesulfonamides.

Authors:  Feng-Ran Li; Zhan-Fang Fan; Su-Jiao Qi; Yan-Shi Wang; Jian Wang; Yang Liu; Mao-Sheng Cheng
Journal:  Molecules       Date:  2017-05-12       Impact factor: 4.411

4.  CAIX aptamer-functionalized targeted nanobubbles for ultrasound molecular imaging of various tumors.

Authors:  Lianhua Zhu; Luofu Wang; Yu Liu; Dan Xu; Kejing Fang; Yanli Guo
Journal:  Int J Nanomedicine       Date:  2018-10-16

5.  Open saccharin-based secondary sulfonamides as potent and selective inhibitors of cancer-related carbonic anhydrase IX and XII isoforms.

Authors:  Melissa D'Ascenzio; Paolo Guglielmi; Simone Carradori; Daniela Secci; Rosalba Florio; Adriano Mollica; Mariangela Ceruso; Atilla Akdemir; Anatoly P Sobolev; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2016-10-26       Impact factor: 5.051

6.  Novel insights on saccharin- and acesulfame-based carbonic anhydrase inhibitors: design, synthesis, modelling investigations and biological activity evaluation.

Authors:  Paolo Guglielmi; Giulia Rotondi; Daniela Secci; Andrea Angeli; Paola Chimenti; Alessio Nocentini; Alessandro Bonardi; Paola Gratteri; Simone Carradori; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051
  6 in total

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