Your browser doesn't support javascript.
loading
Development of novel anilinoquinazoline-based carboxylic acids as non-classical carbonic anhydrase IX and XII inhibitors.
Elsayed, Zainab M; Almahli, Hadia; Nocentini, Alessio; Ammara, Andrea; Supuran, Claudiu T; Eldehna, Wagdy M; Abou-Seri, Sahar M.
Afiliação
  • Elsayed ZM; Scientific Research and Innovation Support Unit, Kafrelsheikh University, Kafrelsheikh, Egypt.
  • Almahli H; Department of Chemistry, University of Cambridge, Cambridge, UK.
  • Nocentini A; Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Firenze, Italy.
  • Ammara A; Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Firenze, Italy.
  • Supuran CT; Department of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Firenze, Italy.
  • Eldehna WM; Department of Pharmaceutical Chemistry, Kafrelsheikh University, Kafrelsheikh, Egypt.
  • Abou-Seri SM; School of Biotechnology, Badr University in Cairo, Badr City, Cairo, Egypt.
J Enzyme Inhib Med Chem ; 38(1): 2191163, 2023 Dec.
Article em En | MEDLINE | ID: mdl-36942698
As part of our ongoing endeavour to identify novel inhibitors of cancer-associated CA isoforms IX and XII as possible anticancer candidates, here we describe the design and synthesis of small library of 2-aryl-quinazolin-4-yl aminobenzoic acid derivatives (6a-c, 7a-c, and 8a-c) as new non-classical CA inhibitors. On account of its significance in the anticancer drug discovery and in the development of effective CAIs, the 4-anilinoquinazoline privileged scaffold was exploited in this study. Thereafter, the free carboxylic acid functionality was appended in the ortho (6a-c), meta (7a-c), or para-positon (8a-c) of the anilino motif to furnish the target inhibitors. All compounds were assessed for their inhibitory activities against the hCA I, II (cytosolic), IX, and XII (trans-membrane, tumour-associated) isoforms. Moreover, six quinazolines (6a-c, 7b, and 8a-b) were chosen by the NCI-USA for in vitro anti-proliferative activity evaluation against 59 human cancer cell lines representing nine tumour subpanels.
Assuntos
Palavras-chave

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Anidrases Carbônicas / Neoplasias Limite: Humans Idioma: En Revista: J Enzyme Inhib Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Egito País de publicação: Reino Unido

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Anidrases Carbônicas / Neoplasias Limite: Humans Idioma: En Revista: J Enzyme Inhib Med Chem Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2023 Tipo de documento: Article País de afiliação: Egito País de publicação: Reino Unido