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Design, synthesis and mechanistic study of new dual targeting HDAC/tubulin inhibitors.
El-Zoghbi, Mona S; Bass, Amr Ka; A Abuo-Rahma, Gamal El-Din; Mohamed, Mamdouh Fa; Badr, Mohamed; Al-Ghulikah, Hanan A; Abdelhafez, El-Shimaa Mn.
Afiliación
  • El-Zoghbi MS; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Menoufia University, Egypt.
  • Bass AK; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Menoufia University, Egypt.
  • A Abuo-Rahma GE; Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, Minia, 61519, Egypt.
  • Mohamed MF; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Deraya University, New Minia, Minia, Egypt.
  • Badr M; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sohag University, Sohag, 82524, Egypt.
  • Al-Ghulikah HA; Department of Biochemistry, Faculty of Pharmacy, Menoufia University, Menoufia, Egypt.
  • Abdelhafez EM; Department of Chemistry, College of Science, Princess Nourah Bint Abdulrahman University, PO Box 84428, Riyadh, 11671, Saudi Arabia.
Future Med Chem ; 16(7): 601-622, 2024 04.
Article en En | MEDLINE | ID: mdl-38436113
ABSTRACT

Aim:

The purpose of this work is to create and synthesize a new class of chemicals 3-cyano-2-substituted pyridine compounds with expected multitarget inhibition of histone deacetylase (HDAC) and tubulin. Materials &

methods:

The target compounds (3a-c, 4a-c and 5a-c) were synthesized utilizing 6-(4-methoxyphenyl)-2-oxo-4-(3,4,5-trimethoxyphenyl)-3-cyanopyridine, with various linkers and zinc-binding groups (ZBGs).

Results:

Most of the tested compounds showed promising growth inhibition, and hydroxamic acid-containing hybrids possessed higher HDAC inhibition than other ZBGs. Compound 4b possessed the highest potency; however, it showed the most tubulin polymerization inhibition. Docking studies displayed good binding into HDAC1 and six pockets and tubulin polymerization protein.

Conclusion:

Compound 4b could be considered a good antitumor candidate to go further into in vivo and clinical studies.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Histona Desacetilasas / Antineoplásicos Idioma: En Revista: Future Med Chem Año: 2024 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Reino Unido
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
Buscar en Google

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Inhibidores de Histona Desacetilasas / Antineoplásicos Idioma: En Revista: Future Med Chem Año: 2024 Tipo del documento: Article País de afiliación: Egipto Pais de publicación: Reino Unido