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Design and synthesis of mono-and di-pyrazolyl-s-triazine derivatives, their anticancer profile in human cancer cell lines, and in vivo toxicity in zebrafish embryos.
Farooq, Muhammad; Sharma, Anamika; Almarhoon, Zainab; Al-Dhfyan, Abudalla; El-Faham, Ayman; Taha, Nael Abu; Wadaan, Mohammad A M; Torre, Beatriz G de la; Albericio, Fernando.
Afiliación
  • Farooq M; Bioproducts Research Chair, College of Science, Department of Zoology, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
  • Sharma A; Catalysis and Peptide Research Unit, School of Health Sciences, University of KwaZulu-Natal, University Road, Westville, Durban 4001, South Africa.
  • Almarhoon Z; Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
  • Al-Dhfyan A; Department of Pharmacology and Toxicology, College of Pharmacy, King Saud University, P. O. Box 2457, Riyadh, Saudi Arabia; Stem Cell & Tissue Re-Engineering, King Faisal Specialist Hospital and Research Center, Riyadh 11211, Saudi Arabia.
  • El-Faham A; Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia; Department of Chemistry, Faculty of Science, Alexandria University, P.O. Box 426, Alexandria 21321, Egypt. Electronic address: aelfaham@ksu.edu.sa.
  • Taha NA; Bioproducts Research Chair, College of Science, Department of Zoology, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
  • Wadaan MAM; Bioproducts Research Chair, College of Science, Department of Zoology, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia.
  • Torre BG; Catalysis and Peptide Research Unit, School of Health Sciences, University of KwaZulu-Natal, University Road, Westville, Durban 4001, South Africa; KRISP, College of Health Sciences, University of KwaZulu-Natal, Westville, Durban 4001, South Africa.
  • Albericio F; Catalysis and Peptide Research Unit, School of Health Sciences, University of KwaZulu-Natal, University Road, Westville, Durban 4001, South Africa; Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia; School of Chemistry and Physics, Universit
Bioorg Chem ; 87: 457-464, 2019 06.
Article en En | MEDLINE | ID: mdl-30927586
s-Triazine is considered a privileged structure, as it is found in several FDA-approved drugs. In the framework of our ongoing medicinal chemistry project based on the use of s-triazine as a scaffold, we synthesized a series of mono- and di-pyrazolyl-s-triazine derivatives and tested them against four human cancer cell lines, namely Human breast carcinoma (MCF 7 and MDA-MB-231), hepatocellular carcinoma (HepG2), colorectal carcinoma (LoVo), and leukemia (K562). The cell viability assay revealed that most of the s-triazine compounds induced cytotoxicity in all four types of human cancer cell lines, however, compounds 4a, and 6g, both of them have a piperidine moiety in their structure were most effective. These two compounds affected the cell viability of cancer cells, with IC50 values within the range between 5 to 9 µM. The cell cycle analysis showed that 4a and 6g induced S and G2/M phase cell cycle arrest in K562 cells. This could be the mechanism by which these molecules induced cytotoxicity in tested cancer cells. The prepared compounds were tested in zebrafish embryos to evaluate in vivo and developmental toxicity of the pyrazolyl-s-triazine derivatives in animals. None of the derivatives were lethal in the concentration range tested.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Triazinas / Diseño de Fármacos / Embrión no Mamífero / Antineoplásicos Límite: Animals / Humans Idioma: En Revista: Bioorg Chem Año: 2019 Tipo del documento: Article País de afiliación: Arabia Saudita Pais de publicación: Estados Unidos
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pirazoles / Triazinas / Diseño de Fármacos / Embrión no Mamífero / Antineoplásicos Límite: Animals / Humans Idioma: En Revista: Bioorg Chem Año: 2019 Tipo del documento: Article País de afiliación: Arabia Saudita Pais de publicación: Estados Unidos