Synthesis, cytotoxicity, and molecular properties prediction of novel 1,3-diarylpyrazole derivatives

A novel combinatorial library of ester and amide derivatives of 1,3-diarylpyrazoles was designed and synthesized. Anticancer activities of these compounds were assessed against MCF7, MDA-MB-231, HeLa, Raji, and HL60 human cancer cells by MTT assay. Out of these, compounds 4c and 5f were found as the...

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Bibliographic Details
Published inMedicinal chemistry research Vol. 22; no. 10; pp. 4893 - 4908
Main Authors Baytas, Sultan Nacak, Inceler, Nazan, Yılmaz, Akın
Format Journal Article
LanguageEnglish
Published Boston Springer US 01.10.2013
Subjects
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Original Research
Pharmacology/Toxicology
1
Synthesis
Pyridine
MTT
Pyrazoles
Anticancer activity
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Summary:A novel combinatorial library of ester and amide derivatives of 1,3-diarylpyrazoles was designed and synthesized. Anticancer activities of these compounds were assessed against MCF7, MDA-MB-231, HeLa, Raji, and HL60 human cancer cells by MTT assay. Out of these, compounds 4c and 5f were found as the most promising anticancer agents with IC 50 values of 8.12 and 9.63 μM in Raji cells, respectively. All compounds exhibited suitable drug-like characteristics according to Lipinski’s rule.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-013-0505-8