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Some Pyrazole and Pyrazolo[3,4‐ d ]pyrimidine Derivatives: Synthesis and Anticancer Evaluation
Author(s) -
Shamroukh Ahmed H.,
Rashad Aymn E.,
AbdelMegeid Randa E.,
Ali Hatem S.,
Ali Mamdouh M.
Publication year - 2014
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201400064
Subject(s) - pyrazole , chemistry , cytotoxicity , in vitro , doxorubicin , pyrimidine , mcf 7 , stereochemistry , cytotoxic t cell , cell culture , pharmacology , cancer cell , combinatorial chemistry , biochemistry , cancer , chemotherapy , biology , human breast , medicine , genetics
5‐Amino‐1‐ p ‐tolyl‐1 H ‐pyrazole‐4‐carbonitrile ( 1 ) was used for the preparation of some novel pyrazoles and pyrazolo[3,4‐ d ]pyrimidines 2 – 10 . Moreover, the cytotoxicity and in vitro anticancer activities of the prepared compounds were also assessed against the MCF‐7 breast cancer, HepG2 liver cancer, and A549 lung carcinoma cell lines, along with investigation of the effect of the synthesized compounds on the expression of urokinase plasminogen activator (uPA). The tested compounds exhibited remarkable cytotoxic activity against MCF‐7 and HepG2 cells. Among the tested compounds, 2 and 9 revealed promising anticancer activity compared to the activity of the commonly used anticancer drug, doxorubicin, by inhibiting the expression of uPA.