Design and synthesis of some new tri-substituted pyrazole derivatives as anticancer agents

作者：Fahmy Hoda H; Srour Aladdin M^*; Ismail Mohamed A; Khater Mai A; Serrya Rabah A; El Manawaty May A

来源：Research on Chemical Intermediates, 2016, 42(9): 6881-6892.

DOI：10.1007/s11164-016-2502-2

• Tri-substituted pyrazole
• Vilsmeier-Haack
• Antiproliferative
• Anticancer

A new series of tri-substituted pyrazole derivatives were designed as anti-cancer agents and synthesized, starting with the formylation of semicarbazone via the Vilsmeier-Haack reaction to give 3-(4-bromophenyl)-1H-pyrazole-4-carbaldehyde I which was the precursor of compounds 1-9. The new chemical entities were screened for their anti-cancer activity on various human cancer cell lines, namely: hepatocellular carcinoma HepG2, breast cancer MCF-7, lung carcinoma A549 and prostatic cancer PC3. Most of the synthesized compounds showed remarkable activity on the tested cell lines, while compound 2 had the highest potency against the HepG2 cell line with an IC50 of 9.13 mu M compared with doxorubicin (IC50 = 34.24 mu M), the reference standard used in this study, and compound 7 was the most active on the rest of the three cell lines; MCF-7, A549 and PC3 (IC50 = 16.52, 6.52 and 9.13 mu M, respectively) relative to IC50 = 20.85, 5.93 and 38.02 mu M of the standard. Thus, some of the synthesized tri-substituted pyrazole derivatives, specially 2 and 7, have the potential to be developed into potent anticancer agents.

• 出版日期2016-9