title: Synthesis and in vitro biological evaluation of novel pyrazole derivatives as potential antitumor agents.
abstract: The synthesis of twenty seven novel pyrazole derivatives bearing aryl substituted groups at positions 1 and 3 of the pyrazole structural motif and various functional groups at position 4 is presented. The critical step for their synthesis is the TCT/DMF promoted cyclization of the corresponding hydrazine precursors, which provided the desired pyrazole skeleton. The anticancer properties of the novel pyrazole derivatives were evaluated in vitro against human prostate (DU145), melanoma (A2058) and breast cancer (MCF-7) cell lines. Among the compounds tested, pyrazole 5a and its methoxy derivatives 3d,e were assayed as the most potent, displaying selective activity against the MCF-7 cell line with IC(50) values of 14, 10 and 12 µM respectively. Results herein indicate that the reported backbone represents a promising structural lead for further development as antitumor agents.
authors: Chemistry Laboratory, Agricultural University of Athens, Iera odos 75, Athens 11855, Greece.
authors: Michael S
authors: MS
authors: Christodoulou
authors: Nikolas
authors: N
authors: Fokialakis
authors: Sangkil
authors: S
authors: Nam
authors: Richard
authors: R
authors: Jove
authors: Alexios-Leandros
authors: AL
authors: Skaltsounis
authors: Serkos A
authors: SA
authors: Haroutounian
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003500:Cyclization; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005260:Female; D006801:Humans; D006834:Hydrazines / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D008297:Male; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D006834:Hydrazines; D011720:Pyrazoles