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Synthesis of 1‐Substituted 3‐Aryl‐5‐aryl(hetaryl)‐2‐pyrazolines and Study of Their Antitumor Activity
Author(s) -
Insuasty Braulio,
Chamizo Leidy,
Muñoz Jhon,
Tigreros Alexis,
Quiroga Jairo,
Abonía Rodrigo,
Nogueras Manuel,
Cobo Justo
Publication year - 2012
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.201100170
Subject(s) - aryl , chemistry , pyrazole , thiophene , stereochemistry , in vitro , pyrazoline , cancer cell lines , cancer , cancer cell , medicinal chemistry , biochemistry , medicine , organic chemistry , alkyl
Abstract Three series of novel 1,3,5‐trisubstituted 2‐pyrazoline derivatives containing thiophene and benzodioxol moieties as potential antitumor agents were synthesized. The in vitro antitumor activity of the obtained compounds was determined at the National Cancer Institute (NCI). The 5‐(benzo[ d ][1,3]dioxol‐5‐yl)‐3‐(4‐methoxyphenyl)‐4,5‐dihydro‐1 H ‐pyrazole‐1‐carbothioamide ( 9a ) is the most prominent of the compounds due to its remarkable activity toward leukemia (RPMI‐8226), renal cancer (UO‐31) and prostate cancer (DU‐145) cell lines with GI 50 values of 1.88, 1.91 and 1.94 µM, respectively.