35711-41-2Relevant academic research and scientific papers
Synthesis, structure and in vitro anti-trypanosomal activity of non-toxic arylpyrrole-based chalcone derivatives
Hoppe, Heinrich C.,Isaacs, Michelle,Khanye, Setshaba D.,Kruger, Cuan,Oderinlo, Ogunyemi O.,Smith, Vincent J.,Veale, Clinton G. L.,Zulu, Ayanda I.
, (2020/04/10)
With an intention of identifying chalcone derivatives exhibiting anti-protozoal activity, a cohort of relatively unexplored arylpyrrole-based chalcone derivatives were synthesized in moderate to good yields. The resultant compounds were evaluated in vitro for their potential activity against a cultured Trypanosoma brucei brucei 427 strain. Several compounds displayed mostly modest in vitro anti-trypanosomal activity with compounds 10e and 10h emerging as active candidates with IC50 values of 4.09 and 5.11 μM, respectively. More importantly, a concomitant assessment of their activity against a human cervix adenocarcinoma (HeLa) cell line revealed that these compounds are non-toxic.
ANDROGEN RECEPTOR ANTAGONISTS
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, (2019/08/26)
Compounds that inhibit the androgen receptor, pharmaceutical compositions comprising one or more of the compounds, as well as methods of treating cancer using such compounds are described.
