Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 37, Issue -, Pages -Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2021.127837
Keywords
T-ALL; Structure-activity relationships; Inhibitor; Rumbrin; Auxarconjugatin-B
Categories
Funding
- AMED [JP18lm0203004]
- JSPS KAKENHI [JP17H06371, JP18K05075]
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T-cell acute lymphoblastic leukemia (T-ALL) is a challenging disease to cure, but a synthesized octatetraenylpyrrole analog has shown promising growth-inhibiting activity specifically in T-ALL-derived cells, making it a potential candidate for developing targeted drugs.
T-cell acute lymphoblastic leukemia (T-ALL) is a hardly curable disease with a high relapse rate. 20 analogs were synthesized based on the structures of two kinds of fungi-derived polyenylpyrrole products (rumbrin (1) and auxarconjugatin-B (2)) to suppress the growth of T-ALL-derived cell line CCRF-CEM and tested for growth-inhibiting activity. The octatetraenylpyrrole analog gave an IC50 of 0.27 mu M in CCRF-CEM cells, while it did not affect Burkitt lymphoma-derived cell line Raji and the cervical cancer cell line HeLa, or the oral cancer cell line HSC-3 (IC50 > 10 mu M). This compound will be a promising compound for developing T-ALL-specific drugs.
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