Synthesis of polyenylpyrrole derivatives with selective growth inhibitory activity against T-cell acute lymphoblastic leukemia cells

[Display omitted] 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-deriv...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2021-04, Vol.37, p.127837-127837, Article 127837
Hauptverfasser: Yoshida, Chihiro, Higashi, Tomoya, Hachiro, Yoshifumi, Fujita, Yuki, Yagi, Takuya, Takechi, Azusa, Nakata, Chihiro, Miyashita, Kazuya, Kitada, Nobuo, Saito, Ryohei, Obata, Rika, Hirano, Takashi, Hara, Takahiko, Maki, Shojiro A.
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Sprache:eng
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Zusammenfassung:[Display omitted] 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 μM 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 μM). This compound will be a promising compound for developing T-ALL-specific drugs.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2021.127837