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

Synthesis of polyenylpyrrole derivatives with selective growth inhibitory activity against T-cell acute lymphoblastic leukemia cells.
Bioorg Med Chem Lett. 2021 Feb 10;:127837
Authors: Yoshida C, Higashi T, Hachiro Y, Fujita Y, Yagi T, Takechi A, Nakata C, Miyashita K, Kitada N, Saito R, Obata R, Hirano T, Hara T, Maki SA
Abstract
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.
PMID: 33581250 [PubMed - as supplied by publisher]

Source: Bioorganic and Medicinal Chemistry Letters - February 10, 2021 Category: Chemistry Authors: Yoshida C, Higashi T, Hachiro Y, Fujita Y, Yagi T, Takechi A, Nakata C, Miyashita K, Kitada N, Saito R, Obata R, Hirano T, Hara T, Maki SA Tags: Bioorg Med Chem Lett Source Type: research