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1.
Pigment Cell Melanoma Res ; 36(6): 588-593, 2023 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-37819763

RESUMEN

The Society for Melanoma Research (SMR) was created 20 years ago and has unequivocally contributed to the vast progress of the field, particularly for the treatment of melanoma patients with metastatic disease by facilitating synergistic collaborations between clinicians, researchers at the bench, and industry. In commemoration of the 20th anniversary of the first SMR International Congress (held in 2003 in Philadelphia), we look to the future by highlighting the perspectives of the next generation of rising stars, medical, and graduate students across six continents.


Asunto(s)
Melanoma , Humanos , Melanoma/terapia , Melanoma/patología
2.
Bioorg Med Chem Lett ; 52: 128393, 2021 11 15.
Artículo en Inglés | MEDLINE | ID: mdl-34606997

RESUMEN

In the current study a late-stage diversification of unactivated olefins labd-8(17)-en-15-oic acid (1a) and methyl labd-8(17)-en-15-oate (1b) via Heck-Matsuda arylation is described. The reaction provided straightforward and practical access to a series of novel aryl-labdane-type derivatives (HM adducts 3a-h) in moderate to good yields in a highly regio- and stereoselective manner at room temperature under air atmosphere. The cytotoxic activity of these compounds was investigated in vitro against three different human cell lines (THP-1, K562, MCF-7). Of these, HM adduct 3h showed a selective effect in all cancer cell lines tested and was selected for extended biological investigations in a leukemia cell line (K562), which demonstrated that the cytotoxic/antiproliferative activity observed in this compound might be mediated by induction of cell cycle arrest at the sub-G1 phase and by autophagy-induced cell death. Taken together, these findings indicate that further investigation into the anticancer activity against chronic myeloid leukemia from aryl-labdane-type derivatives may be fruitful.


Asunto(s)
Antineoplásicos/farmacología , Diterpenos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Línea Celular Tumoral , Proliferación Celular/efectos de los fármacos , Diterpenos/síntesis química , Diterpenos/química , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Estructura Molecular , Especies Reactivas de Oxígeno/metabolismo , Relación Estructura-Actividad
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