Prenylated Chalcones as Anticancer Agents Against Castration-Resistant Prostate Cancer
Prenylated chalcones have garnered attention as potential anticancer agents due to their ability to modulate multiple cancer-related pathways. In this study, we synthesized and evaluated nine novel prenylated chalcone derivatives for their antiproliferative effects against castration-resistant prost...
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| Format: | Article |
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MDPI AG
2025-06-01
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| Series: | Scientia Pharmaceutica |
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| Online Access: | https://www.mdpi.com/2218-0532/93/2/25 |
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| author | Marcos Morales-Reyna Elisa Elvira Figueroa-Angulo José Espinoza-Hicks Alejandro Camacho-Dávila César López-Camarillo Laura Isabel Vázquez-Carrillo Alfonso Salgado-Aguayo Ángeles Carlos-Reyes Violeta Deyanira Álvarez-Jiménez Jonathan Puente-Rivera María Elizbeth Alvarez-Sánchez |
| author_facet | Marcos Morales-Reyna Elisa Elvira Figueroa-Angulo José Espinoza-Hicks Alejandro Camacho-Dávila César López-Camarillo Laura Isabel Vázquez-Carrillo Alfonso Salgado-Aguayo Ángeles Carlos-Reyes Violeta Deyanira Álvarez-Jiménez Jonathan Puente-Rivera María Elizbeth Alvarez-Sánchez |
| author_sort | Marcos Morales-Reyna |
| collection | DOAJ |
| description | Prenylated chalcones have garnered attention as potential anticancer agents due to their ability to modulate multiple cancer-related pathways. In this study, we synthesized and evaluated nine novel prenylated chalcone derivatives for their antiproliferative effects against castration-resistant prostate cancer (CRPC) cell lines, DU145 and PC3. Among these, compounds 6d and 7j demonstrated potent cytotoxic activity, with IC<sub>50</sub> values comparable to cisplatin, and exhibited selective toxicity towards cancer cells over non-tumorigenic RWPE-1 cells. Mechanistic investigations revealed that these compounds induce apoptosis via mitochondrial membrane depolarization and increased late apoptotic events. Flow cytometry confirmed activation of both early and late apoptotic pathways. These findings highlight the potential of chalcone derivatives 6d and 7j as promising therapeutic candidates for CRPC treatment and support further development of chalcone-based molecules in precision oncology. |
| format | Article |
| id | doaj-art-ec83ac9e3e2e46108e9c5f82eccf4fea |
| institution | Kabale University |
| issn | 0036-8709 2218-0532 |
| language | English |
| publishDate | 2025-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Scientia Pharmaceutica |
| spelling | doaj-art-ec83ac9e3e2e46108e9c5f82eccf4fea2025-08-20T03:27:25ZengMDPI AGScientia Pharmaceutica0036-87092218-05322025-06-019322510.3390/scipharm93020025Prenylated Chalcones as Anticancer Agents Against Castration-Resistant Prostate CancerMarcos Morales-Reyna0Elisa Elvira Figueroa-Angulo1José Espinoza-Hicks2Alejandro Camacho-Dávila3César López-Camarillo4Laura Isabel Vázquez-Carrillo5Alfonso Salgado-Aguayo6Ángeles Carlos-Reyes7Violeta Deyanira Álvarez-Jiménez8Jonathan Puente-Rivera9María Elizbeth Alvarez-Sánchez10Laboratorio de Patogénesis Celular y Molecular Humana y Veterinaria, Posgrado en Ciencias Genómicas, Universidad Autónoma de la Ciudad de México, Ciudad de México 03100, MexicoLaboratorio de Patogénesis Celular y Molecular Humana y Veterinaria, Posgrado en Ciencias Genómicas, Universidad Autónoma de la Ciudad de México, Ciudad de México 03100, MexicoFacultad de Ciencias Químicas, Universidad Autónoma de Chihuahua, México, Circuito Universitario s/n, Campus Universitario II, Chihuahua 31125, MexicoFacultad de Ciencias Químicas, Universidad Autónoma de Chihuahua, México, Circuito Universitario s/n, Campus Universitario II, Chihuahua 31125, MexicoPosgrado en Ciencias Genómicas, Universidad Autónoma de la Ciudad de México, Ciudad de México 03100, MexicoLaboratorio de Patogénesis Celular y Molecular Humana y Veterinaria, Posgrado en Ciencias Genómicas, Universidad Autónoma de la Ciudad de México, Ciudad de México 03100, MexicoLaboratorio de Investigación en Enfermedades Reumáticas, Instituto Nacional de Enfermedades Respiratorias, Ciudad de México 14080, MexicoLaboratorio de Investigación en Enfermedades Reumáticas, Instituto Nacional de Enfermedades Respiratorias, Ciudad de México 14080, MexicoLaboratorio de Biología Molecular y Bioseguridad Nivel 3, Centro Médico Naval-SEMAR, Ciudad de México 04470, MexicoLaboratorio de Patogénesis Celular y Molecular Humana y Veterinaria, Posgrado en Ciencias Genómicas, Universidad Autónoma de la Ciudad de México, Ciudad de México 03100, MexicoLaboratorio de Patogénesis Celular y Molecular Humana y Veterinaria, Posgrado en Ciencias Genómicas, Universidad Autónoma de la Ciudad de México, Ciudad de México 03100, MexicoPrenylated chalcones have garnered attention as potential anticancer agents due to their ability to modulate multiple cancer-related pathways. In this study, we synthesized and evaluated nine novel prenylated chalcone derivatives for their antiproliferative effects against castration-resistant prostate cancer (CRPC) cell lines, DU145 and PC3. Among these, compounds 6d and 7j demonstrated potent cytotoxic activity, with IC<sub>50</sub> values comparable to cisplatin, and exhibited selective toxicity towards cancer cells over non-tumorigenic RWPE-1 cells. Mechanistic investigations revealed that these compounds induce apoptosis via mitochondrial membrane depolarization and increased late apoptotic events. Flow cytometry confirmed activation of both early and late apoptotic pathways. These findings highlight the potential of chalcone derivatives 6d and 7j as promising therapeutic candidates for CRPC treatment and support further development of chalcone-based molecules in precision oncology.https://www.mdpi.com/2218-0532/93/2/25chalconesprostate cancerdrug resistanceanticancer activity |
| spellingShingle | Marcos Morales-Reyna Elisa Elvira Figueroa-Angulo José Espinoza-Hicks Alejandro Camacho-Dávila César López-Camarillo Laura Isabel Vázquez-Carrillo Alfonso Salgado-Aguayo Ángeles Carlos-Reyes Violeta Deyanira Álvarez-Jiménez Jonathan Puente-Rivera María Elizbeth Alvarez-Sánchez Prenylated Chalcones as Anticancer Agents Against Castration-Resistant Prostate Cancer Scientia Pharmaceutica chalcones prostate cancer drug resistance anticancer activity |
| title | Prenylated Chalcones as Anticancer Agents Against Castration-Resistant Prostate Cancer |
| title_full | Prenylated Chalcones as Anticancer Agents Against Castration-Resistant Prostate Cancer |
| title_fullStr | Prenylated Chalcones as Anticancer Agents Against Castration-Resistant Prostate Cancer |
| title_full_unstemmed | Prenylated Chalcones as Anticancer Agents Against Castration-Resistant Prostate Cancer |
| title_short | Prenylated Chalcones as Anticancer Agents Against Castration-Resistant Prostate Cancer |
| title_sort | prenylated chalcones as anticancer agents against castration resistant prostate cancer |
| topic | chalcones prostate cancer drug resistance anticancer activity |
| url | https://www.mdpi.com/2218-0532/93/2/25 |
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