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Polymethoxy-/polyacetyl-flavones cytotoxicity towards colorectal and prostate cancer cell lines: SAR, mechanisms of action and evaluation as potential adjuvants in chemotherapy.

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Bioorganic & medicinal chemistry letters 📖 저널 OA 8.1% 2022: 0/1 OA 2023: 0/1 OA 2024: 0/2 OA 2025: 2/22 OA 2026: 3/36 OA 2022~2026 2025 Vol.130() p. 130404
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Tenta R, Gioti K, Dumontet V, Picot L, Grougnet R

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A set of natural and semi-synthetic polymethoxy- and polyacetyl-flavones (PMFs/PAFs) was evaluated towards colorectal (HCT116) and prostate (PC-3) cancer cells.

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APA Tenta R, Gioti K, et al. (2025). Polymethoxy-/polyacetyl-flavones cytotoxicity towards colorectal and prostate cancer cell lines: SAR, mechanisms of action and evaluation as potential adjuvants in chemotherapy.. Bioorganic & medicinal chemistry letters, 130, 130404. https://doi.org/10.1016/j.bmcl.2025.130404
MLA Tenta R, et al.. "Polymethoxy-/polyacetyl-flavones cytotoxicity towards colorectal and prostate cancer cell lines: SAR, mechanisms of action and evaluation as potential adjuvants in chemotherapy.." Bioorganic & medicinal chemistry letters, vol. 130, 2025, pp. 130404.
PMID 40957467 ↗

Abstract

A set of natural and semi-synthetic polymethoxy- and polyacetyl-flavones (PMFs/PAFs) was evaluated towards colorectal (HCT116) and prostate (PC-3) cancer cells. The most active compounds were then combined with 5-fluorouracil (5-FU) or with adriamycin (ADR) in order to determine a potential synergism, focusing on contingent changes in cell cycle and apoptosis. Two derivatives were strongly cytotoxic. They also induced G0/G1 cell cycle arrest, but differently behaved when combined to the reference drugs 5-FU or ADR. The induction of apoptosis was stronger towards HCT116, noticeably increasing the activity of 5-FU, suggesting a potential additive effect. Besides, the results of soluble caspase-cleaved K18 showed that another phenomenon such as autophagy may be involved towards PC-3 cells and should be deciphered. Consequently, these two PMFs are considered as suitable candidates for further studies in hit-to‑lead approach, in a context of a therapeutic protocol involving natural products as chemosensitizers, aiming to increase the potency and to reduce the side effects of antitumor drugs.

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