Synthesis and evaluation of aporphinoid 5-HTR ligands as inhibitors of PC3 prostate cancer cell growth.
1/5 보강
Aporphines are a class of isoquinoline alkaloids that are endowed with a range of biological activities.
APA
Okpattah D, Karki A, et al. (2025). Synthesis and evaluation of aporphinoid 5-HTR ligands as inhibitors of PC3 prostate cancer cell growth.. Bioorganic & medicinal chemistry letters, 128, 130328. https://doi.org/10.1016/j.bmcl.2025.130328
MLA
Okpattah D, et al.. "Synthesis and evaluation of aporphinoid 5-HTR ligands as inhibitors of PC3 prostate cancer cell growth.." Bioorganic & medicinal chemistry letters, vol. 128, 2025, pp. 130328.
PMID
40633811 ↗
Abstract 한글 요약
Aporphines are a class of isoquinoline alkaloids that are endowed with a range of biological activities. The 5-HT7R is an emerging biological target for prostate cancer therapeutics. In this manuscript, we report the synthesis and evaluation of aporphine enantiomers as 5-HT7R ligands, as well as their activity in inhibiting the proliferation of prostate cancer cells (specifically, PC3). The (S)-enantiomers displayed higher affinity at the 5-HT7R than the racemates and the (R)-enantiomer counterparts. The (S)-enantiomers were found to be antagonists at the 5-HT7R. Racemates as well as their respective enantiomers were selective for the 5-HT7R receptor over other serotonin and dopamine receptors evaluated. In the anticancer activity assays, the compounds showed more potent cytotoxic effects than the selective 5-HT7R antagonist control SB269970. However, no correlation was observed between the 5-HT7R affinity or 5-HT7R antagonist activity and anticancer potency, suggesting that other non-5-HT7R mechanisms play a role in the anticancer effects of the compounds. Compounds (R)-1 and (R)-4 were identified as the most potent anti-proliferative compounds and will be useful as lead molecules for prostate cancer therapeutic development in future studies.
🏷️ 키워드 / MeSH 📖 같은 키워드 OA만
- Humans
- Male
- Antineoplastic Agents
- Aporphines
- Cell Line
- Tumor
- Cell Proliferation
- Dose-Response Relationship
- Drug
- Drug Screening Assays
- Antitumor
- Ligands
- Molecular Structure
- PC-3 Cells
- Prostatic Neoplasms
- Receptors
- Serotonin
- Serotonin Antagonists
- Stereoisomerism
- Structure-Activity Relationship
- Isoquinolines
- Alkaloids
- 5-HT7R
- Anti-proliferation
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🏷️ 같은 키워드 · 무료전문 — 이 논문 MeSH/keyword 기반
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