Journal
ACS OMEGA
Volume 6, Issue 7, Pages 4842-4849Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsomega.0c05822
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Funding
- JSPS KAKENHI [18H02583, 17H04325, 18K14344]
- IBM junior faculty grant
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Newly synthesized bi-naphthyl derivatives 2 and 3 exhibited stronger inhibitory effects on androgen-independent prostate cancer cell lines compared to the parent molecule, showing potential as lead compounds for cancer treatment.
To improve the biological effects of the lead compound 5'-chloro-2,2'-dihydroxychalcone (CI-DHC), bicyclic aromatic chalcones were designed, synthesized, and evaluated against androgen-independent prostate cancer (PCa) DU145 and PC-3 cell proliferation. Newly synthesized bi-naphthyl derivatives 2 and 3 suppressed the proliferation of these two cell lines and also taxane-resistant prostate cancer cell lines at a submicromolar level. The two compounds were 4-18 times more potent than the parent molecule Cl-DHC. A structure-activity relationship analysis revealed that the orientation of the 10g-electron ring-A naphthalene had a significant effect on the activity. Mode-of-action studies in KB-VIN cells demonstrated that 2 and 3 arrested cells in mitosis at prometaphase and metaphase followed by induction of sub-G1 accumulation. Thus, 2 and 3 have good potential as leads for continued development of treatments for cancers especially for not only androgen-independent PCa but also multidrug-resistant tumors.
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