A series of symmetrical disubstituded 1,8-diamidoanthraquinones were synthesized and evaluated for anti-proliferation, telomerase inhibitory by TRAP assay, and hTERT expression by SEAP assay. All of the compounds tested, except for compounds 3a and 3s were selected by the NCI screening system. In addition, compounds 4e and 4k exhibited inhibitory effects on telomerase activity. Taken together, our findings indicated that the analysis of cytotoxicity and telomerase inhibition might provide information applicable for further developing potential telomerase targeting strategy.
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http://dx.doi.org/10.1016/j.ejmech.2012.01.044 | DOI Listing |
Bioorg Med Chem Lett
December 2024
Department of Medicinal Chemistry and Natural Medicine Chemistry, College of Pharmacy, HarBin Medical University, Harbin, PR China. Electronic address:
The telomeric G-quadruplex (G4) along with the telomerase catalytic subunit hTERT are crucial in the extension of telomeres. Tumor cells can establish replicative immortality by activating the telomere-maintenance mechanism (TMM).Small molecule ligands can limit cancer telomere lengthening by by targeting at G4 and hTERT.
View Article and Find Full Text PDFInt J Mol Sci
December 2024
Department of Ophthalmology, University Hospital, Martin-Luther-University Halle-Wittenberg, 06120 Halle (Saale), Germany.
Local anesthetics are commonly used in ophthalmic surgery. However, their use can affect the healing process. This study aimed to investigate the potential impact of anesthetic substances at clinically relevant concentrations and incubation times (3 min), specifically oxybuprocaine (OBPC, 0.
View Article and Find Full Text PDFTransl Cancer Res
September 2024
Huzhou Key Laboratory of Precise Prevention and Control of Major Chronic Diseases, School of Medicine, Huzhou University, Huzhou, China.
Background: Telomerase is activated in most cancer cells, and thus telomerase is an ideal target for cancer therapy. The human liver-associated candidate tumour suppressor LPTS/PinX1, is the only human protein reported to bind with the telomerase catalytic subunit telomerase reverse transcriptase (TERT) and inhibit telomerase activity. The C-terminal fragment of LPTS/PinX1 (LPTS/PinX1290-328) contains a telomerase inhibitory domain that is needed for inhibition of telomere elongation and induction of apoptosis.
View Article and Find Full Text PDFBioorg Chem
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Mashreq, Baghdad 10023, Iraq; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Horus University-Egypt, New Damietta 34518, Egypt. Electronic address:
In this work, additional effort was applied to design new BIBR1532-based analogues with potential inhibitory activity against telomerase and acting as multitarget antitumor candidates to overcome the resistance problem. Therefore, novel substituted N-phenyl-2-((6-phenylpyridazin-3-yl)thio)acetamide candidates (4a-n) were synthesized. Applying the lead optimization strategy of the previously designed compound 8e; compound 4l showed an improved telomerase inhibition of 64.
View Article and Find Full Text PDFTissue Cell
December 2024
Department of Histology and Embryology, Dali University, Dali, China; Yunnan Provincial Key Laboratory of Entomological Biopharmaceutical R&D, Dali University, Dali, China.
This study aimed to investigate effect of Periplaneta americana extract CII-3 (CII-3) in senescence of SKOV3 cells. Proliferation, colony forming and cell senescence of SKOV3 cells were determined. ROS production was evaluated by flow cytometry.
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