451447-65-7Relevant academic research and scientific papers
Novel hybrids of podophyllotoxin and formononetin inhibit the growth, migration and invasion of lung cancer cells
Yang, Chengli,Xie, Qiongli,Zeng, Xian,Tao, Nengyin,Xu, Yingshu,Chen, Yongzheng,Wang, Jing,Zhang, Lei
, p. 445 - 454 (2019)
In this study, three hybrids of podophyllotoxin and formononetin were synthesized and evaluated for anticancer efficacy. Some of the derivatives exhibited potent cytotoxicity against a panel of human and mouse cancer cell lines, with IC50 value
Podophyllotoxin-pterostilbene fused conjugates as potential multifunctional antineoplastic agents against human uveal melanoma cells
Zhang, Lei,Wang, Jing,Liu, Lai,Zheng, Chengyue,Wang, Yang,Chen, Yongzheng,Wei, Gang
, p. 10601 - 10608 (2017)
Uveal melanoma is the most common primary intraocular malignancy with a high tendency for early metastasis. There is an urgent need for novel anticancer agents for the therapy of uveal melanoma. In this paper, two novel conjugates of podophyllotoxin-pterostilbene were prepared and evaluated for their cytotoxicity against human uveal melanoma cells (MUM-2B and C918) by the CCK-8 assay. Conjugate B1 exhibited a significant IC50 value of 0.081 ± 0.004 μM against MUM-2B cells. Treatment of MUM-2B cells with B1 caused S cell cycle arrest through reductions in CyclinB1, CDK1 and CDK2 levels. In addition, B1 showed antimigratory activity by down-regulating the expression of VEGFR-2 and MMP-2, and up-regulating the level of E-cadherin. Furthermore, B1 treatment resulted in the induction of apoptosis as characterized by Hoechst 33342 staining, flow cytometry and cleavage of procaspases-3, -8, and -9. Finally, B1 significantly inhibited TOPOIIα and TOPOIIβ expression, simultaneously suppressing the ERK1/2 and AKT pathways in MUM-2B cells.
Novel isatin derivatives of podophyllotoxin: Synthesis and cytotoxic evaluation against human leukaemia cancer cells as potent anti-MDR agents
Zhang, Lei,Chen, Fan,Wang, Jing,Chen, Yongzheng,Zhang, Zeguo,Lin, Ya,Zhu, Xinling
, p. 97816 - 97823 (2015)
Multidrug resistance (MDR) is a major cause of chemotherapy failure in cancer therapy. In this study, a series of isatin derivatives of podophyllotoxin were synthesized and evaluated for their cytotoxic activity against human leukemia K562 cells and adriamycin-resistant K562/ADR cells using CCK-8 assay in vitro. All derivatives exhibited higher potency of antiproliferative effects against K562 and K562/ADR cell lines than the control drugs etoposide and adriamycin at nanomolar range, and markedly reduced the resistant factors. Among them, the cytotoxicities exhibited by compounds 8c and 8i were found to comparable or more effective than podophyllotoxin. In particular, 8c exhibited significant cytotoxicity against resistance K562/ADR cells with IC50 value of 0.067 ± 0.010 μM. Furthermore, cell cycle analysis revealed that 8c could remarkably induce K562/ADR cell cycle arrest in the G2/M phase. Meanwhile, the effect of 8c on apoptosis inducing was also observed notably by flow cytometry and Hoechst 33342 staining. Moreover, western blotting analysis suggested that 8c had the potential to overcome the resistance of K562/ADR cells by down-regulating the expression levels of multi-drug resistance-related proteins, such as Pgp, MRP-1 and GST-π.
Nitric oxide donor type podophyllotoxin derivative as well as preparation method and medical application thereof
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Paragraph 0028; 0029, (2018/10/26)
The invention relates to the field of pharmaceutical chemistry, in particular to a nitric oxide donor type podophyllotoxin derivative (I) as well as a preparation method and medical application thereof. As proved by pharmacological experiments, the nitric oxide donor type podophyllotoxin derivative (I) has remarkable anti-tumor cell proliferation activity, and can be applied to clinical preventionor treatment of tumor diseases. The nitric oxide donor type podophyllotoxin derivative (I) is shown in the description.
Application of podophyllotoxin isatin derivative to anti-leukemia drug and preparation method for podophyllotoxin isatin derivative
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Paragraph 0015, (2017/01/26)
The invention discloses a podophyllotoxin isatin derivative as shown in a formula (I) which is described in the specification. The invention also discloses a preparation method for the derivative and application of the derivative to preparation of an anti
