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Molecules 2019, 24(3), 624; https://doi.org/10.3390/molecules24030624

Nanoformulation of a Novel Pyrano[2,3-c] Pyrazole Heterocyclic Compound AMDPC Exhibits Anti-Cancer Activity via Blocking the Cell Cycle through a P53-Independent Pathway

Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, China
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editors: Alejandro Baeza, Fernando Novio and Juan Luis Paris
Received: 12 January 2019 / Revised: 2 February 2019 / Accepted: 6 February 2019 / Published: 11 February 2019
(This article belongs to the Special Issue Nanomaterials for Cancer Diagnosis and Therapy)
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Abstract

Pyrano[2,3-c]pyrazole derivatives have been reported as exerting various biological activities. One compound with potential anti-tumor activity was screened out by MTT assay from series of dihydropyrazopyrazole derivatives we had synthesized before using a one-pot, four-component reaction, and was named as 6-amino-4-(2-hydroxyphenyl)-3-methyl-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile (hereinafter abbreviated as AMDPC). The IC50 of AMDPC against Bcap-37 breast cancer cells was 46.52 μg/mL. Then the hydrophobic AMDPC was encapsulated in PEG-PLGA block copolymers, and then self-assembled as polymeric micelle (mPEG-PLGA/AMDPC) to improve both physiochemical and release profiles. The effect of mPEG-PLGA/AMDPC on BCAP-37 cancer cells showed similar anti-tumor effects as AMDPC. Furthermore, the anti-tumor mechanism of mPEG-PLGA/AMDPC was investigated, which can probably be attributed to stimulating the expression of P21 gene and therefore protein production on BCAP-37 cells, and then blocked the cell cycle through the P53-independent pathway both in S phase and G2 phase. Thus, mPEG-PLGA/AMDPC is a promising therapeutic agent for cancer treatment, and further in vivo studies will be developed. View Full-Text
Keywords: Pyrano[2,3-c]pyrazole derivatives; nanoformulation; inhibition of cancer cell growth; P21-related S phase and G2 phase arrest Pyrano[2,3-c]pyrazole derivatives; nanoformulation; inhibition of cancer cell growth; P21-related S phase and G2 phase arrest
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Sun, X.; Zhang, L.; Gao, M.; Que, X.; Zhou, C.; Zhu, D.; Cai, Y. Nanoformulation of a Novel Pyrano[2,3-c] Pyrazole Heterocyclic Compound AMDPC Exhibits Anti-Cancer Activity via Blocking the Cell Cycle through a P53-Independent Pathway. Molecules 2019, 24, 624.

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