Next Article in Journal / Special Issue
Contrast-Enhanced Ultrasonography for Screening and Diagnosis of Hepatocellular Carcinoma: A Case Series and Review of the Literature
Previous Article in Journal / Special Issue
Minimising Blood Stream Infection: Developing New Materials for Intravascular Catheters
Review

Development of Newly Synthesized Chromone Derivatives with High Tumor Specificity against Human Oral Squamous Cell Carcinoma

1
Department of Pharmaceutical Sciences, Faculty of Pharmacy and Pharmaceutical Sciences, Josai University, Saitama 350-0295, Japan
2
Department of Medical Molecular Informatics, Meiji Pharmaceutical University, Tokyo 204-858, Japan
3
Department of Oral and Maxillofacial Surgery, Saitama Medical Center, Saitama Medical University, Kawagoe 350-8550, Japan
4
Division of Applied Pharmaceutical Education and Research, Hoshi University, Tokyo 142-8501, Japan
5
Meikai University Research Institute of Odontology (M-RIO), 1-1 Keyakidai, Sakado, Saitama 350-0283, Japan
*
Authors to whom correspondence should be addressed.
Received: 3 August 2020 / Revised: 23 August 2020 / Accepted: 24 August 2020 / Published: 26 August 2020
Since many anticancer drugs show severe adverse effects such as mucositis, peripheral neurotoxicity, and extravasation, it was crucial to explore new compounds with much reduced adverse effects. Comprehensive investigation with human malignant and nonmalignant cells demonstrated that derivatives of chromone, back-bone structure of flavonoid, showed much higher tumor specificity as compared with three major polyphenols in the natural kingdom, such as lignin-carbohydrate complex, tannin, and flavonoid. A total 291 newly synthesized compounds of 17 groups (consisting of 12 chromones, 2 esters, and 3 amides) gave a wide range of the intensity of tumor specificity, possibly reflecting the fitness for the optimal 3D structure and electric state. Among them, 7-methoxy-3-[(1E)-2-phenylethenyl]-4H-1-benzopyran-4-one (compound 22), which belongs to 3-styrylchromones, showed the highest tumor specificity. 22 induced subG1 and G2 + M cell population in human oral squamous cell carcinoma cell line, with much less keratinocyte toxicity as compared with doxorubicin and 5-FU. However, 12 active compounds selected did not necessarily induce apoptosis and mitotic arrest. This compound can be used as a lead compound to manufacture more active compound. View Full-Text
Keywords: chromone; tumor specificity; QSAR analysis; apoptosis; cell cycle analysis chromone; tumor specificity; QSAR analysis; apoptosis; cell cycle analysis
Show Figures

Figure 1

MDPI and ACS Style

Sugita, Y.; Takao, K.; Uesawa, Y.; Nagai, J.; Iijima, Y.; Sano, M.; Sakagami, H. Development of Newly Synthesized Chromone Derivatives with High Tumor Specificity against Human Oral Squamous Cell Carcinoma. Medicines 2020, 7, 50. https://0-doi-org.brum.beds.ac.uk/10.3390/medicines7090050

AMA Style

Sugita Y, Takao K, Uesawa Y, Nagai J, Iijima Y, Sano M, Sakagami H. Development of Newly Synthesized Chromone Derivatives with High Tumor Specificity against Human Oral Squamous Cell Carcinoma. Medicines. 2020; 7(9):50. https://0-doi-org.brum.beds.ac.uk/10.3390/medicines7090050

Chicago/Turabian Style

Sugita, Yoshiaki, Koichi Takao, Yoshihiro Uesawa, Junko Nagai, Yosuke Iijima, Motohiko Sano, and Hiroshi Sakagami. 2020. "Development of Newly Synthesized Chromone Derivatives with High Tumor Specificity against Human Oral Squamous Cell Carcinoma" Medicines 7, no. 9: 50. https://0-doi-org.brum.beds.ac.uk/10.3390/medicines7090050

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop