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3. DHQZ-17, a potent inhibitor of the transcription factor HNF4A, suppresses tumorigenicity of head and neck squamous cell carcinoma in vivo

Author

Ganesh Venkatraman, Kumarswamyreddy Nandarapu, Shilpa Tentu, Prakash Muthuraj, Suresh K. Rayala, and Kesavan Venkitasamy

Subjects
0301 basic medicine, Programmed cell death, Time Factors, Cell cycle checkpoint, Physiology, Clinical Biochemistry, Mice, Nude, Antineoplastic Agents, Apoptosis, Inhibitory Concentration 50, 03 medical and health sciences, 0302 clinical medicine, Cell Line, Tumor, medicine, Animals, Humans, Cytotoxicity, Transcription factor, Cell Proliferation, Quinazolinones, Dose-Response Relationship, Drug, Squamous Cell Carcinoma of Head and Neck, Chemistry, Cell growth, Cell Cycle Checkpoints, Cell Biology, medicine.disease, Xenograft Model Antitumor Assays, Head and neck squamous-cell carcinoma, 030104 developmental biology, Hepatocyte Nuclear Factor 4, Head and Neck Neoplasms, Cell culture, 030220 oncology & carcinogenesis, Carcinoma, Squamous Cell, Cancer research, Female
Abstract

A series of 2, 3-dihydroquinazolinone derivatives were synthesized, characterized and their anticancer activity was determined. Among the compounds synthesized and screened, one compound (17) showed potent anticancer activity against human head and neck squamous cell carcinoma cell line, SCC131 and was non-toxic to normal cells. The compound inhibited the growth of SCC131 cells, with an IC50 of 1.75 μM, triggered apoptotic mode of cell death and caused tumor regression of SCC131 tumor xenografts in athymic mice. To decipher the target for the lead compound, a high throughput qPCR array was performed. Results showed that the compound 17, inhibited the expression of a vital transcription factor HNF4A, involved in regulation of metabolic pathways. Thus, the present work has identified a lead compound 17, with potent anticancer activity, minimal normal cell toxicity and a plausible target and hence definitely holds future prospects as an anticancer agent.

Published
2017
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