Synthesis and Evaluation of a 3,4-dihydro-2H-benzoxazine Derivative as a Potent CDK9 Inhibitor for Anticancer TherapySynthesis and Evaluation of a 3,4-dihydro-2H-benzoxazine Derivative as a Potent CDK9 Inhibitor for Anticancer Therapy
- Authors
- Song, Taehun; Lee, Moonsub; Bae, Inhwan; Byun, Joo-Yun; Ahn, Young Gil; Kim, Young Hoon; Chun, Young-Jin
- Issue Date
- Mar-2021
- Publisher
- WILEY-V C H VERLAG GMBH
- Keywords
- CDK9 selective inhibitor; Anticancer; 3,4-Dihydro-2H-Benzoxazine derivatives; Transcription
- Citation
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.42, no.3, pp 416 - 419
- Pages
- 4
- Journal Title
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- Volume
- 42
- Number
- 3
- Start Page
- 416
- End Page
- 419
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/52667
- DOI
- 10.1002/bkcs.12204
- ISSN
- 0253-2964
1229-5949
- Abstract
- Cyclin-dependent kinase (CDK) 9 is a protein kinase that plays a major regulatory role in the process of transcription, thereby representing an attractive target in cancer therapy. A series of novel, highly potent, selective derivatives (coined compounds 8-15) were designed, synthesized, and evaluated for their inhibitory effect on CDK functions using cancer cell lines. Here, we showed that our compound 8 exhibited a potent CDK9 inhibitory activity in ICR mice, with an IC50 value of 2.3 nM as well as favorable pharmacokinetic properties. Using an MV4-11 xenograft mouse model, compound 8 showed antitumor efficacy at a dose of 10 mg/kg; compound 8 treatment was well tolerated, with no adverse effects on body weight or animal health. Our in vitro and in vivo findings strongly suggest that compound 8 holds great promise for the development of highly potent CDK9 inhibitors in anticancer approaches.
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