Design, synthesis, and structure-activity relationships of new benzofuro[3,2-b]pyridin-7-ols as DNA topoisomerase II inhibitors
- 주제(키워드) Antiproliferative activity , Benzofuro[3 , 2-b]pyridin-7-ol , Fused heterocycles , Hydroxyl-substituent , Structure-activity relationship , Topoisomerase inhibition
- 등재 SCIE, SCOPUS
- 발행기관 Elsevier Ltd
- 발행년도 2018
- URI http://www.dcollection.net/handler/ewha/000000150100
- 본문언어 영어
- Published As http://dx.doi.org/10.1016/j.bmcl.2018.01.048
- 저작권 이화여자대학교 논문은 저작권에 의해 보호받습니다.
초록/요약
Human DNA topoisomerases have become attractive targets for developing more effective anticancer drugs. In this study, a series of new benzofuro[3,2-b]pyridin-7-ols were designed and synthesized for the first time and screened for their topoisomerase I and II inhibitory and antiproliferative activity. Structure-activity relationships revealed the position of ortho- and para-hydroxyl group at 2-phenyl ring, and meta-hydroxyl group at 4-phenyl ring of benzofuro[3,2-b]pyridin-7-ol are important for potent and selective topo II inhibitory activity. Compound 11 showed the most selective and potent topo II inhibition (100% inhibition at 100 µM) and strongest antiproliferative activity (IC50 = 0.86 µM) than all the positive controls in HeLa cell line. © 2018 Elsevier Ltd
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