Androstane-3β-O-sulfonate 및 -sulfamate 유도체 합성과 steroid sulfatase 저해효과

• 영문명: Synthesis and Steroid Sulfatase Inhibitory Effect of Androstane-3β-O-sulfonate and -sulfamate Derivatives
• 발행기관: 대한약학회
• 저자명: 박지현(Ji-Hyun Park) 마은숙(Eunsook Ma)
• 간행물 정보: 『약학회지』제62권 제6호(2018년), 401~409쪽, 전체 9쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2018.12.31

영문 초록

The development of potent steroid sulfatase inhibitors is an important new therapeutic strategy for the treatment of postmenopausal women with breast cancer. In postmenopausal breast cancer, the desulfation of dehydroepiandrostene sulfate (DHEAS) by steroid sulfatase (STS) that takes place in peripheral tissues becomes as an important step in estrogen production. Androstane-3β-O-mesylsulfonate, -3β-O-tosylsulfonate, and -3β-O-sulfamate derivatives with substituents at positions 5 and 6 were synthesized using DHEA as the parent structure and STS inhibitory activity was measured at 3 μM in human Jeg-3 cells. 6β-Chloro-5α-hydroxyandrostane-3β-O-sulfamate (13) was found to be the most active compound with STS inhibition 71%.

목차

서 론(Introduction)

실험 방법(Experimental Methods)

결과 및 고찰(Results and Discussion)

결 론(Conclusion)

키워드

breast cancer steroid sulfatase inhibitor androstane-3β-O-sufonate androstane-3β-O-sulfamate