5707-56-2Relevant articles and documents
Design and synthesis of 3-benzylaminocoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors
Chang, Chiao-Nien,Chen, Mei-Jou,Chiu, Pei-Fang,Hng, Yue,Liang, Pi-Hui,Lin, I-Chun,Lin, Mei-Hsiang,Lin, Tzung-Sheng,Liu, I-Chen,Lu, Yeh-Lin,Tsai, Keng-Chang
, (2020)
Steroid sulfatase (STS) is a sulfatase enzyme that catalyzes the conversion of sulfated steroid precursors to free steroid. The inhibition of STS could abate estrogenic steroids that stimulate the proliferation and development of breast cancer, and therefore STS is a potential target for adjuvant endocrine therapy. In this study, a series of 3-benzylaminocoumarin-7-O-sulfamate derivatives targeting STS were designed and synthesized. Structure-relationship activities (SAR) analysis revealed that attachment of a benzylamino group at the 3-position of coumarin improved inhibitory activity. Compound 3j was found to have the highest inhibition activity against human placenta isolated STS (IC50 0.13 μM) and MCF-7 cell lines (IC50 1.35 μM). Kinetic studies found compound 3j to be an irreversible inhibitor of STS, with KI and kinact value of 86.9 nM and 158.7 min?1, respectively.
Synthetic and crystallographic studies of a new inhibitor series targeting Bacillus anthracis dihydrofolate reductase
Beierlein, Jennifer M.,Frey, Kathleen M.,Bolstad, David B.,Pelphrey, Phillip M.,Joska, Tammy M.,Smith, Adrienne E.,Priestley, Nigel D.,Wright, Dennis L.,Anderson, Amy C.
experimental part, p. 7532 - 7540 (2009/12/07)
Bacillus anthracis, the causative agent of anthrax, poses a significant biodefense danger. Serious limitations in approved therapeutics and the generation of resistance have produced a compelling need for new therapeutic agents against this organism. Baci
Facile synthesis of 5,6-dimethoxy-1-tetralone
Lahiri, Saswata,Ramarao,Rao, B. Venkateswara,Rao, A.V. Rama,Chorghade, Mukund S.
, p. 71 - 72 (2013/09/08)
A facile synthesis of 5,6-dimethoxy-1-tetralone, a key intermediate in the synthesis of an antidepressant compound, ABT-200, was developed from the inexpensive starting material guaiacol.