5707-56-2Relevant academic research and scientific papers
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.
Crossing the Boundaries between Marine and Muguet: Discovery of Unusual Lily-of-the-Valley Odorants Devoid of Aldehyde Functions
Jordi, Samuel,Kraft, Philip
, (2018/06/04)
Since 6-isopropyl- (11) and 6-isobutyl-2H-benzo[b][1,4]dioxepin-3(4H)-one (12) instead of the expected marine odor had been reported to possess lily-of-the-valley notes, albeit weaker than benchmark odorants, the influence of a cyclopropyl ring instead of
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
Serotonin reuptake inhibitor
-
, (2008/06/13)
A serotonin reuptake inhibitor containing a cyclic amine represented by the following formula, a prodrug thereof, or a pharmaceutically acceptable salt of said cyclic amine or prodrug as an active ingredient: wherein R0 is a hydrogen atom, a halogen atom, an alkyl group, a substituted alkyl group, a hydroxyl group, an alkoxy group or the like, R3 is a hydrogen atom or the like, Y is an alkylene group or the like, Z is a hydrogen atom, a cycloalkyl group, an aryl group or the like, n is 1, 2 or 3, and m is 2, 3, 4, 5 or 6.
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.
Synthesis and in vitro antibacterial activities of novel conformationally restricted hygromycin A analogues
Cooper, Christopher B.,Blair, Kyle T.,Jones, Christopher S.,Minich, Martha L.
, p. 1747 - 1752 (2007/10/03)
The preparation of semisynthetic conformationally restricted hygromycin A analogues are described. Antibacterial results from these compounds suggest active conformations for this class of agents.
Total synthesis of the β-adrenergic receptor antagonist, the tetrahydroisoquinoline MY336-a and its epimer
Kaufman, Teodoro S.
, p. 2497 - 2505 (2007/10/03)
The first total synthesis of the novel β-adrenergic receptor antagonist MY336-a 1 and its epimer 2 has been achieved from 2,3-dimethoxytoluene, by Jackson cyclisation of N-benzyl-N-tosylamido acetals, Lewis acid-mediated addition of silicon-based nucleoph
Studies on the Natural β-Adrenergic Receptor Antagonist MY336-a: Synthesis of a 3-Dehydroxymethyl Analogue
Kaufman, Teodoro S.
, p. 403 - 404 (2007/10/02)
The preparation of a polysubstituted tetrahydroisoquinoline, which lacks only the 3-CH2OH group of MY336-a, is described.
