Hng, Yue published the artcileDesign and synthesis of 3-benzylaminocoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors, Safety of 2,3-Dimethoxybenzaldehyde, the main research area is benzylaminocoumarin sulfamate synthesis anticancer SAR steroid sulfatase breast cancer; Breast cancer; Coumarin; Hormone dependent cancer; Irreversible inhibitors; Steroid sulfatase; Sulfamate.
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–activity relationship (SAR) anal. 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, resp.
Bioorganic Chemistry published new progress about Antitumor agents. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Safety of 2,3-Dimethoxybenzaldehyde.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem