Targeting the Hsp90 C-terminal domain by the chemically accessible dihydropyrimidinone scaffold.
نویسندگان
چکیده
Hsp90 C-terminal ligands are potential new anti-cancer drugs alternative to the more studied N-terminal inhibitors. Here we report the identification of a new dihydropyrimidinone binding the C-terminus, which is not structurally related to other well-known natural and nature-inspired inhibitors of this second druggable Hsp90 site.
منابع مشابه
Identification of the key structural elements of a dihydropyrimidinone core driving toward more potent Hsp90 C-terminal inhibitors.
Hsp90 C-terminal modulation represents an attractive strategy for the development of potent and safer antitumor compounds. Continuing our investigation on DHPM type inhibitors here we report a new set of potent C-terminal ligands which allowed us to identify the key structural features crucial for the biological activity.
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ورودعنوان ژورنال:
- Chemical communications
دوره 51 18 شماره
صفحات -
تاریخ انتشار 2015