The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 2,6-Dichloropurine( cas:5451-40-1 ) is researched.Safety of 2,6-Dichloropurine.Bhattarai, Sanjay; Pippel, Jan; Meyer, Anne; Freundlieb, Marianne; Schmies, Constanze; Abdelrahman, Aliaa; Fiene, Amelie; Lee, Sang-Yong; Zimmermann, Herbert; El-Tayeb, Ali; Yegutkin, Gennady G.; Straeter, Norbert; Mueller, Christa E. published the article 《X-Ray Co-Crystal Structure Guides the Way to Subnanomolar Competitive Ecto-5-Nucleotidase (CD73) Inhibitors for Cancer Immunotherapy》 about this compound( cas:5451-40-1 ) in Advanced Therapeutics (Weinheim, Germany). Keywords: mammary gland neoplasm CD73 cancer immunotherapy. Let’s learn more about this compound (cas:5451-40-1).
Ecto-5-nucleotidase (CD73, EC 3.1.3.5) catalyzes the extracellular hydrolysis of AMP yielding adenosine, which induces immunosuppression, angiogenesis, metastasis, and proliferation of cancer cells. CD73 inhibition is therefore proposed as a novel strategy for cancer (immuno)therapy, and CD73 antibodies are currently undergoing clin. trials. Despite considerable efforts, the development of small mol. CD73 inhibitors has met with limited success. To develop a suitable drug candidate, a high resolution (2.05 Å) co-crystal structure of the CD73 inhibitor PSB-12379, a nucleotide analog, in complex with human CD73 is determined This allows the rational design and development of a novel inhibitor (PSB-12489) with subnanomolar inhibitory potency toward human and rat CD73, high selectivity, as well as high metabolic stability. A co-crystal structure of PSB-12489 with CD73 (1.85 Å) reveals the interactions responsible for increased potency. PSB-12489 is the most potent CD73 inhibitor to date representing a powerful tool compound and novel lead structure.
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Reference:
Oxazolidine – Wikipedia,
Oxazolidine | C3H7NO – PubChem