Application In Synthesis of N-Boc-1,6-DiaminohexaneIn 2020 ,《Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers》 appeared in Journal of Medicinal Chemistry. The author of the article were Cao, Chaoguo; Yang, Jie; Chen, Yong; Zhou, Peiting; Wang, Yingwei; Du, Wu; Zhao, Lifeng; Chen, Yuanwei. The article conveys some information:
The nuclear protein poly(ADP-ribose) polymerase-1 (PARP1) has a well-established role in the signaling and repair of DNA and is a validated therapeutic target for cancers and other human diseases. Here, we have designed, synthesized, and evaluated a series of small-mol. PARP1 degraders based on the proteolysis-targeting chimera (PROTAC) concept. Our efforts have led to the discovery of highly potent PARP1 degraders, as exemplified by compound 18 (SK-575). SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations and induces potent and specific degradation of PARP1 in various human cancer cells even at low picomolar concentrations SK-575 achieves durable tumor growth inhibition in mice when used as a single agent or in combination with cytotoxic agents, such as temozolomide and cisplatin. These data demonstrate that SK-575 is a highly potent and efficacious PARP1 degrader. The experimental process involved the reaction of N-Boc-1,6-Diaminohexane(cas: 51857-17-1Application In Synthesis of N-Boc-1,6-Diaminohexane)
N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is a compound useful in organic synthesis used in the preparation of mixed self-assembled monolayers (SAMs) that resist adsorption of proteins using the reaction of amines with a SAM that presents interchain carboxylic anhydride groupsApplication In Synthesis of N-Boc-1,6-Diaminohexane
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