183896-00-6Relevant articles and documents
Changshanone derivatives and their pharmaceutical compositions and uses
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, (2022/01/12)
The present application relates to a changshanone derivative and a pharmaceutical composition and use thereof, the changshanone derivative is shown in formula I, wherein m is 1 to 4, n is 1 to 10, A is H or a detection marker, such as a biotin marker. The present application further relates to a pharmaceutical composition comprising a derivative of changshanone of formula I and its application in the treatment of cancer. Equation I.
From Inhibition to Degradation: Targeting the Antiapoptotic Protein Myeloid Cell Leukemia 1 (MCL1)
Papatzimas, James W.,Gorobets, Evgueni,Maity, Ranjan,Muniyat, Mir Ishruna,Maccallum, Justin L.,Neri, Paola,Bahlis, Nizar J.,Derksen, Darren J.
, p. 5522 - 5540 (2019/06/17)
Protein-protein interactions (PPIs) have emerged as significant targets for therapeutic development, owing to their critical nature in diverse biological processes. An ideal PPI-based target is the protein myeloid cell leukemia 1 (MCL1), a critical prosurvival factor in cancers such as multiple myeloma where MCL1 levels directly correlate to disease progression. Current strategies for halting the antiapoptotic properties of MCL1 revolve around inhibiting its sequestration of proapoptotic factors. Existing inhibitors disrupt endogenous regulatory proteins; however, this strategy actually leads to an increase of MCL1 protein levels. Here, we show the development of hetero-bifunctional small molecules capable of selectively targeting MCL1 using a proteolysis targeting chimera (PROTAC) methodology leading to successful degradation. We have confirmed the involvement of the E3 ligase CUL4A-DDB1 cereblon ubiquitination pathway, making these PROTACs a first step toward a new class of antiapoptotic B-cell lymphoma 2 family protein degraders.
POLYCYCLIC EPOXIDES AND COMPOSITIONS THEREOF WITH ANTI-CANCER ACTIVITIES
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, (2016/12/01)
The present technology provides polycyclic epoxides of Formula I, compositions comprising such expoxides and methods of using such epoxides. In particular, these compounds are useful for inhibiting cancer cell proliferation and tumor angiogenesis or treating ovarian, breast, prostate, liver, pancreatic, and colon cancers, as well as leukemia.