- MCL1 INHIBITORS AND USES THEREOF
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The present disclosure provides compounds, such as compounds of Formula I, and compositions that are MCL1 inhibitors.
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- ANDROGEN RECEPTOR MODULATORS AND METHODS FOR THEIR USE
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The present invention relates to compounds of formula (I)-(VI) and/or (A)-(H-I), or any subgenera thereof, or a pharmaceutically acceptable salt, tautomer or stereoisomer. The compounds of the present disclosure are useful in modulating androgen receptor activity and for treating cancer including prostate cancer.
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Paragraph 1074; 1075
(2020/05/06)
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- Design, synthesis, and structure-activity-relationship of a novel series of CXCR4 antagonists
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The important roles of the CXCL12/CXCR4 axis in numerous pathogenic pathways involving HIV infection and cancer metastasis make the CXCR4 receptor an attractive target for the development of therapeutic agents. Through scaffold hybridization of a few known CXCR4 antagonists, a series of novel aminopyrimidine derivatives was developed. Compound 3 from this new scaffold demonstrates excellent binding affinity with CXCR4 receptor (IC50 = 54 nM) and inhibits CXCL12 induced cytosolic calcium increase (IC50 = 2.3 nM). Furthermore, compound 3 possesses good physicochemical properties (MW 353, clogP 2.0, PSA 48, pKa 6.7) and exhibits minimal hERG and CYP isozyme (e.g. 3A4, 2D6) inhibition. Collectively, these results strongly support further optimization of this novel scaffold to develop better CXCR4 antagonists.
- Li, Zhanhui,Wang, Yujie,Fu, Chunyan,Wang, Xu,Wang, Jun Jun,Zhang, Yi,Zhou, Dongping,Zhao, Yuan,Luo, Lusong,Ma, Haikuo,Lu, Wenfeng,Zheng, Jiyue,Zhang, Xiaohu
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- Enantioselective α-benzylation of aldehydes via photoredox organocatalysis
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The first enantioselective aldehyde α-benzylation using electron-deficient aryl and heteroaryl substrates has been accomplished. The productive merger of a chiral imidazolidinone organocatalyst and a commercially available iridium photoredox catalyst in the presence of household fluorescent light directly affords the desired homobenzylic stereogenicity in good to excellent yield and enantioselectivity. The utility of this methodology has been demonstrated via rapid access to an enantioenriched drug target for angiogenesis suppression.
- Shih, Hui-Wen,Vander Wal, Mark N.,Grange, Rebecca L.,MacMillan, David W. C.
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supporting information; experimental part
p. 13600 - 13603
(2010/11/18)
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