- Protective effects of 10,11-dihydro-5H-dibenzo[b,f]azepine hydroxamates on vascular cognitive impairment
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A series of 10,11-dihydro-5H-dibenzo [b,f]azepine hydroxamates (4–15) were synthesized, behaving as histone deacetylase inhibitors, and examined for their influence on vascular cognitive impairment (VCI), which correlated with dementia. The results reveal
- Kaur, Navdeep,Fang, Yao-Ching,Lee, Hsueh-Yun,Singh, Arshdeep,Nepali, Kunal,Lin, Mei-Hsiang,Yeh, Teng-Kuang,Lai, Mei-Jung,Chan, Lung,Tu, Yong-Kwang,Banerjee, Suddhasatwa,Hu, Chaur-Jong,Liou, Jing-Ping
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- TRICYCLIC MODULATORS OF PP2A
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Chemical modulators of PP2A, comprising tricyclic sulfonimidamides are disclosed. The compounds are useful in preventing or treating cancer, diabetes, autoimmune disease, solid organ transplant rejection, graft vs host disease, chronic obstructive pulmonary disease (COPD), non-alcoholic fatty liver disease, abdominal aortic aneurysm, chronic liver disease, heart failure, neurodegenerative disease and cardiac hypertrophy. The compounds are of formula (I)
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Page/Page column 174-175
(2021/09/04)
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- HECT E3 LIGASE INHIBITORS AND USES THEREOF
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The present invention relates to tricyclic derivatives of formula (I), which are useful as inhibitors of HECT-domain-containing E3 ligases, in particular NEDD4. The present invention also refers to pharmaceutical compositions comprising compounds of formu
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Page/Page column 49
(2020/12/29)
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- Reengineered tricyclic anti-cancer agents
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The phenothiazine and dibenzazepine tricyclics are potent neurotropic drugs with a documented but underutilized anti-cancer side effect. Reengineering these agents (TFP, CPZ, CIP) by replacing the basic amine with a neutral polar functional group (e.g., RTC-1, RTC-2) abrogated their CNS effects as demonstrated by in vitro pharmacological assays and in vivo behavioral models. Further optimization generated several phenothiazines and dibenzazepines with improved anti-cancer potency, exemplified by RTC-5. This new lead demonstrated efficacy against a xenograft model of an EGFR driven cancer without the neurotropic effects exhibited by the parent molecules. Its effects were attributed to concomitant negative regulation of PI3K-AKT and RAS-ERK signaling.
- Kastrinsky, David B.,Sangodkar, Jaya,Zaware, Nilesh,Izadmehr, Sudeh,Dhawan, Neil S.,Narla, Goutham,Ohlmeyer, Michael
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supporting information
p. 6528 - 6534
(2015/10/05)
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