4614-56-6Relevant academic research and scientific papers
ANTI-MSR1 ANTIBODIES AND METHODS OF USE THEREOF
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Paragraph 0486, (2019/11/28)
Provided herein are antibodies and antigen-binding fragments that bind MSR1 and methods of use thereof. According to certain embodiments, the antibodies bind human MSR1 with high affinity. In certain embodiments, the antibodies bind MSR1 without blocking, or blocking less than 90%, of modified LDL binding to MSR1. In some embodiments, the antibodies bind cell surface expressed-MSR1 and are internalized. The antibodies of the invention may be fully human antibodies. The invention includes anti-MSR1 antibodies, or antigen-binding fragments thereof, conjugated to drugs or therapeutic compounds.
Late-stage C-H amination of abietane diterpenoids
Lapuh, María Ivana,Dana, Alejandro,Di Chenna, Pablo H.,Darses, Benjamin,Durán, Fernando J.,Dauban, Philippe
supporting information, p. 4736 - 4746 (2019/05/24)
This study aims at highlighting the synthetic versatility of the rhodium-catalyzed C-H amination reactions using iodine(iii) oxidants for the late-stage functionalization of natural products. Inter-and intramolecular nitrene insertions have been performed from various abietane diterpenoids, leading to the amination of the C-3, C-6, C-7, C-11 and C-15 positions. Ca. 20 aminated compounds have been isolated with yields of up to 86% and high levels of regio-, chemo-and stereoselectivities.
BIS-OCTAHYDROPHENANTHRENE CARBOXAMIDES AND PROTEIN CONJUGATES THEREOF
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Paragraph 0609, (2018/12/04)
Provided herein are compounds, compositions and methods for the treatment of diseases and disorders associated with the liver X receptor, including bis-octahydrophenanthrene carboxamides and protein (e.g., antibody) drug conjugates thereof.
CYCLODEXTRIN PROTEIN DRUG CONJUGATES
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Paragraph 0568; 0569, (2018/12/04)
Provided herein are compounds, compositions, conjugates and methods for the treatment of diseases, and/or conditions such as, but not limited to, proliferative diseases. In certain embodiments, compounds, compositions, and conjugates are provided, which include cyclodextrin-based linker-payloads and protein conjugates thereof, and/or in combination with other agents. By administering these compounds, compositions, and conjugates as described herein to specific target cells, side-effects due to non-specific binding phenomena, for example, to non-target cells are reduced.
Phenolic diterpenoid derivatives as anti-influenza a virus agents
Dang, Zhao,Jung, Katherine,Zhu, Lei,Xie, Hua,Lee, Kuo-Hsiung,Chen, Chin-Ho,Huang, Li
, p. 355 - 358 (2015/03/30)
A series of diterpenoid derivatives based on podocarpic acid were synthesized and evaluated as anti-influenza A virus agents. Several of the novel podocarpic acid derivatives exhibited nanomolar activities against an H1N1 influenza A virus (A/Puerto Rico/8/34) that was resistant to two anti-influenza drugs, oseltamivir and amantadine. This class of compounds inhibits the influenza virus by targeting the viral hemagglutinin-mediated membrane fusion. These results indicated that podocarpic acid derivatives may serve as potential drug candidates to fight drug-resistant influenza A virus infections.
Copper(I)-catalyzed cycloaddition of methyl O-propargylpodocarpate and azides at room temperature
Nguyen, Dao M.,Miles, D. Howard
experimental part, p. 1759 - 1771 (2011/06/24)
Copper iodide was employed as an efficient catalyst for the synthesis of 1,2,3-triazole derivatives of podocarpic acid at room temperature through "click" chemistry cycloaddition reactions of methyl O-propargylpodocarpate and propargyl O-propargylpodocarpate with azides.
Design, synthesis, and characterization of BK channel openers based on oximation of abietane diterpene derivatives
Cui, Yong-Mei,Yasutomi, Eriko,Otani, Yuko,Ido, Katsutoshi,Yoshinaga, Takashi,Sawada, Kohei,Ohwada, Tomohiko
experimental part, p. 8642 - 8659 (2011/02/25)
Oxime ether derivatives at the benzylic position of unsubstituted, dichloro, trichloro, and monobromo derivatives of the aromatic C-ring of dehydroabietic acid and podocarpic acid were synthesized and evaluated as BK channel openers in an assay system of CHO-K1 cells expressing hBKα channels. Detailed SAR analysis showed that the oximation was particularly effective in the cases of dehydroabietic acid derivatives, and some of these oxime derivatives showed more potent BK channel activities than the standard compound, NS1619. The present studies provide a new structural basis for development of efficient BK channel openers.
Design, synthesis and characterization of podocarpate derivatives as openers of BK channels
Cui, Yong-Mei,Yasutomi, Eriko,Otani, Yuko,Yoshinaga, Takashi,Ido, Katsutoshi,Sawada, Kohei,Ohwada, Tomohiko
scheme or table, p. 5197 - 5200 (2009/05/07)
We found that the podocarpic acid structure provides a new scaffold for chemical modulators of large-conductance calcium-activated K+ channels (BK channels). Structure-activity analysis indicates the importance of both the arrangement (i.e., location and orientation) of the carboxylic acid functionality of ring A and the hydrophobic region of ring C for expression of BK channel-opening activity.
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters
Singh, Sheo B.,Ondeyka, John G.,Liu, Weiguo,Chen, Steve,Chen, Tom S.,Li, Xiaohua,Bouffard, Aileen,Dropinski, James,Jones, A. Brian,McCormick, Sherrie,Hayes, Nancy,Wang, Jianhua,Sharma, Neelam,MacNaul, Karen,Hernandez, Melba,Chao, Yu-Sheng,Baffic, Joanne,Lam, My-Hanh,Burton, Charlotte,Sparrow, Carl P.,Menke, John G.
, p. 2824 - 2828 (2007/10/03)
Liver X receptors are nuclear receptors that regulate metabolism of cholesterol. They are activated by oxysterols resulting in increased transcription of the ABCA1 gene, promoting cholesterol efflux and HDL formation. We have identified podocarpic acid an
Design, synthesis, and structure-activity relationship of podocarpic acid amides as liver X receptor agonists for potential treatment of atherosclerosis
Liu, Weiguo,Chen, Steve,Dropinski, James,Colwell, Lawrence,Robins, Michael,Szymonifka, Michael,Hayes, Nancy,Sharma, Neelam,MacNaul, Karen,Hernandez, Melba,Burton, Charlotte,Sparrow, Carl P.,Menke, John G.,Singh, Sheo B.
, p. 4574 - 4578 (2007/10/03)
A series of podocarpic acid amides were identified as potent agonists for Liver X receptor α and β subtypes, which are members of a nuclear hormone receptor superfamily that are involved in the regulation of a variety of metabolic pathways including chole
