- Organopalladium Approaches to Prostaglandines. 3. Synthesis of Bicyclic and Tricyclic 7-Oxaprostaglandin Endoperoxide Analogues via Oxypalladation of Norbornadiene
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Oxypalladation of norbornadiene provides an organopalladium intermediate 12 readily carbonylated and subsequently elaborated into the first bicyclic and tricyclic 7-oxaprostaglandin endoperoxide analogues 18 and 24 in 22percent and 24percent overall yields, respectively.
- Larock, Richard C.,Leach, Douglas R.
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- PROTEIN-MACROMOLECULE CONJUGATES AND METHODS OF USE THEREOF
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The present disclosure provides protein-macromolecule conjugates, releasable linkers, and macromolecules, as defined herein. The disclosed conjugates provide unique properties that are based at least upon the properties of linker and number of linker-Macromolecule moieties. Also provided herein are a method of synthesis and use of conjugates in treating diseases and disorders.
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Paragraph 0514; 0515-0516
(2021/04/10)
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- Hapten design and monoclonal antibody to fluoroacetamide, a small and highly toxic chemical
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Fluoroacetamide (FAM) is a small (77 Da) and highly toxic chemical, formerly used as a rodenticide and potentially as a poison by terrorists. Poisoning with FAM has occurred in humans, but few reliably rapid detection methods and antidotes have been reported. Therefore, producing a specific antibody to FAM is not only critical for the development of a fast diagnostic but also a potential treatment. However, achieving this goal is a great challenge, mainly due to the very low molecular weight of FAM. Here, we design two groups of FAM haptens for the first time, maximally exposing the fluorine or amino groups, with the aid of linear aliphatic or phenyl-contained spacer arms. Interestingly, whereas the hapten with fluorine at the far end of the hapten did not induce an antibody response to FAM, the hapten with an amino group at the far end and phenyl-contained spacer arm triggered a significantly specific antibody response. Finally, a monoclonal antibody (mAb) named 5D11 was successfully obtained with an IC50 value of 97 μg mL?1 and negligible cross-reactivities to the other nine functional and structural analogs.
- Yang, Ling,Zhang, Xiya,Shen, Dongshuai,Yu, Xuezhi,Li, Yuan,Wen, Kai,Shen, Jianzhong,Wang, Zhanhui
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- BIOLOGICALLY ACTIVE MOLECULE CONJUGATES, REAGENTS AND METHODS OF MANUFACTURE, AND THERAPEUTIC USES
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The present disclosure relates to conjugates comprising biologically active molecules linked to a multimeric antigen-binding compound or a multimeric immunoglobulin via a linker. The disclosure further provides reagents and methods of manufacturing the conjugates and the linkers. The disclosure also provides compositions comprising the conjugates, methods of modifying abnormal cell growth and methods of treatment using the conjugates or the compositions.
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Paragraph 00244
(2015/12/30)
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- Water solubility, antioxidant activity and cytochrome C binding of four families of exohedral adducts of C60 and C70
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Over the past decade, surface-modified, water soluble fullerenes have been shown by many different investigators to exhibit strong antioxidant activity against reactive oxygen species (ROS) in vitro and to protect cells and tissues from oxidative injury a
- Witte, Patrick,Beuerle, Florian,Hartnagel, Uwe,Lebovitz, Russell,Savouchkina, Anastasia,Sali, Sevda,Guldi, Dirk,Chronakis, Nikos,Hirsch, Andreas
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p. 3599 - 3613
(2008/10/09)
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- Efficient chemoselective deprotection of silyl ethers using catalytic 1-chloroethyl chloroformate in methanol
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Fast and chemoselective desilylation of silyl-protected alcohols was achieved using a catalytic amount of 1-chloroethyl chloroformate in methanol. With a minimal amount of 1-chloroethyl chloroformate as the source for anhydrous HCl, extremely efficient cleavage of silyl ethers of primary and secondary alcohols was accomplished, and chemoselective deprotection of one silyl ether in the presence of another silyl or other acid-labile group was possible through controlling the amount of the chloroformate and reaction time.
- Yeom, Chang-Eun,Kim, Young Jong,Lee, So Young,Shin, Yong Je,Kim, B. Moon
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p. 12227 - 12237
(2007/10/03)
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- Cyclic five-membered phosphinate esters as transition state analogues for obtaining phosphohydrolase antibodies
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Two novel cyclic five-membered phosphinate esters (6 and 7) were synthesized and used as transition state analogues (TSAs) for raising phosphohydrolase antibodies. The key step in the syntheses was a McCormack reaction between (2-chloroethyl)dichlorophosphite and 1,4-diphenyl-1,3-butadiene to form isomeric cyclic phosphinyl chlorides which upon further elaboration yielded the TSAs. X-ray crystal structures of two cyclic phosphinate TSA precursors (14a and 14b) show highly compressed CPC bond angles of 94°-97° indicating that the CPC bond angles in 6 and 7 are significantly distorted towards the ideal trigonal bipyramidal equatorial-apical transition state angle of 90° formed during phosphate ester hydrolysis. Antibodies were raised to 6 and 7 using standard hybridoma technology. One antibody. Jel 541, an IgM class antibody, was obtained that was capable of catalyzing the hydrolysis of phosphonate substrate 9 and, to a much lesser extent, phosphate substrate 8. This antibody bound TSA 6 approximately 100 times more tightly than TSA 7 as determined by solid phase radio immune assays. The activity of the antibody-catalyzed reaction was completely inhibited by the presence of TSA 6. Although the relative instability and poor solubility of Jel 541 made it impossible to perform a detailed kinetic analysis of the antibody-catalyzed reactions, these results demonstrate that phospholydrolase antibodies can indeed be obtained using cyclic five membered phosphinates as haptens.
- Hum, Gabriel,Wooler, Krista,Lee, Jeremy,Taylor, Scott D.
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p. 642 - 655
(2007/10/03)
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- Compositions and methods for enhanced drug delivery
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The present invention relates to methods of delivering pharmaceutical agents across membranes, including the skin layer or mucosal membranes of a patient. A pharmaceutical agent is covalently bonded to a chemical modifier, via a physiologically cleavable bond, such that the membrane transport and delivery of the agent is enhanced.
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- Synthesis of Two Novel Phosphorylcholine Esters for Probes in Immunological Studies
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For use in immunological studies on phosphorylcholine (PC)-binding immunoglobulins, two PC esters were synthesized.Ester 5, obtained in 65percent overall yield, contained a covalently bound mercury atom at a specific site as required in an X-ray diffracti
- Spande, Thomas F.
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p. 3081 - 3084
(2007/10/02)
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