1122-12-9Relevant academic research and scientific papers
Highly homogeneous antibody modification through optimisation of the synthesis and conjugation of functionalised dibromopyridazinediones
Bahou, Calise,Richards, Daniel A.,Maruani, Antoine,Love, Elizabeth A.,Javaid, Faiza,Caddick, Stephen,Baker, James R.,Chudasama, Vijay
, p. 1359 - 1366 (2018)
Due to their exquisite cysteine-selectivity, excellent stability, and ability to functionally rebridge disulfide bonds, dibromopyridazinediones are emerging as an exciting new class of bioconjugation reagents, particularly in the field of antibody conjugation. Despite this, relatively little work has been performed on the optimisation of their synthesis and subsequent reaction with immunoglobulins. Herein we present a novel synthetic route towards functionalised dibromopyridazinediones, proceeding via an isolatable dibromopyridazinedione-NHS ester. Reaction of this activated intermediate with a variety of amines produces functional dibromopyridazinediones in good to excellent yields. The disulfide rebridging capacity of these reagents was optimised on the clinically relevant IgG1 trastuzumab, resulting in a general method which allows for the generation of site-selectively modified native trastuzumab with over 90% homogeneity (no disulfide scrambling) without the need for protein engineering or enzymatic conjugation.
Towards the cis-bromination of double bonds
Carman,Derbyshire,Hansford,Kadirvelraj,Robinson
, p. 117 - 126 (2001)
The bromination of olefins yielding a trans-1,2-dibromo-product was studied. Reagents were proposed to brominate the double bonds of cis-olefins mildly and stereospecifically. Reagents delivering two bromine atoms to the same side of olefins through a cyclic six-membered transition state were studied.
Co-sensitization of N719 with polyphenylenes from the Bergman cyclization of maleimide-based enediynes for dye-sensitized solar cells
Dong, Luhua,Zheng, Zhiwei,Wang, Youfu,Li, Xing,Hua, Jianli,Hu, Aiguo
, p. 11607 - 11614 (2015)
The co-sensitization of N719 with conjugated polyphenylenes for dye-sensitized solar cells (DSSCs) was demonstrated. The conjugated polyphenylenes (6-BC and 7-BC), which contain two triphenylamine (TPA) groups as electron donors and carboxylic acids as ad
PHOTOCHEMICAL TRANSFORMATION OF TETRABROMOFURAN BY OXYGEN INTO 2,3,4,4-TETRABROMOBUT-2-EN-4-OLIDE IN THE SOLID STATE
Shoppee, Charles W.
, p. 45 - 52 (1985)
The solid-state photo-oxidation (1) -> (2) recorded by Torrey in 1897 has been verified and structure (2) confirmed; a possible mechanism for the transformation involving free radicals is suggested.In contrast, the bromination (5) -> (2) reported by Hill and Cornelison in 1894 could not be repeated despite many attempts.An ionic mechanism for the preparation (4) -> (6) is proposed; the semi-aldehyde (6) in solution exists solely in the lactol form (7).
Targeting the DIO3 enzyme using first-in-class inhibitors effectively suppresses tumor growth: a new paradigm in ovarian cancer treatment
Alfandari, Adi,Ashur-Fabian, Osnat,Ellis, Martin,Finkelshtein, Yael,Katzav, Aviva,Kidron, Debora,Lerer, Bernard,Lifschytz, Tzuri,Mondal, Santanu,Moskovich, Dotan,Mugesh, Govindasamy,Rosemarin, Amit,Ungati, Harinarayana,Weisz, Avivit
, p. 6248 - 6257 (2021/09/28)
The enzyme iodothyronine deiodinase type 3 (DIO3) contributes to cancer proliferation by inactivating the tumor-suppressive actions of thyroid hormone (T3). We recently established DIO3 involvement in the progression of high-grade serous ovarian cancer (H
PIM KINASE INHIBITOR COMPOSITIONS AND USES THEREOF
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Paragraph 0226, (2020/11/12)
This disclosure relates to compounds and compositions useful as inhibitors of PIM kinases. Also provided are methods of synthesis and methods of use of PIM inhibitors in treating individuals suffering from cancerous malignancies.
Reversible covalent linkage of functional molecules
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Page/Page column 62, (2016/04/26)
The present invention relates to the use of a compound containing a moiety of formula (I) as a reagent for linking a compound of formula R1—H which comprises a first functional moiety of formula F1 to a second functional moiety of fo
Maleimide-based acyclic enediyne for efficient DNA-cleavage and tumor cell suppression
Song, Depeng,Sun, Shiyuan,Tian, Yu,Huang, Shuai,Ding, Yun,Yuan, Yuan,Hu, Aiguo
supporting information, p. 3195 - 3200 (2015/04/27)
A pH-sensitive acyclic enediyne (1) was synthesized for efficient DNA-cleavage and tumor cell suppression. Unlike other acyclic enediynes, this novel enediyne transforms into a highly reactive enediyne (2) in an acidic environment only, which undergoes Be
TYPE III DEIODINASE INHIBITORS AND USES THEREOF
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Page/Page column 32; 33, (2015/11/10)
The present invention relates to compounds that inhibit the activity of Type III deiodinase (DIO3). The present invention further relates to methods for treating or preventing depression, depression associated with other psychiatric or general medical dis
A dithienylethene-based rewritable hydrogelator
Van Herpt, Jochem T.,Stuart, Marc C. A.,Browne, Wesley R.,Feringa, Ben L.
supporting information, p. 3077 - 3083 (2014/03/21)
Dithienylethene photochromic switching units have been incorporated into a hydrogelating system based on a tripeptide motif. The resulting hybrid system provided both a photochromic response and the ability to gelate water under acidic and neutral conditi
