1122-12-9Relevant articles and documents
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.
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).
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.
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