- A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS
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The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
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Paragraph 000398; 000399
(2021/03/02)
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- A CONJUGATE OF A TUBULYSIN ANALOG WITH BRANCHED LINKERS
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The present invention relates to the conjugation of a tubulysin analog compound to a cell-binding molecule with branched/side-chain linkers for having better delivery of the conjugate compound and targeted treatment of abnormal cells. It also relates to a branched-linkage method of conjugation of a tubulysin analog molecule to a cell-binding ligand, as well as methods of using the conjugate in targeted treatment of cancer, infection and autoimmune disease.
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Page/Page column 12; 185-186
(2019/07/17)
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- Pd(II)-catalyzed C(sp3)-H arylation of amino acid derivatives with click-triazoles as removable directing groups
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By using click-triazoles as conveniently approachable and removable directing groups, the direct palladium-catalyzed C(sp3)-H arylation of amino acid derivatives with various aryl iodides bearing different electronic properties has been achieved. Notably, the desired amino acid molecule can be obtained by the cleavage of the tethered click-triazoles after the catalytic reaction, which aims to provide a practical protocol for the accessibility of both natural and synthetic amino acids.
- Zhang, Guofu,Xie, Xiaoqiang,Zhu, Jianfei,Li, Shasha,Ding, Chengrong,Ding, Ping
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supporting information
p. 5444 - 5449
(2015/05/20)
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- Developing new chemical tools for DNA methyltransferase 1 (DNMT 1): A small-molecule activity-based probe and novel tetrazole-containing inhibitors
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DNA methylation is an important epigenetic modification catalyzed by DNA methyltransferases (DNMTs). Abnormal expression of endogenous DNMTs in human causes alterations in the genome methylation patterns which subsequently lead to the development of cance
- Zhu, Biwei,Ge, Jingyan,Yao, Shao Q.
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p. 2917 - 2927
(2015/03/30)
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- Ligand and metal complex having the same
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A ligand and a metal complex having the ligand are provided. The ligand and a paramagnetic metal ion form a metal complex with high stability, high relaxivity and high biocompatibility. The metal complex of the present invention is applicable to the prepa
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Page/Page column 18
(2015/03/03)
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- Design and synthesis of calcium responsive magnetic resonance imaging agent: Its relaxation and luminescence studies
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Calcium concentration modulation both inside and outside cell is of considerable interest for nervous system function in normal and pathological conditions. MRI has potential for very high spatial resolution at molecular/cellular level. Design, synthesis and evaluation of Gd-DO3A-AME-NPHE, a calcium responsive MRI contrast agent is presented. The probe is comprised of a Gd3+-DO3A core coupled to iminoacetate coordinating groups for calcium induced relaxivity switching. In the absence of Ca2+ ions, inner sphere water binding to the Gd-DO3A-AME-NPHE is restricted with longitudinal relaxivity, r1 = 4.37 mM-1 s-1 at 4.7 T. However, addition of Ca2+ triggers a marked enhancement in r1 = 6.99 mM-1 s-1 at 4.7 T (60% increase). The construct is highly selective for Ca2+ over competitive metal ions at extracellular concentration. The r1 is modulated by changes in the hydration number (0.2 to 1.05), which was confirmed by luminescence emission lifetimes of the analogous Eu3+ complex. T1 phantom images establish the capability of complex of visualizing changes in [Ca2+] by MRI.
- Tanwar, Jyoti,Datta, Anupama,Chauhan, Kanchan,Kumaran, S. Senthil,Tiwari, Anjani K.,Kadiyala, K. Ganesh,Pal, Sunil,Thirumal,Mishra, Anil K.
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p. 225 - 232
(2014/06/24)
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- PHENYLALANINE DIPEPTIDE DERIVATIVES, COMPOSITIONS AND USE THEREOF
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Disclosed are a compound of formula I, stereoisomers, pharmaceutically acceptable salts or hydrates thereof, a pharmaceutical composition comprising the smae, a process for preparing the same and use thereof. The compound may also be used to prepare a medicament to treat viral infections, especially to prepare a medicament to treat hepatitis B virus and human immunodeficiency virus with little toxic side effects.
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Page/Page column 12-13
(2009/10/06)
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- Small molecule macroarray construction via Ugi four-component reactions
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(Chemical Equation Presented) We report the construction of small molecule macroarrays via Ugi four-component reactions on planar cellulose supports. Array synthesis was enabled by the development of a high efficiency photocleavable linker system and the
- Lin, Qi,O'Neill, Jennifer C.,Blackwell, Helen E.
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p. 4455 - 4458
(2007/10/03)
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- Synthesis of novel bifunctional Schiff-base ligands derived from condensation of 1-(p-nitrobenzyl)ethylenediamine and 2-(p-nitrobenzyl)-3-monooxo-1,4,7-triazaheptane with salicylaldehyde
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Two potentially tetradentate (N2O2) and pentadentate (N3O3) bifunctional Schiff-base ligands, N,N′-bis(2-hydroxybenzyl)-1-(p-aminobenzyl)ethylenediamine (7) and N,N′-bis(2-hydroxybenzyl)-2-(p-aminobenzyl)-3-monooxo-1,4,7- triazaheptane (5′) have been prepared and characterized by various spectroscopic methods (IR, FAB-MS, NMR). They are derived from the condensation reactions of the C-functionalized diamines 1-(p-nitrobenzyl)ethylenediamine and 2-(p-nitrobenzyl)-3-monooxo-1,4,7-triazaheptane with 2.1 equiv. of salicylaldehyde. The first complexation trials with 99mTc are reported.
- Mishra, Anil Kumar,Panwar, Puja,Chopra, Madhu,Sharma, Rakesh Kumar,Chatal, Jean-Francois
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p. 1054 - 1058
(2007/10/03)
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- Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists.
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A structure-based focused library approach was employed in an effort to identify more lipophilic replacements for the N-benzylpyroglutamyl group of the VCAM/VLA-4 antagonist 2. This effort led to the discovery of two new classes of potent antagonists char
- Chen,Trilles, Richard,Miklowski, Dorota,Huang, Tai-Nan,Fry, David,Campbell, Robert,Rowan, Karen,Schwinge, Virginia,Tilley, Jefferson W
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p. 1679 - 1682
(2007/10/03)
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