89288-22-2Relevant articles and documents
Synthesis of Water-Soluble Chiral DOTA Lanthanide Complexes with Predominantly Twisted Square Antiprism Isomers and Circularly Polarized Luminescence
Dai, Lixiong,Zhang, Junhui,Chen, Yuqing,Mackenzie, Lewis E.,Pal, Robert,Law, Ga-Lai
supporting information, p. 12506 - 12510 (2019/10/02)
One-step cyclization of a tetraazamacrocycle 5 with 70% yield in a 25-g scale was performed. Its chiral DOTA derivatives, L4, has ?93% of TSAP coordination isomer in its Eu(III) and Yb(III) complexes in aqueous solution. [GdL4]5- exhibits a high relaxivity, making it a promising and efficient MRI contrast agent. High luminescence dissymmetry factor (glum) values of 0.285 (ΔJ = 1) for [TbL3]- and 0.241 (ΔJ = 1) for [TbL4]5- in buffer solutions were recorded.
CHIRAL CYCLEN COMPOUNDS AND THEIR USES
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Paragraph 0089; 0184, (2018/04/13)
The present invention relates to the preparation of a series of chiral DOTA, D03A, D02A, DO1A, cyclen and their metal complexes, which display properties superior to those of previous DOTA- based compounds, and hence are potentially valuable as a platform for diagnostic applications. The chiral DOTAs reveal a high abundance of twisted square antiprism (TSA) geometry favoring them to be used as potential MRI contrast agents, whereas their rapid labelling properties at mild conditions make them excellent candidates for use as radiometal chelators.
ANTIBODY DRUG CONJUGATES
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, (2017/01/02)
This application discloses anti-P-cadherin antibodies, antigen binding fragments thereof, and antibody drug conjugates of said antibodies or antigen binding fragments, particularly antibody drug conjugates comprising anti-P-cadherin antibodies conjugated to auristatin analogs. The invention also relates to methods of treating cancer using the antibody drug conjugates. Also disclosed herein are methods of making the antibodies, antigen binding fragments, and antibody drug conjugates, and methods of using the antibodies and antigen binding fragments as diagnostic reagents.
COMPOUNDS FOR POSITRON EMISSION TOMOGRAPHY
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Paragraph 0373-0375, (2016/12/26)
Described herein are compounds, compositions, and methods for diagnosing and/or monitoring pathogenic disease using positron emission tomography. Also described are conjugates of the formula B-L-P, wherein B is a radical of a targeting agent selected from vitamin receptor binding ligands (such as folate), PSMA binding ligands, or PSMA inhibitors; L is a divalent linker comprising aspartic acid, lysine, or arginine, and P is a radical of an imaging agent or radiotherapy agent, such as a radionuclide or radionuclide containing group, or a radical of a compound capable of binding a radionuclide, such as a metal chelating group.
Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
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Page/Page column 67, (2016/02/03)
Antiproliferative compounds having a structure represented by formula (II), where n, R1, R2, R3, R4, and R5 are as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody:
CYTOTOXIC PEPTIDES AND CONJUGATES THEREOF
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, (2015/07/07)
Disclosed herein are novel cytotoxic peptides of formula (I) as described herein: Formula (I) and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel cytotoxic peptide linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.
Asymmetric synthesis of 3,3,5,5-tetrasubstituted 1,2-dioxolanes: Total synthesis of epiplakinic acid F
Tian, Xiang-Yin,Han, Jian-Wei,Zhao, Qiong,Wong, Henry N. C.
supporting information, p. 3686 - 3700 (2014/06/09)
The first enantioselective total synthesis of epiplakinic acid F (1) was achieved through a pivotal step involving a radical-mediated asymmetric peroxidation of vinylcyclopropanes with molecular oxygen to construct highly substituted 1,2-dioxolanes. Subsequent conversions of the chiral 1,2-dioxolanes led to total synthesis of epiplakinic acid F (1) and the confirmation of its absolute configuration. The enantiomer of epiplakinic acid F methyl ester (2) was also prepared. This journal is the Partner Organisations 2014.
Synthesis and Evaluation of an Enantiomerically Enriched Bifunctional Chelator for 64Cu-Based Positron Emission Tomography (PET) Imaging
Chong, Hyun-Soon,Sun, Xiang,Zhong, Yongliang,Bober, Kamil,Lewis, Michael R.,Liu, Dijie,Ruthengael, Varyanna C.,Sin, Inseok,Kang, Chi Soo
, p. 1305 - 1313 (2015/10/05)
We report the synthesis and evaluation of an enantiomerically enriched bifunctional chelator, (S)-C-NE3TA. The bifunctional chelator was efficiently prepared by regioselective and stereoselective ring opening of an aziridinium ion. The new chiral chelator instantly and almost completely bound to 64Cu at room temperature. The corresponding 64Cu-radiolabeled complex remained intact in human serum for 48 h without any measurable transchelation and was tolerant to a rigorous EDTA challenge for 24 h. The 64Cu-radiolabeled (S)-C-NE3TA complex was stable in mice and produced an excellent biodistribution profile. The results of the in vitro and in vivo evaluations indicate that the new optically active chelator is a promising candidate for PET imaging applications.
New thiazole carboxamides as potent inhibitors of Akt kinases
Chang, Shaohua,Zhang, Zhang,Zhuang, Xiaoxi,Luo, Jinfeng,Cao, Xianwen,Li, Honglin,Tu, Zhengchao,Lu, Xiaoyun,Ren, Xiaomei,Ding, Ke
supporting information; experimental part, p. 1208 - 1212 (2012/03/11)
A new series of 2-substituted thiazole carboxamides were identified as potent pan inhibitors against all three isoforms of Akt (Akt1, Akt2 and Akt3) by systematic optimization of weak screening hit N-(1-amino-3-phenylpropan-2-yl)- 2-phenylthiazole-5-carboxamide (1). One of the most potent compounds, 5m, inhibited the kinase activities of Akt1, Akt2 and Akt3 with IC50 values of 25, 196 and 24 nM, respectively. The compound also potently inhibited the phosphorylation of downstream MDM2 and GSK3β proteins, and displayed strongly antiproliferative activity in prostate cancer cells. The inhibitors might serve as lead compounds for further development of novel effective anticancer agents.
Synthesis and anti-hepatitis B virus activities of Matijing-Su derivatives
Xu, Bixue,Huang, Zhengming,Liu, Changxiao,Cai, Zegui,Pan, Weidong,Cao, Peixue,Hao, Xiaojiang,Liang, Guangyi
experimental part, p. 3118 - 3125 (2009/09/25)
A series of derivatives of Matijing-Su (MTS, N-(N-benzoyl-l-phenylalanyl)-O-acetyl-l-phenylalanol) was synthesized and evaluated for their anti-hepatitis B virus (HBV) activities in 2.2.15 cells. The IC50 of compounds 9c (1.40 μM), 9g (2.33 μM) and 9n (2.36 μM), etc. and the selective index of 9n (45.93) of the inhibition on the replication of HBV DNA were higher than those of the positive control lamivudine [41.59, (IC50: 82.42 μM)]. Compounds 11d, 12a and 12e also exhibited significant anti-HBV activities.