C:Corrosive;
2824-46-6Relevant academic research and scientific papers
IMMUNOMODULATOR ANTIBODY DRUG CONJUGATES AND USES THEREOF
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Paragraph 00529-00532, (2020/12/30)
Provided herein are compounds, trifunctional antibody products thereof, and methods and pharmaceutical compositions for use in treatment of inflammatory and/or proliferative diseases.
HEMIASTERLIN DERIVATIVES FOR CONJUGATION AND THERAPY
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Paragraph 00264, (2016/08/23)
Provided herein are hemiasterlin derivatives, conjugates thereof, compositions comprising the derivatives or conjugates thereof, methods of producing the derivatives and conjugates thereof, and methods of using the derivatives, conjugates, and compositions for the treatment of cell proliferation. The derivatives, conjugates, and compositions are useful in methods of treatment and prevention of cell proliferation and cancer, methods of detection of cell proliferation and cancer, and methods of diagnosis of cell proliferation and cancer. In an embodiment, the hemiasterlin derivatives are according to Formula 1000: or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein Ar, L, W1, W4, W5, SG, and R are as described herein.
Highly selective fluorescence off-on probes for biothiols and imaging in live cells
Zhang, Di,Chen, Wei,Kang, Jianming,Ye, Yong,Zhao, Yufen,Xian, Ming
, p. 6837 - 6841 (2014/10/16)
Three sulfonyl benzothiazole-based fluorescent probes (RSHP1, RSHP2, and RSHP3) for the detection of biothiols (cysteine, homocysteine, and glutathione) are developed based on thiol-mediated nucleophilic aromatic substitutions. The probes exhibited good selectivity and sensitivity toward biothiols over other analytes. The probes were successfully applied for visualizing endogenous thiols in living cells. This journal is the Partner Organisations 2014.
Ring opening of pymisyl-protected aziridines with organocuprates
Bornholdt, Jan,Felding, Jakob,Clausen, Rasmus P.,Kristensen, Jesper L.
supporting information; experimental part, p. 12474 - 12480 (2010/12/25)
The pyrimidine-2-sulfonyl (pymisyl) group is introduced as a new protecting group that can be used to activate aziridines towards ring opening. It is readily introduced and removed under mild conditions. Regioselective ring opening of pymisyl-protected 2-methyl-aziridine with organocuprates gives the corresponding sulfonamides in high yields, and the pymisyl group can subsequently be removed upon treatment with a thiolate. The versatility of this new nitrogen protecting group is illustrated with a new synthesis of Selegiline, a monoamine oxidase-B inhibitor marketed for the treatment of Parkinson's disease. Easy on'easy off: The pymisyl group is introduced as a new protecting group for the activation of aziridines towards ring opening with organocuprates (see scheme). It is readily removed under very mild conditions with thiolates. The versatility of the approach is illustrated in a new synthesis of Selegiline, a drug marketed for the treatment of Parkinson's disease.
SELECTIVE HYDROXAMIC ACID BASED MMP-12 AND MMP-13 INHIBITORS
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Page/Page column 86-87, (2010/04/03)
The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/ or MMP- 13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).
Heterocyclic pentafluorophenyl sulfonate esters as shelf stable alternatives to sulfonyl chlorides
Bornholdt, Jan,Fj?re, Karianne Wilhemsen,Felding, Jakob,Kristensen, Jesper Langgaard
experimental part, p. 9280 - 9284 (2010/01/16)
Heterocyclic pentafluorophenyl sulfonate esters are shelf stable alternatives to the often less stable sulfonyl chlorides. They are easily prepared from thiols and react readily with primary and secondary amines to produce sulfonamides in high yields.
Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery
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Page/Page column 12, (2010/02/11)
A library of macrocyclic compounds of the formula (I) where part (A) is a (CH2)y—NH— bivalent radical, a —(CH2)y— bivalent radical or a covalent bond; where part (B) is a (CH2)z—NH— bivalent radical, a —(CH2)z— bivalent radical, or a covalent bond; where part (C) is a (CH2)t—NH— bivalent radical, a —(CH2)t— bivalent radical, or a covalent bond; and where part (T) is a —Y-L-Z— radical wherein Y is CH2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for their preparation of these compounds in a combinatorial manner, is also disclosed.
Synthesis of certain diarylsulfonylureas as antitumor agents
Youssef,Al-Abdullah,El-Khamees
, p. 404 - 418 (2007/10/03)
A new series of N-aryl-N′-heteroaryl or N,N′-diheteroaryl sulfonylurea or sulfonylthiourea was synthesized and screened for their antitumor activity at the National Cancer Institute (NCI). N-(3-Chlorophenyl)-N′-(6-methyl-uracil-2-sulfonyl)urea (28) with GI50, TGI, LC50 (MG-MID) values of 66.1, 83.2, 93.3 μM, respectively is the most active compound in this study. It showed a remarkable activity more than sulofenur against HL-60 (TB) and RPMI-8226 leukemia, HOP-92 Non small lung cancer, KM12 colon cancer, SF-295 CNS cancer, PC-3 prostate cancer, OVCAR-4 Ovarian cancer, CAKI-1 and UO-31 Renal cancer, and MDA-MB-435 Breast cancer with GI50 values of 0.3, 2.7, 6.9, 14.7, 8.2, 9.3, 2.0, 2.1, 3.4, 11.3 μM, respectively.
Solution-phase synthesis of a hindered N-methylated tetrapeptide using Bts-protected amino acid chlorides: Efficient coupling and methylation steps allow purification by extraction
Vedejs, Edwin,Kongkittingam, Chutima
, p. 2309 - 2318 (2007/10/03)
N-Benzothiazole-2-sulfonyl (Bts)-protected amino acid chlorides were used to prepare the hindered cyclosporin 8-11 tetrapeptide subunit 1. The synthesis was performed via 3a and the deprotected amines 5a, 13, and 19, including three repeated cycles involving N-methylation using iodomethane/potassium carbonate, deprotection of the Bts group, and N- acylation with a N-Bts-amino acid chloride such as 9b or 9c. Among three Bts cleavage methods compared (H3PO2/THF; NaBH4/EtOH; PhSH/K2CO3), the third gave somewhat higher overall yields. N-Acylation of 5a with the Bts-protected N-methylamino acid chloride 10b followed by deprotection was also highly efficient and could be used as an alternative route to 11. Each of the deprotected amines was isolated without chromatography using simple extraction methods to remove neutral byproducts. The tetrapeptide 1 was obtained in analytically pure form as the monohydrate.
N-heteroarenesulfonyl-protected amino acid reagents for peptide synthesis
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, (2008/06/13)
This invention relates to the use of heteroarenesulfonyl groups as protecting groups for amino groups, particularly the amino groups of amino acids, and specifically to nitrogen-protected (N-protected) amino acid reagents, which are particularly well-suited for use in peptide syntheses. In particular, the N-protected amino acid reagent is an N-heteroarenesulfonyl-protected amino acid halide. The heteroarenesulfonyl protecting groups are readily removed under relatively mild conditions.
