(3-Oxo-1,2,3,4-tetrahydro-2-quinoxalinyl)acetic acid
CAS Number:
136584-14-0
Molecular Formula:
C10H10N2O3
Allocolchicinoids bearing a Michael acceptor fragment for possible irreversible binding of tubulin
Literature Information
Publication Date
2020-06-04
DOI
10.1039/D0MD00060D
Impact Factor
0
Authors
Ekaterina S. Sazanova, Iuliia A. Gracheva, Diane Allegro, Pascale Barbier, Elena V. Svirshchevskaya, Alexey Yu Fedorov
View Original
Abstract
We describe an attempt to apply the concept of covalent binding towards the highly active allocolchicinoids selected on the basis of SAR analysis of previously synthesized molecules. To achieve the irreversible binding of the agent to the cysteine residues of the colchicine site of tubulin protein, we synthesized a number of new allocolchicinoids bearing the acceptor moiety. Some of the new derivatives possess cytotoxic activity against COLO-357, BxPC-3, HaCaT, and HEK293 cell lines in a low nanomolar range of concentrations. A substoichiometric mode of microtubule assembly inhibition was demonstrated. The most active compounds possess close to colchicine general toxicity on mice.
Recommended Journals
Related Literature
Penning spectroscopy and structure of acetylene oligomers in He nanodroplets
S. Mandal, R. Gopal, M. Shcherbinin, A. D’Elia, H. Srinivas, R. Richter, B. Bapat, S. R. Krishnan, V. Sharma
2020-04-21
Paper
DOI: 10.1039/D0CP00689K
Gas phase reactions of iodide and bromide anions with ozone: evidence for stepwise and reversible reactions‡
Mahendra Bhujel, David L. Marshall, Alan T. Maccarone, Benjamin I. McKinnon, Adam J. Trevitt, Gabriel da Silva, Stephen J. Blanksby, Berwyck L. J. Poad
2020-04-27
Paper
DOI: 10.1039/D0CP01498B
Low-index dielectric metasurfaces supported by metallic substrates for efficient second-harmonic generation in the blue-ultraviolet range
Kwang-Hyon Kim
2020-02-29
Paper
DOI: 10.1039/D0CP00150C
Atomistic insights into the separation mechanism of multilayer graphene membranes for water desalination
Jing Zhang, Chen Chen, Jianuan Pan, Li Zhang, Lijun Liang, Zhe Kong, Xinping Wang, Wei Zhang, Jia-Wei Shen
2020-03-03
Paper
DOI: 10.1039/D0CP00071J
Oxygen surface exchange kinetics of Ba0.5Sr0.5Co0.8Fe0.2O3−δ
V. A. Eremin, M. V. Ananyev, H. J. M. Bouwmeester, E. Kh. Kurumchin, Ch.-Y. Yoo
2020-04-29
Paper
DOI: 10.1039/C9CP06650K
Negative magnetization, complex magnetic ordering and applications of Cr-doped Co2TiO4
Q. S. Fu, X. H. Chen, C. Chakrabarti, C. L. Li, J. Zheng, P. J. Wang, H. X. Yin, Y. Qiu, B. Meng, S. L. Yuan
2020-02-28
Paper
DOI: 10.1039/C9CP06444C
Distinct microscopic mechanisms for the accelerated aggregation of pathogenic Tau mutants revealed by kinetic analysis
Liu Hong
2020-03-17
Paper
DOI: 10.1039/C9CP06083A
Prediction of aqueous free energies of solvation using coupled QM and MM explicit solvent simulations
J. Samuel Arey
2020-03-30
Paper
DOI: 10.1039/D0CP00582G
Gate voltage impact on charge mobility in end-on stacked conjugated oligomers
Miroslav Menšík, Petr Toman, Cheng-Han Chung, Chimed Ganzorig, Jiří Pfleger
2020-03-25
Paper
DOI: 10.1039/C9CP06477J
The energetics of carbonated PuO2 surfaces affects nanoparticle morphology: a DFT+U study
Samuel Moxon, Adam R. Symington, Joshua S. Tse, James Dawson, Joseph M. Flitcroft, Stephen C. Parker, David J. Cooke, Robert M. Harker, Marco Molinari
2020-03-11
Paper
DOI: 10.1039/D0CP00021C
You might also like
Compound Q&A
What are the main uses of 1-(3-Aminophenyl)-3-[(3R)-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-(2-pyridinyl)-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]urea (CAS: 155412-88-7)?
This compound is mainly used as an intermediate in the synthesis of antipsychoti...
155412-88-71-(3-Aminophenyl)-3-...
Compound Q&A
How should waste containing 1-(D-Ribofuranosyl)-1,4-dihydro-3-pyridinecarboxamide (CAS: 19132-12-8) be handled?
Waste containing 1-(D-Ribofuranosyl)-1,4-dihydro-3-pyridinecarboxamide (CAS: 191...
19132-12-81-(D-Ribofuranosyl)-...
Compound Q&A
What regulatory guidelines apply to 2-Methyl-2-propanyl 3-bromo-3-(hydroxymethyl)-1-azetidinecarboxylate (CAS: 2007919-81-3)?
2-Methyl-2-propanyl 3-bromo-3-(hydroxymethyl)-1-azetidinecarboxylate (CAS: 20079...
2007919-81-32-Methyl-2-propanyl ...
Compound Q&A
What is N-(4-Chloro-2-pyridinyl)acetamide (CAS: 245056-66-0)?
N-(4-Chloro-2-pyridinyl)acetamide (CAS: 245056-66-0) is a chemical compound with...
245056-66-0N-(4-Chloro-2-pyridi...
Compound Q&A
What is 5-Chloro-2-hydroxybenzoic acid (CAS: 321-14-2)?
5-Chloro-2-hydroxybenzoic acid, also known as 5-chlorosalicylic acid, is an arom...
321-14-25-Chloro-2-hydroxybe...
Compound Q&A
What precautions should be taken when handling 1,1-Dichloro-1-fluoroethane (CAS: 1717-00-6)?
When handling 1,1-Dichloro-1-fluoroethane (CAS: 1717-00-6), it is important to u...
1717-00-61,1-Dichloro-1-fluor...
Compound Q&A
What are the physical and chemical properties of Fmoc-(2S,3R)-3-phenylpyrrolidine-2-carboxylic acid (CAS: 281655-32-1)?
Fmoc-(2S,3R)-3-phenylpyrrolidine-2-carboxylic acid is a white crystalline solid ...
281655-32-1Fmoc-(2S,3R)-3-pheny...
Compound Q&A
What are the main uses of 4-Amino-5-bromo-2-pyridinecarboxylic acid (CAS: 1363381-01-4)?
4-Amino-5-bromo-2-pyridinecarboxylic acid is primarily used as a precursor in th...
1363381-01-44-Amino-5-bromo-2-py...
Compound Q&A
What precautions should be taken when handling (S)-tert-butyl 2-((2-(4-bromophenyl)-2-oxoethyl)carbamoyl)pyrrolidine-1-carboxylate (CAS: 1007881-98-2)?
Handling this compound should be done with personal protective equipment (PPE) i...
1007881-98-2(S)-tert-butyl 2-((2...
Compound Q&A
What precautions should be taken when handling 8-bromo-2,2-dimethyl-3,4-dihydro-2H-1,4-benzoxazin-3-one (CAS: 688363-73-7)?
When handling 8-bromo-2,2-dimethyl-3,4-dihydro-2H-1,4-benzoxazin-3-one, use prop...
688363-73-78-bromo-2,2-dimethyl...
Source Journal
Recommended Compounds
2-(4-Chlorophenyl)-4-(dimethylamino)-2-(2-(dimethylamino)ethyl)butanenitrile
CAS Number:
1246816-57-8
Molecular Formula:
C16H24ClN3
![2,6-Di(thiophen-2-yl)dithieno[3,2-b:2',3'-d]thiophene structure](https://static.chemtradehub.com/structs/910/910788-24-8-5b70.webp "2,6-Di(thiophen-2-yl)dithieno[3,2-b:2',3'-d]thiophene structure")
2,6-Di(thiophen-2-yl)dithieno[3,2-b:2',3'-d]thiophene
CAS Number:
910788-24-8
Molecular Formula:
C16H8S5
![Methyl 4-({[(2-methyl-2-propanyl)oxy]carbonyl}amino)bicyclo[2.2.2]octane-1-carboxylate structure](https://static.chemtradehub.com/structs/943/943845-74-7-b7e5.webp "Methyl 4-({[(2-methyl-2-propanyl)oxy]carbonyl}amino)bicyclo[2.2.2]octane-1-carboxylate structure")
Methyl 4-({[(2-methyl-2-propanyl)oxy]carbonyl}amino)bicyclo[2.2.2]octane-1-carboxylate
CAS Number:
943845-74-7
Molecular Formula:
C15H25NO4
Recommended Suppliers
Disclaimer
This page provides academic journal information for reference and research purposes only. We are not affiliated with any journal publishers and do not handle publication submissions. For publication-related inquiries, please contact the respective journal publishers directly.
If you notice any inaccuracies in the information displayed, please contact us at support@chemtradehub.com. We will promptly review and address your concerns.