7146-67-0Relevant articles and documents
Impact of N-substituents on crystal packing of N-alkyl-N′-tosylpiperazines and development of new polymorph of tosylbis(2-(tosyloxy)ethyl)amine: Synthesis, DFT, photophysical, cytotoxic property
Kadu, Rahul,Savani, Chirag,Roy, Hetal,Soni,Singh, Atresh Kumar,Vennapu, Dushyanth R.,Singh, Vinay K.
, (2020/11/25)
Diethanol amine (DEA) was selected as a lead compound to prepare N-tosyldiethanol amine 1, N-tosylbis(2-(tosyloxy)ethyl)amine 2 and disubstituted piperazines ca N-alkyl-N′-tosylpiperazines 3–5 in high yield. The new compounds were characterized by using relevant techniques viz. MS, IR, 1H, 13C, DEPT 135 NMR, UV–vis. absorption and fluorescence spectral studies. Single crystal X-ray diffraction technique was used to detect a new polymorphic form of 2 and to measure the influence of various N-substituents on the association of molecules of 3–5 in the solid state. Evidently, the introduction of N-cyclohexyl substituent in 3 successfully switches off all the synthons ca CH…O and CH…N seen in compound 4 and 5. Compounds 4 and 5 holding N-furfuryl and N-benzyl substituents, respectively, adopt other packing strategies based on CH…O, CH…N (4) and CH…O (5) interactions. The antitumor activity of 1–5 was evaluated in vitro against Hep 3B and IMR 32 by the MTT assay and the results were compared with cisplatin. Remarkably, some compounds were found extremely active against both the cell lines and proved to be more potent as cytotoxic agents than cisplatin. Density functional theory and molecular docking studies have been performed to rationalize the experimental results.
NOVEL CYTOTOXIC AGENTS AND CONJUGATES THEREOF
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Page/Page column 97, (2018/04/13)
Provided herein are novel maytansinoid compounds of general formula I. Also provided herein are conjugates comprising the compounds linked to a binding protein via a linker, and conjugating reagents comprising the compounds attached via a linker to at least one functional group capable of reacting with a binding protein. Also provided herein are pharmaceutical compositions comprising the compounds and conjugates, therapeutic methods and uses involving the compounds and conjugates, for example in cancer therapy, and novel synthetic processes.
Synthesis, biological evaluation and study of the effect of various N-substituents on the thermal stabilities of some new diethanolamine derivatives
Yar, Muhammad,Mushtaq, Nafeesa,Afzal, Sadia,Khan, Abdul Samad,Khan, Islam Ullah,Akhter, Muhammad Nadeem,Zareen, Seema,Shahzad, Sohail Anjum,Khan, Zulfiqar Ali,Raza Naqvi, Syed Ali,Mahmood, Nasir,Tahir, Lubna,Saleem, Muhammad
, p. 7297 - 7304 (2013/08/23)
Diethanolamine and its derivatives are of considerable interest in medicinal and other industrial products. A series of new diethanolamine derivatives has been synthesized and characterized by 1H NMR, 13C NMR, FTIR and mass spectrometry. All synthesized compounds have been tested for their in vitro antibacterial activity against pathogenic microorganisms Escherichia coli, Staphylococcus aureus, Micrococcus luteus, Pseudomonas aeruginosa, Bacillus subtilis, Pasteurrella mutocida, Rhizopus oryzae and Salmonella typhi. Among the tested compounds, compounds 2a, 2b, 2c, 3a and 4b have been found to be most potent members, which inhibited most of the pathogens used in the assay. Diethanolamine must posses tosyl or trifluoro groups in order to have good antimicrobial activities. All synthesized derivatives exhibited average FRAP activity and considerably good metal chelating activity and compound 2c showed excellent ABTS radical scavanging among all tested derivatives. Thermal stability and the effect of various N-protected groups on the thermal stability and degradation of selected diethanolamine derivatives (free flowing oils at room temperature and solid derivative 2a) has been studied by TGA and DSC analysis.
