42048-23-7Relevant academic research and scientific papers
Rational design and synthesis of 2-anilinopyridinyl-benzothiazole Schiff bases as antimitotic agents
Shaik, Thokhir B.,Hussaini, S.M. Ali,Nayak, V. Lakshma,Sucharitha, M. Lakshmi,Malik, M. Shaheer,Kamal, Ahmed
supporting information, p. 2549 - 2558 (2017/05/09)
Based on our previous results and literature precedence, a series of 2-anilinopyridinyl-benzothiazole Schiff bases were rationally designed by performing molecular modeling experiments on some selected molecules. The binding energies of the docked molecules were better than the E7010, and the Schiff base with trimethoxy group on benzothiazole moiety, 4y was the best. This was followed by the synthesis of a series of the designed molecules by a convenient synthetic route and evaluation of their anticancer potential. Most of the compounds have shown significant growth inhibition against the tested cell lines and the compound 4y exhibited good antiproliferative activity with a GI50 value of 3.8?μM specifically against the cell line DU145. In agreement with the docking results, 4y exerted cytotoxicity by the disruption of the microtubule dynamics by inhibiting tubulin polymerization via effective binding into colchicine domain, comparable to E7010. Detailed binding modes of 4y with colchicine binding site of tubulin were studied by molecular docking. Furthermore, 4y induced apoptosis as evidenced by biological studies like mitochondrial membrane potential, caspase-3, and Annexin V-FITC assays.
PVP-Pd nanoparticles as efficient catalyst for nitroarene reduction under mild conditions in aqueous media
Uberman, Paula M.,García, Carolina S.,Rodríguez, Julieta R.,Martín, Sandra E.
supporting information, p. 739 - 748 (2017/05/19)
The catalytic activity of PVP-Pd nanoparticles synthesized by electrochemical methods was explored in nitroaromatic hydrogenation reaction. In this transformation, the colloidal nanocatalyst proved to have outstanding catalytic activity under sustainable reaction conditions. This mild process efficiently reduced the nitroaromatic group at room temperature, without high pressure of molecular hydrogen and in aqueous medium. Furthermore, several functional groups were tolerated, given the corresponding substituted arylamines in excellent yields and with high TOF. In addition, one-pot reactions and tandem process were explored, in which nitroaromatic hydrogenation reaction was included in the synthesis of modified amines. This methodology was effectively incorporated in tandem reactions and one-pot procedures, achieving N-arylamines functionalized in good isolated yields. Finally, comparison of sustainable chemistry metrics analysis demonstrated that this methodology is a reliable approach to perform the nitro compound hydrogenation process.
Synthesis of 2-anilinopyridine dimers as microtubule targeting and apoptosis inducing agents
Kamal, Ahmed,Ali Hussaini,Lakshma Nayak,Shaheer Malik,Lakshmi Sucharitha,Shaik, Thokhir Basha,Ashraf, Md.,Bagul, Chandrakant
, p. 6755 - 6767 (2015/02/02)
A series of 2-anilinopyridine dimers have been synthesized and evaluated for their anticancer potential. Most of the compounds have showed significant growth inhibition of the cell lines tested and compound 4d was most effective amongst the series display
Azabenzimidazole Compounds
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Paragraph 0206; 0208, (2014/09/03)
The present invention is directed to compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein.
The Preparation of All the Monochloro-α-carbolines and the Assignment of the 13C N.M.R. Spectrum of α-Carboline
Mohamed, Murtedsa bin,Parrick, John
, p. 577 - 593 (2007/10/02)
The five previously unknown chloro-α-carbolines are prepared, the 1H n.m.r. spectra of the chloro-α-carbolines are described, and the 13C n.m.r. spectrum of α-carboline is assigned.
