- Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity
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The Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) is an enzyme that has been implicated as an important drug target in various therapeutic areas, including neurological disorders (Down syndrome, Alzheimer's disease), oncology, and
- Kumar, Kunal,Man-Un Ung, Peter,Wang, Peng,Wang, Hui,Li, Hailing,Andrews, Mary K.,Stewart, Andrew F.,Schlessinger, Avner,DeVita, Robert J.
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supporting information
p. 1005 - 1016
(2018/09/05)
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- Synthesis, crystal structure, molecular docking studies and bio-evaluation of some N4-benzyl-substituted isatin-3-thiosemicarbazones as urease and glycation inhibitors
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Fifteen N4-benzyl-substituted isatin-3-thiosemicarbazones 5a-o were synthesized and evaluated for their urease and glycation inhibitory potential. Lemna aequinocitalis growth and Artemia salina assays were also done to determine their phytotoxi
- Pervez, Humayun,Khan, Nazia,Iqbal, Jamshed,Zaib, Sumera,Yaqub, Muhammad,Tahir, Muhammad Nawaz,Naseer, Muhammad Moazzam
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- Synthesis and in vitro bio-activity evaluation of N4-benzyl substituted 5-chloroisatin- 3-thiosemicarbazones as urease and glycation inhibitors
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A series of fifteen N4-benzyl substituted 5-chloroisatin-3-thiosemicarbazones 5a-o were synthesized and screened mainly for their antiurease and antiglycation effects. Lemna aequinocitalis growth and Artemia salina assays were carried out to de
- Pervez, Humayun,Khan, Nazia,Iqbal, Jamshed,Zaib, Sumera,Yaqub, Muhammad,Naseer, Muhammad Moazzam
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p. 108 - 118
(2018/03/29)
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- Synthesis, X-ray molecular structure, biological evaluation and molecular docking studies of some N4-benzyl substituted 5-nitroisatin-3-thiosemicarbazones
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A series of fifteen N4-benzyl substituted 5-nitroisatin-3-thiosemicarbazones 5a–o was synthesized and evaluated for urease inhibitory, phytotoxic and cytotoxic influences. All the compounds proved to be highly potent inhibitors of the enzyme, s
- Pervez, Humayun,Khan, Nazia,Zaib, Sumera,Yaqub, Muhammad,Naseer, Muhammad Moazzam,Tahir, Muhammad Nawaz,Iqbal, Jamshed
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p. 1022 - 1029
(2017/02/05)
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- Synthesis and antiamoebic activity of 3,7-dimethyl-pyrazolo[3,4-e][1,2,4] triazin-4-yl thiosemicarbazide derivatives
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A series of 3,7-dimethyl-pyrazolo[3,4-e][1,2,4]triazin-4-yl thiosemicarbazide derivatives 3-22 were prepared and evaluated in vitro against HM1:1MSS strain of Entamoeba histolytica, to identify the compounds for antiamoebic activity. They exhibited antiamoebic activity in the range (IC 50 = 0.81-7.31 μM). The results were compared to the activity of known drug metronidazole. It is inferred from the in vitro studies that the compounds 10, 11, 17 and 18 were found to be significantly better inhibitors of E. histolytica since IC50 values in the μM range elicited by these compounds are much lower than metronidazole. Besides, compounds 11 and 17 have shown the most promising antiamoebic activity (IC50 = 0.81 μM of 11, IC50 = 0.84 μM of 17 versus IC50 = 1.81 μM of metronidazole). The study suggests the possibility of developing triazine analogues as potential drug candidates for antiamoebic activity.
- Singh, Shailendra,Husain, Kakul,Athar, Fareeda,Azam, Amir
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p. 255 - 262
(2007/10/03)
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