518299-08-6Relevant articles and documents
Isatin based thiosemicarbazide derivatives as potential inhibitor of α-glucosidase, synthesis and their molecular docking study
Hayat, Shawkat,Iqbal, Naveed,Khan, Khalid Mohammed,Nawaz, Muhammad,Qureshi, Faiza,Rab, Abdur,Rahim, Fazal,Shah, Syed Adnan Ali,Taha, Muhammad,Uddin, Imad,Uddin, Nizam,Wadood, Abdul,Zaman, Khalid
, (2020/07/25)
A new series of isatin based thiosemicarbazide derivatives 1–15 were synthesized and characterized by 1H NMR, 13C NMR and HR-EIMS. The synthetic derivatives were evaluated for α-glucosidase inhibitory potential. All compounds showed
Synthesis and biological evaluation of some N4-substituted 5-nitroisatin-3-thiosemicarbazones
Pervez, Humayun,Manzoor, Nazia,Yaqub, Muhammad,Nasim, Faiz-Ul-Hassan,Khan, Khalid M.
, p. 2251 - 2262 (2012/11/06)
A series of 5-nitroisatin-3-thiosemicarbazones 2a-2l was synthesised and evaluated for selected biological activities. The brine shrimp lethality bioassay was carried out to study their in vitro cytotoxicity potential and besides, their antifungal, phytotoxic and urease inhibitory effects were also investigated. Only compound 2j proved to be active in the brine shrimp assay exhibiting LD50 value 1.16 × 10-3 M. Compounds 2a and 2d displayed moderate antifungal activity (50 and 40%, respectively) against M. canis. Similarly, compound 2l exhibited moderate activity (40%) against the fungal strain, A. flavus. In phytotoxicity assay, all the synthesised compounds including the reference point 2m showed weak to moderate (20-60%) activity at the highest tested concentrations (1,000 μg and 500 μg/ml, respectively). In urease inhibition assay, compounds 2a, 2i and 2k proved to be potent inhibitors demonstrating pronounced inhibition with IC50 values 0.440, 0.901 and 27.880 μM, respectively. These compounds may act as leads for further studies. Springer Science+Business Media, LLC 2011.
Synthesis and primary cytotoxicity evaluation of new 5-nitroindole-2,3-dione derivatives.
Karali, Nilguen
, p. 909 - 918 (2007/10/03)
A new series of 5-nitro-1H-indole-2,3-dione-3-thiosemicarbazones (3a-k) obtained by condensation of 5-nitro-1H-indole-2,3-dione (1) with N-substituted-thiosemicarbazides (2a-k) were treated with morpholine or piperidine and formaldehyde to yield 1-morpholino/piperidinomethyl-5-nitroindole-2,3-dione-3-thiosemicarbazones (4a-m). The structures of all the compounds were determined by analytical and spectral (IR, 1H-NMR, EIMS) methods. Compounds 3b, 3c, 3f, 3k, 4a, 4c, 4f and 4l chosen as prototypes were evaluated in the National Cancer Institute's 3-cell line, one dose in vitro primary cytotoxicity assay. All the compounds that passed the criteria for activity in this assay were scheduled automatically for evaluation against the full panel of 60 human tumour cell lines at a minimum of five concentrations at 10-fold dilutions. Sulphorhodamine B (SRB) protein assay was used to estimate cell stability or growth. The most active compound was found to be 1-morpholinomethyl-5-nitroindole-2,3-dione-3-N-(chlorophenyl)thiosemicarbazone (4l). This compound demonstrated the most marked effects in the National Cancer Institute's 60 human tumour cell line in vitro screen on a non-small cell lung cancer cell line (HOP-62, log(10)GI(50) value -8.00) and on leukaemia cell lines (HL-60(TB), log(10)GI(50) value -6.30; MOLT-4, log(10)GI(50) value -6.18).
