SYNTHESIS AND SPECTRAL STUDIES OF NITROSOUREA DERIVATIVES OF 6-BROMO AND 6-CHLORO-2,3-DIHYDRO-1,4-BENZOTHIAZINES AS POSSIBLE ANTICANCER AGENTS

1996 ◽  
Vol 2 (6) ◽  
Author(s):  
Dinesh Rai ◽  
Vandana Gupta ◽  
R.R. Gupta
2019 ◽  
Vol 19 (4) ◽  
pp. 439-452 ◽  
Author(s):  
Mohamed R. Selim ◽  
Medhat A. Zahran ◽  
Amany Belal ◽  
Moustafa S. Abusaif ◽  
Said A. Shedid ◽  
...  

Objective: Conjugating quinolones with different bioactive pharmacophores to obtain potent anticancer active agents. Methods: Fused pyrazolopyrimidoquinolines 3a-d, Schiff bases 5, 6a-e, two hybridized systems: pyrazolochromenquinoline 7 and pyrazolothiazolidinquinoline 8, different substituted thiazoloquinolines 13-15 and thiazolo[3,2-a]pyridine derivatives 16a-c were synthesized. Their chemical structures were characterized through spectral and elemental analysis, cytotoxic activity on five cancer cell lines, caspase-3 activation, tubulin polymerization inhibition and cell cycle analysis were evaluated. Results: Four compounds 3b, 3d, 8 and 13 showed potent activity than doxorubicin on HCT116 and three compounds 3b, 3d and 8 on HEPG2. These promising derivatives showed increase in the level of caspase-3. The trifloromethylphenyl derivatives of pyrazolopyrimidoquinolines 3b and 3d showed considerable tubulin polymerization inhibitory activity. Both compounds arrested cell cycle at G2/M phase and induced apoptosis. Conclusion: Compounds 3b and 3d can be considered as promising anticancer active agents with 70% of colchicine activity on tubulin polymerization inhibition and represent hopeful leads that deserve further investigation and optimization.


2014 ◽  
Vol 14 (7) ◽  
pp. 984-993 ◽  
Author(s):  
Gabriela Luna-Palencia ◽  
Federico Martinez-Ramos ◽  
Ismael Vasquez-Moctezuma ◽  
Manuel Fragoso-Vazquez ◽  
Jessica Mendieta-Wejebe ◽  
...  

1958 ◽  
Vol 80 (23) ◽  
pp. 6265-6271 ◽  
Author(s):  
Thomas P. Johnston ◽  
Lee B. Holum ◽  
John A. Montgomery

1991 ◽  
Vol 56 (4) ◽  
pp. 880-885 ◽  
Author(s):  
Oľga Hritzová ◽  
Dušan Koščík

Intramolecular hydrogen bonds of the N-H···O=C type have been detected in the derivatives of N-substituted N’-benzoyl- and N’-(2-chlorobenzoyl)thiourea on the basis of IR spectral studies. The title compounds can exist in two tautomeric forms.


Il Farmaco ◽  
1998 ◽  
Vol 53 (5) ◽  
pp. 342-345 ◽  
Author(s):  
Izabella Krȩżel

2016 ◽  
Vol 191 (9) ◽  
pp. 1209-1215 ◽  
Author(s):  
M. Velayutham Pillai ◽  
K. Rajeswari ◽  
C. Udhaya Kumar ◽  
C. Ramalingan ◽  
A. Manohar ◽  
...  

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