228574-88-7Relevant academic research and scientific papers
Hybrid Quinazoline 1,3,5-Triazines as Epidermal Growth Factor Receptor (EGFR) Inhibitors with Anticancer Activity: Design, Synthesis, and Computational Study
Pathak, Prateek,Rimac, Hrvoje,Grishina, Maria,Verma, Amita,Potemkin, Vladimir
, p. 822 - 838 (2021)
We report a series of hybrid quinazoline-1,3,5-triazine derivatives as EGFR inhibitors, which were synthesised and tested by using a variety of in vitro, in silico, and in vivo techniques. The derivatives were found to be active against different cancer cell lines and nontoxic against normal ones, with compounds 7 c, 7 d, 7 e, and 7 j being the most potent ones. The derivatives were also evaluated for angiogenesis inhibition potency in chicken eggs, and molecular docking and dynamics simulation studies were carried out to elucidate the fundamental substituent groups essential for their bioactivity. Additionally, a SAR study of the derivatives was performed for future compound optimisation. These studies suggested that the derivatives have a high affinity towards EGFR with favourable pharmacological properties. The most active compound (7 e) was further evaluated for in vivo anticancer activity against DMBA-induced tumours in female Sprague-Dawley rats as well as its effects on plasma antioxidant status, biotransformation enzymes, and lipid profile. The study suggested that 7 e has lead properties against breast cancer and can serve as a starting compound for further development of anti-EGFR compounds.
Discovery of new 1,3,5-triazine scaffolds with potent activityagainst Mycobacterium tuberculosis H37Rv
Sunduru, Naresh,Gupta, Leena,Chaturvedi, Vinita,Dwivedi, Richa,Sinha, Sudhir,Chauhan, Prem M.S.
experimental part, p. 3335 - 3345 (2010/08/06)
A series of eighty one 2,4,6-trisubstituted-1,3,5-triazines were synthesized and evaluated in vitro for the growth inhibition of Mycobacterium tuberculosis H37Rv. Fifteen compounds from this series exhibited good to moderate activity with an MIC in the ra
Synthesis and bioevaluation of hybrid 4-aminoquinoline triazines as a new class of antimalarial agents
Kumar, Ashok,Srivastava, Kumkum,Raja Kumar,Puri,Chauhan, Prem M.S.
scheme or table, p. 6530 - 6533 (2009/09/06)
The emergence and rapid spread of chloroquine resistant strains of Plasmodium falciparum has dramatically reduced the chemotherapeutic options. Towards this goal, a series of new class of hybrid 4-aminoquinoline triazines were synthesized and screened aga
