Synthesis and Biological Evaluation of 6-[(1R)-1-Hydroxyethyl]-2,4a(R),6(S),8a(R)-tetrahydropyrano-[3,2-b]-pyran-2-one and Structural Analogues of the Putative Structure of Diplopyrone

2018 ◽  
Vol 84 (2) ◽  
pp. 666-678 ◽  
Author(s):  
Nicholas C. Lazzara ◽  
Robert J. Rosano ◽  
Purav P. Vagadia ◽  
Matthew T. Giovine ◽  
Mark W. Bezpalko ◽  
...  
MedChemComm ◽  
2019 ◽  
Vol 10 (8) ◽  
pp. 1445-1456 ◽  
Author(s):  
Casey J. Maguire ◽  
Graham J. Carlson ◽  
Jacob W. Ford ◽  
Tracy E. Strecker ◽  
Ernest Hamel ◽  
...  

Cyclic chalcones and structural analogues evaluated as cytotoxic agents.


2018 ◽  
Vol 83 (17) ◽  
pp. 10627-10635 ◽  
Author(s):  
Velayudham Ramadoss ◽  
Angel Josabad Alonso-Castro ◽  
Nimsi Campos-Xolalpa ◽  
César R. Solorio-Alvarado

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (05) ◽  
pp. 50-58
Author(s):  
P. V Bhagwanrao ◽  
◽  
P. G. Ingole ◽  
S. R Butle

We report a novel scaffold of 2-phenylpyrido[2,3-d]pyrimidine derivatives designed as structural analogues of dinaciclib. Sixteen derivatives were synthesised and evaluated for their CDK2/5 inhibition activity. Compounds 4-(2-(3-methoxybenzylidene)hydrazineyl)-2-phenylpyrido[2,3-d]pyrimidine (7i) and 4-(2-(3-nitrobenzylidene)hydrazineyl)-2-phenylpyrido[2,3-d]pyrimidine (7n) show promising IC50 and kinase selectivity. These compounds also show moderate anti-proliferative activity in the colon cancer HCT116 and breast cancer MCF7 cell lines. In molecular docking studies with CDK2, compounds 7i and 7nshow binding similar to dinaciclib.


2015 ◽  
Vol 101 ◽  
pp. 133-149 ◽  
Author(s):  
Katja Wiechmann ◽  
Hans Müller ◽  
Volker Huch ◽  
David Hartmann ◽  
Oliver Werz ◽  
...  

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