- Amide derivatives of 4-azaindole: Design, synthesis, and EGFR targeting anticancer agents
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A series of amide derivatives of azaindole-oxazoles (11a–n) were designed and synthesized and their structures were confirmed by 1HNMR, 13CNMR and mass spectral analysis. Further, these derivatives were screened for their anticancer activity against human cancer cell lines viz; MCF7 (breast), A549 (lung) and A375 (melanoma). In vitro anticancer activity screening indicated that most of the hybrids exhibited potent inhibitory activities in a variety of cancer cell lines. Among the compounds 11d, 11e, 11f, 11j, 11k, 11l, 11m, and 11n were exhibited more potent activity than standard, in those mainly two compounds 11m and 11j were exhibited excellent activity in MCF-7 cell line with IC50 values 0.034 and 0.036 μM. Moreover, all these compounds were carried out their molecular docking studies on EGFR receptor results indicated that two potent compounds 11m and 11j were strongly binds to protein EGFR (PDB ID: 4hjo). It was found that the energy calculations were in good agreement with the observed IC50 values.
- Venkat Swamy, Puli,Kiran Kumar, Vukoti,Radhakrishnam Raju, Ruddarraju,Venkata Reddy, Regalla,Chatterjee, Anindita,Kiran, Gangarapu,Sridhar, Gattu
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supporting information
p. 71 - 84
(2019/11/16)
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- Tryptophan-based fluorophores for studying protein conformational changes
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With the continuing interest in deciphering the interplay between protein function and conformational changes, small fluorescence probes will be especially useful for tracking changes in the crowded protein interior space. Presently, we describe the poten
- Talukder, Poulami,Chen, Shengxi,Liu, C. Tony,Baldwin, Edwin A.,Benkovic, Stephen J.,Hecht, Sidney M.
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supporting information
p. 5924 - 5934
(2015/01/09)
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- VIRAL REPLICATION INHIBITORS
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The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.
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Page/Page column 198
(2013/04/13)
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- 3-Amino-1-arylpropyl azaindoles and uses thereof
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The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
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Page/Page column 35
(2008/06/13)
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- THERAPEUTIC AGENTS I
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Compounds of formula(I), processes for preparing such compounds, their use in the treatment of obesity, psychiatric disorders, cognitive disorders, memory disorders, schizophrenia, epilepsy, and related conditions, and neurological disorders such as dementia, multiple sclerosis, Parkinson's disease, Huntington's chorea and Alzheimer's disease and pain related disorders, and pharmaceutical compositions containing them.
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Page/Page column 88
(2010/02/12)
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