5888-53-9Relevant articles and documents
Synthesis of targeted dibenzo[b,f]thiepines and dibenzo[b,f]oxepines as potential lead molecules with promising anti-breast cancer activity
Ansari, Mohd. Imran,Arun, Ashutosh,Chakravarti, Bandana,Hajela, K.,Hussain, Mohd. Kamil,Konwar, Rituraj
, p. 113 - 124 (2020/12/04)
A targeted library of substituted dibenzo[b,f]thiepines and dibenzo[b,f]oxepines (prototypes I, II and III), and structurally analogous to tamoxifen have been synthesized as a new class of anti-breast cancer agents. All the prototype molecules exhibited potential antiproliferative activity against ER + ve and ER-ve breast cancer cell lines. Dibenzo[b,f]thiepine prototypes were found to be more active. Of all the compound tested, 14b exhibited potent in-vitro antiproliferative activity at 1.33 μM and 5 μM concentration in MCF-7 and MDA-MB-231 cell lines and was devoid of any cytotoxicity in normal HEK cells even at 50 μM. Cell cycle analysis showed that the compound 14b inhibited cell proliferation due to G0/G1 arrest in MCF-7 cells. Annexin-V FITC and PI staining experiments confirmed that the cell inhibition was primarily due to apoptosis and not by necrosis, which was also supported by LDH release assay experiment. Molecular docking studies showed better binding interaction of the new dibenzo[b,f]thiepine analogue 14b with the estrogen receptor (ER) as compared to 4-hydroxy-tamoxifen and this enhanced binding might be responsible for its estrogen antagonistic activity that induces cell cycle arrest, apoptosis and inhibition of breast cancer cells.
Synthesis of the Polycyclic Ring Systems of Artocarpol A and D
Paduraru, M. Peggy,Wilson, Peter D.
, p. 4911 - 4913 (2007/10/03)
(Equation Presented) The first synthesis of the polycyclic ring systems of artocarpol A and D has been accomplished. These natural products were isolated recently from the root bark of Artocarpus rigida, and artocarpol A has been shown to have potent anti
1-aralkyl-1,2,4-triazoles
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, (2008/06/13)
This invention relates to 1 and 4-aralkyl-1,2,4-triazoles, their enantiomorphs, acid addition salts and metal salt complexes. This invention also relates to the method of preparation and use of these compounds. These compounds are highly active broad-spec