5888-53-9Relevant academic research and scientific papers
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, receptor affinity and effect on pentylenetetrazole-induced seizure threshold of novel benzodiazepine analogues: 3-Substituted 5-(2-phenoxybenzyl)-4H-1,2,4-triazoles and 2-amino-5-(phenoxybenzyl)-1,3,4- oxadiazoles
Mashayekh, Siavash,Rahmanipour, Narges,Mahmoodi, Behnaz,Ahmadi, Fatemeh,Motaharian, Dina,Shahhosseini, Soraya,Shafaroodi, Hamed,Banafshe, Hamid R.,Shafiee, Abbas,Navidpour, Latifeh
, p. 1929 - 1937 (2014/03/21)
The new series of 5-(2-phenoxybenzyl)-4H-1,2,4-triazoles, possessing C-3 thio, alkylthio and ethoxy substituents, and 2-amino-5-(2-phenoxybenzyl)-1,3,4- oxadiazoles were designed and synthesized as novel benzodiazepine analogues. Most of them revealed sim
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
Substituted (2-Phenoxyphenyl)acetic Acids with Antiinflammatory Activity. 1
Atkinson, David C.,Godfrey, Keith E.,Meek, Bernard,Saville, John F.,Stillings, Michael R.
, p. 1353 - 1360 (2007/10/02)
The synthesis and antiinflammatory activity of a series of substituted (2-phenoxyphenyl)acetic acids are described.Initial screening in the adjuvant arthritis test showed that halogen substitution in the phenoxy ring enhanced activity considerably.Ulcerogenic potential, as measured by the minimum ulcerogenic dose (MUD), was low in almost all the acids tested. acetic acid possessed the most favorable combination of potency with low toxicity, including ulcerogenicity, and this compound is now in therapeutic use.
Cyanoaralkylheterocyclic compounds
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, (2008/06/13)
This invention relates to phenoxy, phenylthio, phenylsulfinyl and phenylsulfonyl substituted cyano aralkyl imidazoles and triazoles, their enantiomorphs, acid addition salts and metal salt complexes thereof as well as their methods of preparation and use
