1391041-98-7Relevant articles and documents
Study on anti-proliferative effect of benzoxathiole derivatives through inactivation of NF-κB in human cancer cells
Venkateswararao, Eeda,Anh, Hoang Le Tuan,Sharma, Vinay K.,Lee, Ki-Cheul,Sharma, Niti,Kim, Youngsoo,Jung, Sang-Hun
supporting information; experimental part, p. 4523 - 4527 (2012/08/07)
To investigate the anti-proliferative effect of a newly discovered NF-kB inhibitor, 6,6-dimethyl-2-(phenylimino)-6,7-dihydrobenzo[d][1,3]oxathiol-4(5H)- one (1a), a series of its analogs (1b-n) were prepared and evaluated for their NF-κB inhibition and anti-proliferative activity against various human cancer cell lines. Slight variation of hydrophobicity by replacement of dimethyl group of 1a at 6-position with bulky isopropyl group and introduction of para-fluoro substitution on 2-phenyl group showed good NF-κB inhibitory activity and anti-proliferative activity. However, excessive increase in hydrophobicity with 2,4,6-trichloro substituents on phenyl group resulted in the loss of both the activities. From the SAR results, 2-phenylimino-6,7- dihydrobenzo[d][1,3]oxathiol-4(5H)-one was identified as the lead scaffold for investigating new anticancer agent through inactivation of NF-κB.