844883-17-6Relevant academic research and scientific papers
Synthesis and evaluation of antiproliferative activity of novel quinazolin-4(3H)-one derivatives
Venkatesh, Ramineni,Kasaboina, Suresh,Janardhan, Sridhara,Jain, Nishant,Bantu, Rajashaker,Nagarapu, Lingaiah
, p. 2070 - 2081 (2016/10/03)
Two series of novel quinazolin-4(3H)-one derivatives (10a–g and 11a–g) have been synthesized and evaluated for their in vitro antiproliferative activity against human HeLa, MIAPACA, MDA-MB-231, and IMR-31 cancer cell lines. The synthesized compounds were characterized by spectral (Fourier transform infrared, 1H nuclear magnetic resonance, 13C nuclear magnetic resonance, high-resolution mass spectra) methods. Among them, compounds 11e and 11g exhibited potent in vitro antiproliferative activity with GI50 values 0.02, less than 0.01 μM against MIAPACA human cancer cell line. Significantly, compounds 10a, 10b, 10c, 10g, 11b, 11c, 11d, 11e, 11f showed activity with GI50 values ranging from 0.1 to 0.87 μM against human cancer cell lines MIAPACA, MDA-MB-231, and IMR-31. We have explored the probable binding mode and key active site interactions in HDAC8 and EHMT2 proteins. The docking results are complementary to the experimental results.
Synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers
Lee, Jie Eun,Koh, Hun Yeong,Seo, Seon Hee,Baek, Yi Yeon,Rhim, Hyewhon,Cho, Yong Seo,Choo, Hyunah,Pae, Ae Nim
scheme or table, p. 4219 - 4222 (2010/09/04)
T-type calcium channel is one of therapeutic targets for the treatment of cardiovascular diseases and neuropathic pain. In this study, as a part of our ongoing efforts to develop potent T-type calcium channel blockers, we designed oxazole derivatives subs
