659748-14-8Relevant academic research and scientific papers
3,4-Dihydroquinazoline derivatives inhibit the activities of cholinesterase enzymes
Park, Byeongyeon,Nam, Ji Hye,Kim, Jin Han,Kim, Hyoung Ja,Onnis, Valentina,Balboni, Gianfranco,Lee, Kyung-Tae,Park, Jeong Ho,Catto, Marco,Carotti, Angelo,Lee, Jae Yeol
, p. 1179 - 1185 (2017/06/19)
A series of 3,4-dihydroquinazoline derivatives consisting of the selected compounds from our chemical library on the diversity basis and the new synthetic compounds were in vitro tested for their inhibitory activities for both acetylcholinesterase (AChE, from electric eel) and butyrylcholinesterase (BChE, from equine serum) enzymes. It was discovered that most of the compounds displayed weak AChE and strong BuChE inhibitory activities. In particular, compound 8b and 8d were the most active compounds in the series against BChE with IC50 values of 45?nM and 62?nM, as well as 146- and 161-fold higher affinity to BChE, respectively. To understand the excellent activity of these compounds, molecular docking simulations were performed to get better insights into the mechanism of binding of 3,4-dihydroquinazoline derivatives. As expected, compound 8b and 8d bind to both catalytic anionic site (CAS) and peripheral site (PS) of BChE with better interaction energy values than AChE, in agreement with our experimental data. Furthermore, the non-competitive/mixed-type inhibitions of both compounds further confirmed their dual binding nature in kinetic studies.
Synthesis and SAR studies of a novel series of T-type calcium channel blockers
Park, Seong Jun,Park, Sung Jun,Lee, Min Joo,Rhim, Hyewhon,Kim, Yoonjee,Lee, Jung-Ha,Chung, Bong Young,Lee, Jae Yeol
, p. 3502 - 3511 (2007/10/03)
For the novel, potent, and selective T-type Ca2+ channel blockers, a series of sulfonamido-containing 3,4-dihydroquinazoline derivatives were prepared and evaluated for their blocking actions on T- and N-type Ca2+ channels. Among the
Growth inhibition of human cancer cells in vitro by T-type calcium channel blockers
Lee, Jae Yeol,Park, Seong Jun,Park, Sung Jun,Lee, Min Joo,Rhim, Hyewhon,Seo, Seon Hee,Kim, Ki-Sun
, p. 5014 - 5017 (2007/10/03)
This paper describes the preliminary biological results that novel T-type calcium channel blockers inhibit the growth of human cancer cells by blocking calcium influx into the cell, based on unknown mechanism on the cell cycle responsible for cellular proliferation. Among the selected compounds from compound library, compound 9c (KYS05041) was identified to be nearly equipotent with Cisplatin against some human cancers in the micromolar range.
3,4-Dihydroquinazoline derivatives as T-type calcium channel blockers and method of preparing the same
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Page/Page column 6-7, (2008/06/13)
The present invention relates to 3,4-dihydroquinazoline derivatives as T-type calcium channel blockers and a method of preparing the same. The present invention further relates to a composition comprising the same. The composition comprising the 3,4-dihyd
3,4-Dihydroquinazoline derivatives as T-type calcium channel blockers and method of preparing the same
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Page/Page column 4-5, (2008/06/13)
The present invention relates to 3,4-dihydroquinazoline derivatives as T-type calcium channel blockers and a method of preparing the same. The present invention further relates to a composition comprising the same. The composition comprising the 3,4-dihyd
Synthesis of 2-substituted 3,4-dihydroquinazoline derivatives via regioselective addition of a carbon nucleophile to a carbodiimide
Lee, Bum Hoon,Lee, Jae Yeol,Chung, Bong Young,Lee, Yong Sup
, p. 95 - 105 (2007/10/03)
Synthesis of 2-alkyl or phenyl-substituted 3,4-dihydroquinazoline derivatives (6) is described via regioselective carbon nucleophilic addition (RMgBr and RM) to a carbodiimide (4) followed by intramolecular conjugate addition.
3,4-Dihydroquinazoline derivatives as novel selective T-type Ca 2+ channel blockers
Lee, Yong Sup,Lee, Bum Hoon,Park, Seong Jun,Kang, Soon Bang,Rhim, Hyewhon,Park, Jin-Yong,Lee, Jung-Ha,Jeong, Seong-Woo,Lee, Jae Yeol
, p. 3379 - 3384 (2007/10/03)
For LVA T-type Ca2+ channel blockers, 3,4-dihydroquinazoline derivatives as new scaffolds were prepared and evaluated for the inhibitory activity against two members of the recombinant T-type Ca2+ channel family. Among them, 8a (KYS0
