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Shrestha, Aarajana,Park, Seojeong,Jang, Hae Jin,Katila, Pramila,Shrestha, Ritina,Kwon, Youngjoo,Lee, Eung-Seok Elsevier 2018 Bioorganic & medicinal chemistry Vol.26 No.18
<P><B>Abstract</B></P> <P>DNA Topoisomerase IIα (topo IIα) is one of the most effective therapeutic targets to control cancer. In an effort to develop novel and effective topo IIα targeting anti-proliferative agent, a phenolic series of indenopyridinone and indenopyridinol were designed and prepared using efficient multi-component one pot synthetic method. Total twenty-two synthesized compounds were assessed for topo I and IIα inhibition, and anti-proliferation in three different human cancer cell lines. Overall structure-activity relationship study explored the significance of <I>meta-</I>phenolic group at 4-position and <I>para-</I>phenolic group at 2- and/or 4-position of indenopyridinone skeleton for strong topo IIα-selective inhibition and anti-proliferative activity against human cervix (HeLa) and colorectal (HCT15) cell lines. Compound <B>12</B> with excellent topo IIα inhibition (93.7%) was confirmed as a DNA intercalator that could be a new promising lead to develop effective topo IIα-targeted anticancer agents.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Phenolic series of indenopyridinone were synthesized. </LI> <LI> SAR study was performed by comparing topo inhibitory and anti-proliferative activity. </LI> <LI> <I>para-</I>Phenolic group at 2- and/or 4-position of indenopyridinones is important. </LI> <LI> Compound <B>12</B> acted as DNA-intercalative potent topo IIα inhibitor. </LI> <LI> Indenopyridinone as potential scaffold for anticancer activity. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Aarajana Shrestha,,Ritina Shrestha,Sumin Lee,박필훈,Eung-Seok Lee 대한화학회 2021 Bulletin of the Korean Chemical Society Vol.42 No.3
6-Hydroxy-benzofuran-3-(2H)-ones exhibiting LPS stimulated ROS inhibition in RAW 264.7 macrophage
Katila, Pramila,Shrestha, Aastha,Shrestha, Aarajana,Shrestha, Ritina,Park, Pil-Hoon,Lee, Eung-Seok Elsevier 2019 Bioorganic chemistry Vol.87 No.-
<P><B>Abstract</B></P> <P>The design and synthesis of a series of thirty-two halogenated 1-tetralone or 6-amino-1-tetralone chalcone derivatives was achieved by the Claisen-Schmidt condensation reaction and were evaluated for their inhibitory effects against ROS production in LPS-stimulated RAW 264.7 macrophages. It was observed that the introduction of amino moiety into 1-tetralone skeleton greatly increased the inhibitory potency compared to corresponding 1-tetralone chalcones. Among the synthesized compounds, compound <B>18</B> which consists of 6-amino-1-tetralone skeleton together with <I>o</I>-fluorobenzylidene showed the most potent ROS inhibitory effect with IC<SUB>50</SUB> value of 0.25 ± 0.13 µM. SAR analysis revealed that amino moiety at the 6th position of 1-tetralone chalcones have an important role for exerting the greater ROS inhibitory potency in LPS-stimulated RAW 264.7 macrophages than those exhibited by 1-tetralone chalcones alone.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Halogenated 1-tetralone/6-amino-1-tetralone chalcone derivatives were synthesized. </LI> <LI> ROS Inhibitory effect in LPS-stimulated RAW 264.7 macrophages was examined. </LI> <LI> Compounds <B>18</B> showed the most potent ROS inhibition potency. </LI> <LI> Intro duction of amino group at the 6th position was enhanced the ROS inhibition. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Pramila Katila,Aastha Shrestha,아라자나쉬레스타,Ritina Shrestha,박필훈,이응석 대한화학회 2018 Bulletin of the Korean Chemical Society Vol.39 No.12
A new series of thirty-two fluorinated and/or hydroxylated 2-arylidene-1-indanone derivatives were systematically designed, synthesized, and evaluated for their inhibitory activity against LPS-stimulated ROS production in RAW 264.7 macrophages. 5/6-Fluoro-1-indanone or 4-, 5-, 6-, or 7-hydroxyindanone moiety along with ortho-, meta-, or para-hydroxyphenyl, furanyl or thiophenyl moiety was prepared and evaluated. Among the synthesized compounds, compound 11 possessing 6-hydroxy-1-indanone moiety along with 5-chlorothiophenyl moiety was found to have the most potent inhibitory effect on the production of ROS in LPS-stimulated RAW 264.7 macrophages with an IC50 value of 3.29??M.
Kadayat, Tara Man,Park, Seojeong,Shrestha, Aarajana,Jo, Hyunji,Hwang, Soo-Yeon,Katila, Pramila,Shrestha, Ritina,Nepal, Mahesh Raj,Noh, Keumhan,Kim, Sang Kyoon,Koh, Woo-Suk,Kim, Kil Soo,Jeon, Yong Hyun American Chemical Society 2019 Journal of medicinal chemistry Vol.62 No.17
<P>With the aim of developing new effective topoisomerase IIα-targeted anticancer agents, we synthesized a series of hydroxy- and halogenated 2,4-diphenyl indeno[1,2-<I>b</I>]pyridinols using a microwave-assisted single step synthetic method and investigated structure-activity relationships. The majority of compounds with chlorophenyl group at 2-position and phenol group at the 4-position of indeno[1,2-<I>b</I>]pyridinols exhibited potent antiproliferative activity and topoisomerase IIα-selective inhibition. Of the 172 compounds tested, <B>89</B> showed highly potent and selective topoisomerase IIα inhibition and antiproliferative activity in the nanomolar range against human T47D breast (2.6 nM) cancer cell lines. In addition, mechanistic studies revealed compound <B>89</B> is a nonintercalative topoisomerase II poison, and in vitro studies showed it had promising cytotoxic effects in diverse breast cancer cell lines and was particularly effective at inducing apoptosis in T47D cells. Furthermore, in vivo administration of compound <B>89</B> had significant antitumor effects in orthotopic mouse model of breast cancer.</P> [FIG OMISSION]</BR>