69676-26-2Relevant academic research and scientific papers
Discovery and Biological Evaluations of Halogenated 2,4-Diphenyl Indeno[1,2- b]pyridinol Derivatives as Potent Topoisomerase IIα-Targeted Chemotherapeutic Agents for Breast Cancer
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,Jeong, Tae Cheon,Kwon, Youngjoo,Lee, Eung-Seok
supporting information, p. 8194 - 8234 (2019/10/11)
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-b]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-b]pyridinols exhibited potent antiproliferative activity and topoisomerase IIα-selective inhibition. Of the 172 compounds tested, 89 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 89 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 89 had significant antitumor effects in orthotopic mouse model of breast cancer.
Identification of novel 2-benzyl-1-indanone analogs as interleukin-5 inhibitors
Boggu, Pulla Reddy,Cho, Jungsuk,Kim, Youngsoo,Jung, Sang-Hun
, p. 65 - 75 (2018/05/03)
A novel series of 2-benzyl-1-indanone analogs were investigated as IL-5 inhibitory activity. Among the synthesized compounds, 7-(cyclohexylmethoxy)-2-(4-hydroxybenzyl)-2,3-dihydro-1H-inden-1-one (7s, 100.0% inhibition at 30 μM, IC50 = 4.0 μM), and 7-(cyclohexylmethoxy)-2-(3-hydroxybenzyl)-2,3-dihydro-1H-inden-1-one (7t, 95.0% inhibition at 30 μM, IC50 = 6.0 μM) showed the best inhibitory activity against IL-5. The 2-benzyl-1-indanone analogs showed moderate to strong IL-5 inhibitory activity. Especially, hydroxyl (HBD/HBA) substituent at position 3 or 4 on phenyl ring B showed potent IL-5 inhibition. Additionally, the bulky hydrophobic cyclohexylmethoxy group at position 7 of the 1-indanone ring is favorable for the inhibitory activity.
Studies on propafenone-type modulators of multidrug resistance VIII: Synthesis and pharmacological activity of indanon analogues
Salem,Richter,Hitzler,Chiba,Ecker
, p. 147 - 158 (2007/10/03)
A series of indanones with structural analogy to propafenone was synthesized and their MDR-modulating activity was measured using the daunomycin efflux assay. Structure-activity relationship studies showed a good correlation of pharmacological activity wi
Synthesis of Pyridobenzofurans
Sarbagya, D. P.,Rangachari, K.,Mazumdar, A. K. D.,Banerji, K. D.
, p. 891 - 893 (2007/10/02)
Some diarylpyridobenzofurans have been conveniently synthesised in 50-65percent yield by the condensation of 2-arylidene-6-methoxycoumaran-3-ones (III) with phenacylpyridinium halides in the presence of ammonium acetate.In a similar manner some 5-h
