116734-25-9Relevant academic research and scientific papers
Exploration of quinolone and quinoline derivatives as potential anticancer agents
Iqbal, Jamshed,Ejaz, Syeda Abida,Khan, Imtiaz,Ausekle, Elina,Miliutina, Mariia,Langer, Peter
, p. 613 - 626 (2019)
Background: Among the different types of cancers, breast cancer, bone cancer and cervical cancer are the most common gender specific cancer types that are affecting the women worldwide. Currently, many enzymatic and cellular pathways are known as drug targets for the treatment of cancer. Even though many improvements have been made in the therapy of various types of cancer, but the major disadvantage of available anti-cancer drugs is their non-selective behavior towards cancer cells as well as normal cells. Objectives: In the light of this fact, the searching of new compounds with selective behavior only towards cancer cells is critically important. Previously, we have identified several series of compounds as the potential inhibitors of these families. Methods: Herein, we investigate quinolones and quinolines for their anti-cancer activity against breast cancer cells (MCF–7), bone marrow cancer cells (K–562) and cervical cancer cells (HeLa) by MTT assay. The most effective derivatives were further subjected to flow cytometry analysis followed by fluorescence microscopic analysis by using 4′,6-diamidine-2′-phenylindole (DAPI) and propidium staining (PI) staining. Results: All the tested compounds were found selective only towards cancer cells. The identified compounds also induced either G2 or S-phase cell cycle arrest within the respective cancer cell line, chromatin condensation and the nuclear fragmentation, as well as maximum interaction with DNA. Conclusions: These results provide evidence that the characteristic chemical features of attached groups are the key factors for their anticancer effects and play a useful role in revealing the mechanisms of action in relation to the known compounds in future research programs. [Figure not available: see fulltext.].
Quinolinic carboxylic acid derivatives as potential multi-target compounds for neurodegeneration: Monoamine oxidase and cholinesterase inhibition
Khan, Nehal A.,Khan, Imtiaz,Abid, Syed M. A.,Zaib, Sumera,Ibrar, Aliya,Andleeb, Hina,Hameed, Shahid,Iqbal, Jamshed
, p. 74 - 85 (2018)
Background: Parkinson's disease (PD), a debilitating and progressive disorder, is among the most challenging and devastating neurodegenerative diseases predominantly affecting the people over 60 years of age. Objectives: To confront PD, an advanced and op
Investigation of quinoline-4-carboxylic acid as a highly potent scaffold for the development of alkaline phosphatase inhibitors: Synthesis, SAR analysis and molecular modelling studies
Khan, Imtiaz,Shah, Syed Jawad Ali,Ejaz, Syeda Abida,Ibrar, Aliya,Hameed, Shahid,Lecka, Joanna,Millán, Jose Luis,Sévigny, Jean,Iqbal, Jamshed
, p. 64404 - 64413 (2015)
The role played by organic chemistry in the pharmaceutical industry continues to be one of the main drives in the drug discovery process. More than ever, the industry demands from organic chemists the development of small molecules, which could be a rich
SAR-based optimization of a 4-quinoline carboxylic acid analogue with potent antiviral activity
Das, Priyabrata,Deng, Xiaoyi,Zhang, Liang,Roth, Michael G.,Fontoura, Beatriz M.A.,Phillips, Margaret A.,De Brabander, Jef K.
supporting information, p. 517 - 521 (2013/07/26)
It is established that drugs targeting viral proteins are at risk of generating resistant strains. However, drugs targeting host factors can potentially avoid this problem. Herein, we report structure-activity relationship studies leading to the discovery
Quinoline-4-methyl esters as human nonpancreatic secretory phospholipase A2 inhibitors
Wu, Yiran,Chen, Zheng,Liu, Ying,Yu, Lanlan,Zhou, Lu,Yang, Suijia,Lai, Luhua
experimental part, p. 3361 - 3366 (2011/07/29)
A series of novel fused heterocycle methyl esters were designed and synthesized as human nonpancreatic secretory phospholipase A2 (hnps-PLA2) competitive inhibitors. Among the 22 synthesized compounds, 17 quinoline-4-methyl esters displayed hnps-PLA2 inhibition activity in the in vitro bioassay. The IC50 value for the best compound 3o was 1.5 μM. The structure-inhibition-activity relationships of the compounds were studied using molecular docking.
COMPOSITIONS AND METHODS FOR MODULATING GATED ION CHANNELS
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Page/Page column Sheet 8/15, (2010/11/27)
Disclosed are quinoline and quinazoline compounds which modulate the activity of the gated ion channels. Compounds that modulate these gated ion channels are useful in the treatment of diseases and disorders related to pain, inflammation, the neurological system, the gastrointestinal system and genitourinary system. Preferred compounds include quinoline or quinazoline derivatives substituted at the 4- position via N(H), C(O) or O moieties.
