A novel series of substituted pyrazolo-quinoline derivatives 7pa-7qg were synthesized efficiently by using molecular iodine in DMSO and further characterized based on H NMR, C NMR, IR and HRMS spectral studies. All the synthesized derivatives were screened for their in vitro cytotoxic activity against a panel of five different cancer cell lines such as A549, HeLa, SKNSH, HepG2 and MCF7. The compounds 7pc, 7pd, and 7pj exhibited considerable to promising anti-proliferative activity with IC values of 3.76, 3.87 and 3.83 µM against SKNSH cancer cell line. It was revealed that the compounds 7pa and 7pg have shown very close IC values of 2.43 and 6.01 µM, against A549 and MCF7 cancer cell lines respectively, which compared to positive control of Doxorubicin. This is the first report on the synthesis and in vitro anti-proliferative evaluation of pyrazolo-quinoline derivatives.
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http://dx.doi.org/10.1016/j.bmcl.2018.01.023 | DOI Listing |
Russ J Bioorg Chem
December 2022
Department of Pharmaceutical Chemistry, G. Pulla Reddy Pharmacy, 500028 Mehdipatnam, Hyderabad, Telangana India.
Unlabelled: We have synthesized novel pyrazolo-quinoline analogues (-) in an effort to create newer antitubercular drugs against the rising bacterial resistance NMR, IR and ESI-MS spectra were utilized to characterize the synthesised compounds. The antitubercular activity of the target compounds was evaluated against . Six derivatives () displayed very significant activity at 1.
View Article and Find Full Text PDFMol Divers
June 2023
Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, Anand, 388120, Gujarat, India.
An ultrasound-assisted green protocol for one-pot synthesis of a new series of pharmaceutically relevant pyrazolo quinoline derivatives (4a-t) were synthesized, characterized, and evaluated using DFT and biological activities. Pyrazolo quinoline derivatives (4a-t) were synthesized via a three-component tandem reaction of 1,3-dicarbonyl compound (1a-b), substituted aromatic aldehyde (2a-o), and 5-amino indazole (3a) in the presence of 1-butyl-3-methylimidazolium tetrafluoroborate [BMIM]BF ionic liquid in ethanol at ambient conditions. The main purpose of the present work is selective functionalization of pyrazolo quinoline (4a-t) core excluding another potential parallel reaction under environmentally benign reaction conditions.
View Article and Find Full Text PDFHeliyon
October 2021
Pharmaceutical Research Department, Nawah Scientific, Cairo, Egypt.
Tetrahydroquinoline () is an important structure for synthesizing multiple biologically active derivatives. Thus, we developed new quinoline derivatives and investigated them as anticancer agents. First, infrared spectroscopy, nuclear magnetic resonance spectroscopy, and other techniques were used to confirm the structure of synthesized compounds.
View Article and Find Full Text PDFBioorg Med Chem Lett
February 2018
Toxicology Unit, Pharmacology and Toxicology Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 007, Telangana, India.
A novel series of substituted pyrazolo-quinoline derivatives 7pa-7qg were synthesized efficiently by using molecular iodine in DMSO and further characterized based on H NMR, C NMR, IR and HRMS spectral studies. All the synthesized derivatives were screened for their in vitro cytotoxic activity against a panel of five different cancer cell lines such as A549, HeLa, SKNSH, HepG2 and MCF7. The compounds 7pc, 7pd, and 7pj exhibited considerable to promising anti-proliferative activity with IC values of 3.
View Article and Find Full Text PDFBiomacromolecules
February 2005
Faculty of Chemistry, Jagiellonian University, Ingardena 3, 30-060 Krakow, Poland.
Novel water-soluble polymeric photosensitizers based on the natural polymer dextran were synthesized and studied. The modified dextran contained photoactive anthracene (An) chromophores. They were soluble in water with the solubility decreasing with an increase in the number of An moieties bound to the polymeric chain.
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