Design, synthesis and biological evaluation of 6‐substituted quinolines derived from cabozantinib as c‐Met inhibitors
Sign Up to like & getrecommendations! Published in 2019 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.201900101
Abstract: Based on the cabozantinib scaffold, novel c‐Met inhibitors were rationalized from the limited knowledge of structure‐activity relationships for the quinoline 6‐position. Emphasis was given to modifications capable of engaging in additional polar interactions with the… read more here.
Keywords: design synthesis; biological evaluation; met inhibitors; substituted quinolines ... See more keywords
Design, synthesis and biological evaluation of substituted aminopyridazin-3(2H)-ones as G0/G1-phase arresting agents with apoptosis-inducing activities.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.09.077
Abstract: A series of aminopyridazin-3(2H)-one derivatives has been designed and synthesized. Their antiproliferative activities were evaluated against three human cancer cell lines (SH-SY5Y human neuroblastoma, K562 human myelogenous leukemia and AGS gastric cancer cell lines) using… read more here.
Keywords: design synthesis; phase; evaluation substituted; biological evaluation ... See more keywords
Structural Modification and Pharmacological Evaluation of Substituted Quinoline-5,8-diones as Potent NSD2 Inhibitors.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01920
Abstract: The histone lysine methyltransferase NSD2 is overexpressed, translocated, or mutated in multiple types of cancers and has emerged as an attractive therapeutic target. However, the development of small-molecule NSD2 inhibitors is still in its infancy,… read more here.
Keywords: modification pharmacological; structural modification; nsd2 inhibitors; substituted quinoline ... See more keywords
Stereoselective Synthesis and Evaluation of C6″-Substituted 5a-Carbasugar Analogues of SL0101 as Inhibitors of RSK1/2.
Sign Up to like & getrecommendations! Published in 2017 at "Organic letters"
DOI: 10.1021/acs.orglett.7b00945
Abstract: A convergent synthesis of 5a-carbasugar analogues of the n-Pr-variant of SL0101 is described. The analogues were synthesized in an effort to find compounds with potent in vivo efficacy in the inhibition of p90 ribosomal s6… read more here.
Keywords: stereoselective synthesis; carbasugar analogues; synthesis evaluation; evaluation substituted ... See more keywords
Design and in vitro biological evaluation of substituted chalcones synthesized from nitrogen mustards as potent microtubule targeted anticancer agents
Sign Up to like & getrecommendations! Published in 2017 at "New Journal of Chemistry"
DOI: 10.1039/c7nj00265c
Abstract: A new series of p-[N,N-bis(2-chloroethyl)amino]benzaldehyde substituted chalcone derivatives were designed and synthesized, and their structures were characterized by spectroscopic techniques and single crystal XRD studies. Compounds 3a–f crystallized in the triclinic system with a centrosymmetric… read more here.
Keywords: biological evaluation; anticancer agents; design vitro; vitro biological ... See more keywords
Design, synthesis and biological evaluation of N-substituted α-hydroxyimides and 1,2,3-oxathiazolidine-4-one-2,2-dioxides with anticonvulsant activity
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2019.1651722
Abstract: Abstract In this investigation, we studied a family of compounds with an oxathiazolidine-4-one-2,2-dioxide skeleton and their amide synthetic precursors as new anticonvulsant drugs. The cyclic structures were synthesized using a three-step protocol that include solvent-free… read more here.
Keywords: design synthesis; biological evaluation; oxathiazolidine one; synthesis biological ... See more keywords
Design, synthesis and evaluation of 2, 6, 8-substituted Imidazopyridine derivatives as potent PI3Kα inhibitors
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2022.2155638
Abstract: Abstract Inhibition of PI3K pathway has become a desirable strategy for cancer treatment. In this work, a series of 2, 6, 8-substituted Imidazo[1,2-a]pyridine derivatives were designed and screened for their activities against PI3Kα and a… read more here.
Keywords: substituted imidazopyridine; design synthesis; derivatives potent; evaluation substituted ... See more keywords
Synthesis and biological evaluation of 3-O-substituted 1-benzyl-6-oxo-1,6-dihydropyridazine derivatives
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Chemical Research"
DOI: 10.1177/1747519819866402
Abstract: On the basis of 2-benzyl-6-hydroxypyridazin-3(2H)-one, a series of its novel O-substituted (including 6-(1,3,5-triazin-2-yl)oxy) derivatives is prepared. It is proven that the substitution reactions in the initial compound occur mainly at the oxygen atom of the… read more here.
Keywords: dihydropyridazin oxy; biological evaluation; oxo dihydropyridazin; benzyl oxo ... See more keywords
Synthesis and Biological Evaluation of 2-Substituted Benzyl-/Phenylethylamino-4-amino-5-aroylthiazoles as Apoptosis-Inducing Anticancer Agents
Sign Up to like & getrecommendations! Published in 2020 at "Molecules"
DOI: 10.3390/molecules25092177
Abstract: Induction of apoptosis is a common chemotherapeutic mechanism to kill cancer cells The thiazole system has been reported over the past decades as a building block for the preparation of anticancer agents. A novel series… read more here.
Keywords: biological evaluation; anticancer agents; anticancer; synthesis biological ... See more keywords