Matches in SemOpenAlex for { <https://semopenalex.org/work/W4281261716> ?p ?o ?g. }
- W4281261716 endingPage "105885" @default.
- W4281261716 startingPage "105885" @default.
- W4281261716 abstract "A series of novel cyanopyrimidine-hydrazone hybrids were synthesized and characterized with various spectroscopic techniques. The synthesized compounds were tested at NCI, USA, on a 60-cell line panel and most of the compounds showed remarkable cytotoxic activity against different cancer cell lines. Compound 5a was found to be the most potent compound of the series and it was further selected for five dose assays wherein it exhibited GI50 value of 0.414 µM and 0.417 µM against HOP-62 and OVCAR-4 cell lines respectively. The in-silico mechanistic studies indicated that these compounds are acting through inhibition of lysine specific demethylase 1 (LSD1) as evident from in to vitro LSD1 inhibition activity of compounds. Among various synthesized derivatives, compound 5a was found to have IC50-value of 0.956 µM. In addition, absorption, distribution, metabolism, excretion and toxicity profile (ADMET) was assessed for these novel derivatives to get an insight on their pharmacokinetic/dynamic attributes which revealed that synthesized compounds showed acceptable metabolic stability in human liver microsomes with minimal inhibition of cytochrome P450s (CYPs). The results indicated that compound 5a could be a promising lead compound for further development as a therapeutic agent for anticancer activity." @default.
- W4281261716 created "2022-05-23" @default.
- W4281261716 creator A5009796917 @default.
- W4281261716 creator A5010833213 @default.
- W4281261716 creator A5019169840 @default.
- W4281261716 creator A5035929598 @default.
- W4281261716 creator A5040093727 @default.
- W4281261716 creator A5044412832 @default.
- W4281261716 creator A5046942387 @default.
- W4281261716 creator A5055187070 @default.
- W4281261716 creator A5061863513 @default.
- W4281261716 creator A5071220673 @default.
- W4281261716 creator A5087972362 @default.
- W4281261716 date "2022-09-01" @default.
- W4281261716 modified "2023-09-29" @default.
- W4281261716 title "Synthesis, biological evaluation and docking studies of methylene bearing cyanopyrimidine derivatives possessing a hydrazone moiety as potent Lysine specific demethylase-1 (LSD1) inhibitors: A promising anticancer agents" @default.
- W4281261716 cites W1989853789 @default.
- W4281261716 cites W1993570389 @default.
- W4281261716 cites W2009867031 @default.
- W4281261716 cites W2010385215 @default.
- W4281261716 cites W2019712140 @default.
- W4281261716 cites W2025672266 @default.
- W4281261716 cites W2030547477 @default.
- W4281261716 cites W2033882650 @default.
- W4281261716 cites W2034084795 @default.
- W4281261716 cites W2035835337 @default.
- W4281261716 cites W2036480842 @default.
- W4281261716 cites W2068588554 @default.
- W4281261716 cites W2081567264 @default.
- W4281261716 cites W2087312216 @default.
- W4281261716 cites W2091399843 @default.
- W4281261716 cites W2112046350 @default.
- W4281261716 cites W2115187133 @default.
- W4281261716 cites W2135193909 @default.
- W4281261716 cites W2318969917 @default.
- W4281261716 cites W2323996569 @default.
- W4281261716 cites W2532165752 @default.
- W4281261716 cites W2557376112 @default.
- W4281261716 cites W2593436234 @default.
- W4281261716 cites W2604759877 @default.
- W4281261716 cites W2749853620 @default.
- W4281261716 cites W2755378295 @default.
- W4281261716 cites W2761191448 @default.
- W4281261716 cites W2767354780 @default.
- W4281261716 cites W2785854718 @default.
- W4281261716 cites W2795372495 @default.
- W4281261716 cites W2899515869 @default.
- W4281261716 cites W2908449964 @default.
- W4281261716 cites W2943121378 @default.
- W4281261716 cites W2946334140 @default.
- W4281261716 cites W2958658309 @default.
- W4281261716 cites W2994718880 @default.
- W4281261716 cites W2998692248 @default.
- W4281261716 cites W2999540553 @default.
- W4281261716 cites W3010409487 @default.
- W4281261716 cites W3022953708 @default.
- W4281261716 cites W3031755535 @default.
- W4281261716 cites W3033198654 @default.
- W4281261716 cites W3036663478 @default.
- W4281261716 cites W3037526368 @default.
- W4281261716 cites W3082335701 @default.
- W4281261716 cites W3087180116 @default.
- W4281261716 cites W3093834981 @default.
- W4281261716 cites W3109846914 @default.
- W4281261716 cites W3119005666 @default.
- W4281261716 cites W3128646645 @default.
- W4281261716 cites W3159870205 @default.
- W4281261716 cites W4212766227 @default.
- W4281261716 cites W4248107770 @default.
- W4281261716 cites W626649172 @default.
- W4281261716 doi "https://doi.org/10.1016/j.bioorg.2022.105885" @default.
- W4281261716 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/35636128" @default.
- W4281261716 hasPublicationYear "2022" @default.
- W4281261716 type Work @default.
- W4281261716 citedByCount "7" @default.
- W4281261716 countsByYear W42812617162022 @default.
- W4281261716 countsByYear W42812617162023 @default.
- W4281261716 crossrefType "journal-article" @default.
- W4281261716 hasAuthorship W4281261716A5009796917 @default.
- W4281261716 hasAuthorship W4281261716A5010833213 @default.
- W4281261716 hasAuthorship W4281261716A5019169840 @default.
- W4281261716 hasAuthorship W4281261716A5035929598 @default.
- W4281261716 hasAuthorship W4281261716A5040093727 @default.
- W4281261716 hasAuthorship W4281261716A5044412832 @default.
- W4281261716 hasAuthorship W4281261716A5046942387 @default.
- W4281261716 hasAuthorship W4281261716A5055187070 @default.
- W4281261716 hasAuthorship W4281261716A5061863513 @default.
- W4281261716 hasAuthorship W4281261716A5071220673 @default.
- W4281261716 hasAuthorship W4281261716A5087972362 @default.
- W4281261716 hasConcept C104317684 @default.
- W4281261716 hasConcept C159110408 @default.
- W4281261716 hasConcept C185592680 @default.
- W4281261716 hasConcept C202751555 @default.
- W4281261716 hasConcept C2776568683 @default.
- W4281261716 hasConcept C2777752112 @default.
- W4281261716 hasConcept C2780349576 @default.
- W4281261716 hasConcept C2781364455 @default.
- W4281261716 hasConcept C41091548 @default.