2023
DOI: 10.1007/s00044-022-03004-8
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Novel fluorinated pyrazole-based heterocycles scaffold: cytotoxicity, in silico studies and molecular modelling targeting double mutant EGFR L858R/T790M as antiproliferative and apoptotic agents

Abstract: Hepatocellular carcinoma (HCC), also known as hepatoma, is the most prevalent type of primary liver cancer. It begins in the hepatocytes, the liver’s major cell type. Cancer that began in another region of the body but has spread to the liver is known as secondary cancer of life; several still unmet demands for better, less toxic therapy to treat this malignant tumor. Several novel pyrazolo[1,5-a]pyrimidine derivatives were synthesized as part of our goal to develop promising anticancer drugs. All the synthesi… Show more

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Cited by 9 publications
(1 citation statement)
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“…The piperidine moiety, as the most prevalent, is found among 59% of FDA-approved small-molecule therapeutics that contain at least one azaheterocycle . On the other hand, the presence of C–F bonds is highly desirable in pharmaceuticals, where 20% of all marketed drugs possess at least one fluorine atom. , It is well established that fluorination of parent test compounds delivers candidates with improved bioavailability, metabolic stability, and lipophilicity (Figure A). Importantly, C–F bonds can be engaged in numerous non-covalent interactions (Figure B), which are relevant for achieving bioactivity …”
Section: Introductionmentioning
confidence: 99%
“…The piperidine moiety, as the most prevalent, is found among 59% of FDA-approved small-molecule therapeutics that contain at least one azaheterocycle . On the other hand, the presence of C–F bonds is highly desirable in pharmaceuticals, where 20% of all marketed drugs possess at least one fluorine atom. , It is well established that fluorination of parent test compounds delivers candidates with improved bioavailability, metabolic stability, and lipophilicity (Figure A). Importantly, C–F bonds can be engaged in numerous non-covalent interactions (Figure B), which are relevant for achieving bioactivity …”
Section: Introductionmentioning
confidence: 99%