108368-96-3Relevant academic research and scientific papers
CRM1 inhibitory and antiproliferative activities of novel 4′-alkyl substituted klavuzon derivatives
Kanbur, Tu??e,Kara, Murat,Kutluer, Meltem,?en, Ayhan,Delman, Murat,Alkan, Aylin,Ota?, Hasan Ozan,Ak?ok, ?smail,?a??r, Ali
, p. 4444 - 4451 (2017)
Klavuzons are 6-(naphthalen-1-yl) substituted 5,6-dihydro-2H-pyran-2-one derivatives showing promising antiproliferative activities in variety of cancer cell lines. In this work, racemic syntheses of nine novel 4′-alkyl substituted klavuzon derivatives were completed in eight steps and anticancer properties of these compounds were evaluated. It is found that size of the substituent has dramatic effect over the potency and selectivity of the cytotoxic activity in cancerous and healthy pancreatic cell lines. The size of the substituent can also effect the CRM1 inhibitory properties of klavuzon derivatives. Strong cytotoxic activity and CRM1 inhibition can be observed only when a small substituent present at 4′-position of naphthalen-1-yl group. However, these substituents makes the molecule more cytotoxic in healthy pancreatic cells rather than cancerous pancreatic cells. Among the tested compounds 1,2,3,4-tetrahydrophenanthren-9-yl substituted lactone was the most cytotoxic compound and its antiproliferative activity was also tested in 3D spheroids generated from HuH-7 cell lines.
Pd-catalyzed allylative dearomatisation using Grignard reagents
Boldrini, Cosimo,Harutyunyan, Syuzanna R.
supporting information, p. 11807 - 11810 (2021/11/30)
Pd-catalyzed allylative dearomatisation of naphthyl halides is shown to be feasible by employing Grignard reagents. The high reactivity of the nucleophile allows for fast reactions and low catalyst loading, while a plethora of successfully substituted compounds illustrate the broad scope. Five membered heteroaromatic compounds are also demonstrated to be reactive under similar conditions.
